Title of Invention	A PROCESS FOR PREPARATION OF MONTELUCAST INTERMEDIATE
Abstract	The process for producing 2-[1-(hydroxymethyl)-cyclopropane] acetic acid with steps of: a) reacting 1,1-cyclopropanedimethanol with aldehydes or acetals of aldehydes in solvents or without solvent using acidic catalyst at elevated temperature with azeotropic removal of water to form benzylidene acetal; b) opening of benzylidene acetal with N-halo succinimide or 1,3-dihalo-5, 5-dimethyl hydantoine using radical initiator in solvent at elevated temperature to obtain (halomethyl) cyclopropanemethyl benzoate; and c) conversion of 1-(halomethyl0 cyclopropanemethyl benzoate to 1-(benzoyloxymethyl) cyclopropane acetonitrile followed by hydrolysis under alkaline condition to obtain (hydroxymethyl) cycloproppane acetic acid.

Title of Invention

A PROCESS FOR PREPARATION OF MONTELUCAST INTERMEDIATE

Abstract

The process for producing 2-[1-(hydroxymethyl)-cyclopropane] acetic acid with steps of: a) reacting 1,1-cyclopropanedimethanol with aldehydes or acetals of aldehydes in solvents or without solvent using acidic catalyst at elevated temperature with azeotropic removal of water to form benzylidene acetal; b) opening of benzylidene acetal with N-halo succinimide or 1,3-dihalo-5, 5-dimethyl hydantoine using radical initiator in solvent at elevated temperature to obtain (halomethyl) cyclopropanemethyl benzoate; and c) conversion of 1-(halomethyl0 cyclopropanemethyl benzoate to 1-(benzoyloxymethyl) cyclopropane acetonitrile followed by hydrolysis under alkaline condition to obtain (hydroxymethyl) cycloproppane acetic acid.

Full Text	FORM 2 THE PATENTS ACT, 1970 COMPLETE SPECIFICATION SECTION 10; RULE 13 INVENTION RELATES TO AN IMPROVEMENT IT PROCESS FOR PRODUCING 1- (hydroxymethyl) cyclopropane acetic acid, an intermediate of Montelukast, a Leucotriene D4 antagonist inhibitor and its derivatives with better yield, high- purity and in shorter reaction time. CENTAUR CHEMICALS PRIVATE LIMITED (a company incorporated under companies act, 1956) at Centaur House, Shantinagar, Vakola, Santacruz (East), Mumbai - 400 055, State of Maharashtra, India The following specification particularly describes the nature of this invention and the matter in which it is to be performed : Improved process for producing 1- (hydroxymethyl)cyclopropane acetic acid, an intermediate of Montelukast, Field of Invention. The present invention relates to an improved process for producing ]-(hydroxymethyl)cyclopropane acetic acid, an intermediate of Montelukast, a Leucotriene D4 antagonist inhibitor and its derivatives. Background of Invention. Montelukast is a Leucotriene D4 antagonist inhibitor of Leucotriene biosynthesis with anti-asthamatic properties. The synthesis of Montelukast involves preparation of an intermediate 2-[1-(hydroxymethyl)-cyclopropane] acetonitrile or its corresponding acid or ester, which in turn is converted to l-(mercaptomethyl)cyclopropane acetic acid. The starting material for this intermediate is 1,1-cyclopropanedimethanol. European Patent 0480717 describe the process for preparation of methyl ester of 2-[l- (hydroxymethyl)cyclopropane] acetic acid. The process involves monobenzoylation of 1,1-cyclopropanedimethanol with benzoyl chloride-pyridine in methylene chloride at 10°C temperature. Under these conditions mixture of mono and dibenzoyl derivative is obtained, which on purification through column chromatography results 47% yield of desired monobenzoyl derivative. The monobenzoyl derivative upon treatment with methanesulfonyl chloride followed by sodium cyanide treatment and hydrolysis with potassium hydroxide produces 2-[1-(hydroxymethyl)-cyclopropane] acetic acid, which is then converted to methyl ester using diazomethane and is purified through column chromatography. The primary disadvantage of this process is the low yield in the first step, which also involves purification through column chromatography. The benzoyl chloride reaction and methanesulfonyl chloride reaction required low temperature (-10° C &-400 C respectively)- The ester finally obtained is also purified by column chromatography. The PCT document No.95/18107 describes the process for preparations of 2-[l-(hydroxymethyl) cyclopropane] acetonitrile via cyclic sulfite using thionyl chloride. The reaction is carried out at low temperature and the overall yield of this process is less due to formation of complicated mixture of cyclic sulfite and other by-products. Further more, it also involves use of corrosive chemicals, such as, thionyl chloride in the process. The document published by Merck Research in Synthetic Communications 27(4),701-704 (1997) described further improvement for preparation of cyclic sulfite using sulfite diester, such as, isopropyl sulfite. However, this process also involves handling of thionyl chloride. Nevertheless, development of more advantageous process for producing 2-[l-(hydroxymethyl) cyclopropane] acetic acid is still desirable. SUMMARY OF THE INVENTION. The present invention relates to improved process for producing 2-p-(hydroxymethyl)cyclopropane] acetic acid. The key step of the process involves preparation of benzylidene derivative of 1,1-cyclopropanedimethanol followed by selective ring opening using N-bromosuccinimide. DETAILED DESCRIPTION OF THE INVENTION. The improved process for producing 2-[1- (hydroxymethyl)cyclopropane] acetic acid envisaged according to the present invention is given in Scheme-I hereunder: In process envisaged in accordance with the Scheme-I hereinabove, U-cyclopropanedimethanol is converted into benzylidene derivative using benzaldehyde in cylcohexane at reflux temperature using p-Tolunesulfonic acid as catalyst. The aldehydes used may be aromatic aldehyde, substituted or unsubstituted. The reaction can be carried out using acetals of aldehyde. The preferred aldehyde is benzaldehyde. The solvent may be aromatic or aliphatic hydrocarbon, tetrahydrofuran, ether, acetonitrile, dimethyl sulfoxide either alone or in combination. The preferred solvent is cyclohexane. The reaction can also be carried out without a solvent. The preferred temperature is between 0 - 150° C and more preferably between 50°- 100°C. The suitable acid catalyst used in the method of present invention include inorganic acids like hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, aliphatic acids like formic acid, propionic acid, maleic acid, etc. hydroxy acids or diacids, aliphatic or aromatic sulfonic acids and the salts thereof. The acidic ion exchange resin can also be employed as catalyst. The cyclic benzylidene derivative is then treated with N-bromosuccinimide at reflux temperature in dichloroethane using benzoyl peroxide as the catalyst to obtain bromo benzoyl derivative. N-Bromosuccinimide may be replaced with other halogenating agents, such as, dihalodimethyl hydantoins. The benzoyl peroxide may be substituted by other peroxides or AIBN or the reaction may also be initiated without catalyst. The bromobenzoyl derivative is then converted into cyanobenzoyl derivative using sodium cyanide or potassium cyanide in organic solvent followed by hydrolysis with alkali like sodium hydroxide or potassium hydroxide to obtain 2-[l-(hydroxymethyl)cyclopropane] acetic acid. Examples that follow will illustrate the present invention in greater detail without in any way limiting the scope of the invention. Example 1. Preparation of 5-cyclopropyl-2-phenyl-l ,3-dioxane. A solution of U-cyclopropanedimethanol (5 Kg, 49 moles), benzaldehyde (6 Kg, 56.6 moles), p-toluene sulfonic acid (30g, 0.17moles) in cyclohexane (25 L) was refluxed with azeotropic removal of water for 6 to 8 hrs. The solution was cooled to 25°-30°C, washed with water (10 L). Distillation of cyclohexane followed by removal of excess benzaldehyde under reduced pressure yielded cyclopropyl-2-phenyl-l ,3-dioxane (8.5-9.0 Kg, 86-96%). Example 2. Preparation of 1-(Bromomethyl)cyclopropane methyl benzoate. To the stirred solution of N-bromosuccinimide (9 Kg, 50.6moles), dibenzoyl peroxide (50g, 0.2moles) in dichloroethane (45 L) under reflux was charged solution of 5-cyclopropyl-2-phenyl-l,3-dioxane (9 Kg, 47.6moles) in dichloroethane (18 L) under reflux during 2 hrs. The solution was cooled to 10° C, washed with water (10 L), 1% aqueous sodium thiosulfate solution (10 L) followed by water (10 L) and concentrated to remove dichloroethane completely to yield 1-(Bromomethyl)cyclopropane methyl benzoate (12 Kg, 94 %). Example 3. Preparation of t-(benzoyloxymethyl) cyclopropane acetonitrile. To the stirred solutions of l-(bromomethyl) cyclopropanemethyl benzoate (12 Kg, 44.6 moles) in dimethyl sulfoxide (40 L) was added sodium cyanide ( 2.4 Kg, 49 moles). The solution was heated to 55-65° C for 2 to 3 hrs. and then cooled to 10°C, diluted with water (10 L) and extracted with toluene ( 3 x 15 L). Combined toluene layer was washed with water (2 x 10 L) and taken directly for next stage. Example 4 Preparation of H hydroxy methyl) cyclopropane acetonitrile. To the stirred toluene solution of example 3 at 0-5° C was added methanolic solution of KOH ( 3.37 Kg, 60.1 moles) in 15 L methanol. The reaction mass was stirred for 1 hr. at 0-5° C. The lower layer containing product was separated. Toluene layer was extracted with 25% aqueous methanol (3 x 4.5 L) and finally with 1.5 L water. Combined lower layer containing product was diluted with water (20 L), extracted with n-hexane. Aqueous layer was then extracted with ethylacetate (4 x 20 L). Combined ethyl acetate layer was washed with brine solution (10 L) and taken directly to next stage. Example 5 Preparation of 2-n-(hydroxymethyl) cyclopropane] acetic acid. The stirred solution of 2-[l-(hydroxymethyl) cyclopropane] acetonitrile in methanol (20 L) & water (20 L) and potassium hydroxide (9 Kg, 160.7 moles) was refluxed for 4 to 5 hrs. The methanol was removed under reduced pressure and concentrated HCI was added dropwise at 0-5° C to pH 1. The solution was extracted with ethyl acetate (5 x 20 L). Combined ethyl acetate layer was washed with brine solution (10 L) and concentrated under reduced pressure. Isopropyl ether (15 L) was charged to the residue and solution was cooled to 0-5° C and maintained for 2 hours and filtered to yield 2.4 Kg of 2-(l-hydroxymethyl)cyclopropane)acetic acid. We claim 1) A process for producing 2-[t-(hydroxymethyl)-cyclopropane] acetic acid comprising : a) reacting 1,1-cyclopropanedimethanol with aldehydes or acetals of aldehydes in solvents or without solvent using acidic catalyst at elevated temperature with azeotropic removal of water to form benzylidene acetal; b) opening of benzylidene acetal with N-halo succinimide or 1,3-dihalo-5, 5-dimethyl hydantoine using radical initiator in solvent at elevated temperature to obtain (halomethyl) cyclopropanemethyl benzoate; c) conversion of 1-(halomethyl) cyclopropanemethyl benzoate to 1-(benzoyloxymethyl)cyclopropane acetonitrile followed by hydrolysis under alkaline condition to obtain (hydroxymethyl) cyclopropane acetic acid. 2) A process as claimed in claim 1, wherein the aldehyde used include substituted or unsubstituted aromatic aldehydes or its acetals. 3) A process as claimed in claim 1, wherein the acidic catalyst used include inorganic acids, such as hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid or aliphatic acids like formic acid, propionic acid, maleic acid or substituted or unsubstituted hydroxyacids or diacids or aliphatic or aromatic sulfonic acids or its salts, solid catalyst like acidic ion exchange resins, heteropolyacids, zeotiles. 4) A process as claimed in claim 1, wherein the acidic catalyst can be used alone or in any suitable combination. The reaction can also be carried out without using acidic catalyst. 5) A process as claimed in claim 1, wherein the said solvent used include aliphatic or aromatic hydrocarbon, tetrahydrofuran, ethers, acetonitrile, dimethylsulfoxide, either alone or in suitable combinations. 6) A process as claimed in claim 1 a, the temperature of said reaction is between 25°C- 150°C preferably at temperature ranging between 50°C to 100°C. 7} A process as claimed in claim 1 a, can also be carried out without azeotropic removal of water. 8) A process as claimed in claim 1, wherein the radical initiator catalyst used include substituted or unsubstituted aromatic or aliphatic peroxides like -benzoyl peroxide, di-tert-butyl hydroperoxide , lauryl peroxide or AIBN. Dated this 14th day of October, 2005 ABSTRACT OF THE INVENTION The process for producing 2-[l-(hydroxymethyl)- cyclopropane] acetic acid with steps of : a) reacting 1,1- cyclopropanedimethanol with aldehydes or acetals of aldehydes in solvents or without solvent using acidic catalyst at elevated temperature with azeotropic removal of water to form benzylidene acetal; b) opening of benzylidene acetal with N-halo succinimide or 1,3-dihalo-5, 5-dimethyl hydantoine using radical initiator in solvent at elevated temperature to obtain (halomethyl) cyclopropanemethyl benzoate; and c) conversion of 1-(halomethyl) cyclopropanemethyl benzoate to 1-(benzoyloxymethyl)cyclopropane acetonitrile followed by hydrolysis under alkaline condition to obtain (hydroxymethyl) cyclopropane acetic acid.

Full Text

FORM 2

THE PATENTS ACT, 1970
COMPLETE SPECIFICATION SECTION 10; RULE 13
INVENTION RELATES TO AN IMPROVEMENT IT
PROCESS FOR PRODUCING 1-
(hydroxymethyl) cyclopropane acetic acid, an intermediate of Montelukast, a Leucotriene D4 antagonist inhibitor and its derivatives with better yield, high- purity and in shorter reaction time.
CENTAUR CHEMICALS PRIVATE LIMITED (a company incorporated under companies act, 1956) at Centaur House, Shantinagar, Vakola, Santacruz (East), Mumbai - 400 055, State of Maharashtra, India
The following specification particularly describes the nature of this invention and the matter in which it is to be performed :

Improved process for producing 1-
(hydroxymethyl)cyclopropane acetic acid,
an intermediate of Montelukast,
Field of Invention.
The present invention relates to an improved process for producing ]-(hydroxymethyl)cyclopropane acetic acid, an intermediate of Montelukast, a Leucotriene D4 antagonist inhibitor and its derivatives.
Background of Invention.
Montelukast is a Leucotriene D4 antagonist inhibitor of Leucotriene biosynthesis with anti-asthamatic properties. The synthesis of Montelukast involves preparation of an intermediate 2-[1-(hydroxymethyl)-cyclopropane] acetonitrile or its corresponding acid or ester, which in turn is converted to l-(mercaptomethyl)cyclopropane acetic acid.
The starting material for this intermediate is 1,1-cyclopropanedimethanol.

European Patent 0480717 describe the process for
preparation of methyl ester of 2-[l-
(hydroxymethyl)cyclopropane] acetic acid. The process involves monobenzoylation of 1,1-cyclopropanedimethanol with benzoyl chloride-pyridine in methylene chloride at 10°C temperature. Under these conditions mixture of mono and dibenzoyl derivative is obtained, which on purification through column chromatography results 47% yield of desired monobenzoyl derivative. The monobenzoyl derivative upon treatment with methanesulfonyl chloride followed by sodium cyanide treatment and hydrolysis with potassium hydroxide produces 2-[1-(hydroxymethyl)-cyclopropane] acetic acid, which is then converted to methyl ester using diazomethane and is purified through column chromatography. The primary disadvantage of this process is the low yield in the first step, which also involves purification through column chromatography. The benzoyl chloride reaction and methanesulfonyl chloride reaction required low temperature (-10° C &-400 C respectively)- The ester finally obtained is also purified by column chromatography.

The PCT document No.95/18107 describes the process for preparations of 2-[l-(hydroxymethyl) cyclopropane] acetonitrile via cyclic sulfite using thionyl chloride. The reaction is carried out at low temperature and the overall yield of this process is less due to formation of complicated mixture of cyclic sulfite and other by-products. Further more, it also involves use of corrosive chemicals, such as, thionyl chloride in the process.
The document published by Merck Research in Synthetic Communications 27(4),701-704 (1997) described further improvement for preparation of cyclic sulfite using sulfite diester, such as, isopropyl sulfite. However, this process also involves handling of thionyl chloride.
Nevertheless, development of more advantageous process for producing 2-[l-(hydroxymethyl) cyclopropane] acetic acid is still desirable.

SUMMARY OF THE INVENTION.
The present invention relates to improved process for producing 2-p-(hydroxymethyl)cyclopropane] acetic acid.
The key step of the process involves preparation of benzylidene derivative of 1,1-cyclopropanedimethanol followed by selective ring opening using N-bromosuccinimide.
DETAILED DESCRIPTION OF THE INVENTION.
The improved process for producing 2-[1-
(hydroxymethyl)cyclopropane] acetic acid envisaged
according to the present invention is given in Scheme-I
hereunder:

In process envisaged in accordance with the Scheme-I hereinabove, U-cyclopropanedimethanol is converted into benzylidene derivative using benzaldehyde in cylcohexane at reflux temperature using p-Tolunesulfonic acid as catalyst.
The aldehydes used may be aromatic aldehyde, substituted or unsubstituted. The reaction can be carried out using acetals of aldehyde. The preferred aldehyde is benzaldehyde. The solvent may be aromatic or aliphatic hydrocarbon, tetrahydrofuran, ether, acetonitrile, dimethyl sulfoxide either alone or in combination. The preferred solvent is cyclohexane. The reaction can also be carried out without a solvent.

The preferred temperature is between 0 - 150° C and more preferably between 50°- 100°C.
The suitable acid catalyst used in the method of present invention include inorganic acids like hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, aliphatic acids like formic acid, propionic acid, maleic acid, etc. hydroxy acids or diacids, aliphatic or aromatic sulfonic acids and the salts thereof. The acidic ion exchange resin can also be employed as catalyst.
The cyclic benzylidene derivative is then treated with N-bromosuccinimide at reflux temperature in dichloroethane using benzoyl peroxide as the catalyst to obtain bromo benzoyl derivative.
N-Bromosuccinimide may be replaced with other halogenating agents, such as, dihalodimethyl hydantoins. The benzoyl peroxide may be substituted by other peroxides or AIBN or the reaction may also be initiated without catalyst.

The bromobenzoyl derivative is then converted into cyanobenzoyl derivative using sodium cyanide or potassium cyanide in organic solvent followed by hydrolysis with alkali like sodium hydroxide or potassium hydroxide to obtain 2-[l-(hydroxymethyl)cyclopropane] acetic acid.
Examples that follow will illustrate the present invention in greater detail without in any way limiting the scope of the invention.
Example 1.
Preparation of 5-cyclopropyl-2-phenyl-l ,3-dioxane.
A solution of U-cyclopropanedimethanol (5 Kg, 49 moles), benzaldehyde (6 Kg, 56.6 moles), p-toluene sulfonic acid (30g, 0.17moles) in cyclohexane (25 L) was refluxed with azeotropic removal of water for 6 to 8 hrs. The solution was cooled to 25°-30°C, washed with water (10 L). Distillation of cyclohexane followed by removal of excess benzaldehyde

under reduced pressure yielded cyclopropyl-2-phenyl-l ,3-dioxane (8.5-9.0 Kg, 86-96%).
Example 2.
Preparation of 1-(Bromomethyl)cyclopropane methyl benzoate.
To the stirred solution of N-bromosuccinimide (9 Kg, 50.6moles), dibenzoyl peroxide (50g, 0.2moles) in dichloroethane (45 L) under reflux was charged solution of 5-cyclopropyl-2-phenyl-l,3-dioxane (9 Kg, 47.6moles) in dichloroethane (18 L) under reflux during 2 hrs. The solution was cooled to 10° C, washed with water (10 L), 1% aqueous sodium thiosulfate solution (10 L) followed by water (10 L) and concentrated to remove dichloroethane completely to yield 1-(Bromomethyl)cyclopropane methyl benzoate (12 Kg, 94 %).
Example 3.
Preparation of t-(benzoyloxymethyl) cyclopropane
acetonitrile.

To the stirred solutions of l-(bromomethyl) cyclopropanemethyl benzoate (12 Kg, 44.6 moles) in dimethyl sulfoxide (40 L) was added sodium cyanide ( 2.4 Kg, 49 moles). The solution was heated to 55-65° C for 2 to 3 hrs. and then cooled to 10°C, diluted with water (10 L) and extracted with toluene ( 3 x 15 L). Combined toluene layer was washed with water (2 x 10 L) and taken directly for next stage.
Example 4
Preparation of H hydroxy methyl) cyclopropane acetonitrile.
To the stirred toluene solution of example 3 at 0-5° C was added methanolic solution of KOH ( 3.37 Kg, 60.1 moles) in 15 L methanol. The reaction mass was stirred for 1 hr. at 0-5° C. The lower layer containing product was separated. Toluene layer was extracted with 25% aqueous methanol (3 x 4.5 L) and finally with 1.5 L water. Combined lower layer containing product was diluted with water (20 L), extracted with n-hexane. Aqueous layer was then extracted with ethylacetate (4 x 20 L). Combined ethyl acetate layer was washed with brine solution (10 L) and taken directly to next stage.

Example 5
Preparation of 2-n-(hydroxymethyl) cyclopropane] acetic acid.
The stirred solution of 2-[l-(hydroxymethyl) cyclopropane] acetonitrile in methanol (20 L) & water (20 L) and potassium hydroxide (9 Kg, 160.7 moles) was refluxed for 4 to 5 hrs. The methanol was removed under reduced pressure and concentrated HCI was added dropwise at 0-5° C to pH 1. The solution was extracted with ethyl acetate (5 x 20 L). Combined ethyl acetate layer was washed with brine solution (10 L) and concentrated under reduced pressure. Isopropyl ether (15 L) was charged to the residue and solution was cooled to 0-5° C and maintained for 2 hours and filtered to yield 2.4 Kg of 2-(l-hydroxymethyl)cyclopropane)acetic acid.
We claim
1) A process for producing 2-[t-(hydroxymethyl)-cyclopropane] acetic acid comprising :

a) reacting 1,1-cyclopropanedimethanol with
aldehydes or acetals of aldehydes in solvents or
without solvent using acidic catalyst at elevated
temperature with azeotropic removal of water to
form benzylidene acetal;
b) opening of benzylidene acetal with N-halo succinimide or 1,3-dihalo-5, 5-dimethyl hydantoine using radical initiator in solvent at elevated temperature to obtain (halomethyl) cyclopropanemethyl benzoate;
c) conversion of 1-(halomethyl) cyclopropanemethyl benzoate to 1-(benzoyloxymethyl)cyclopropane acetonitrile followed by hydrolysis under alkaline condition to obtain (hydroxymethyl) cyclopropane acetic acid.

2) A process as claimed in claim 1, wherein the aldehyde used include substituted or unsubstituted aromatic aldehydes or its acetals.
3) A process as claimed in claim 1, wherein the acidic catalyst used include inorganic acids, such as

hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid or aliphatic acids like formic acid, propionic acid, maleic acid or substituted or unsubstituted hydroxyacids or diacids or aliphatic or aromatic sulfonic acids or its salts, solid catalyst like acidic ion exchange resins, heteropolyacids, zeotiles.
4) A process as claimed in claim 1, wherein the acidic catalyst can be used alone or in any suitable combination. The reaction can also be carried out without using acidic catalyst.
5) A process as claimed in claim 1, wherein the said solvent used include aliphatic or aromatic hydrocarbon, tetrahydrofuran, ethers, acetonitrile, dimethylsulfoxide, either alone or in suitable combinations.
6) A process as claimed in claim 1 a, the temperature of said reaction is between 25°C- 150°C preferably at temperature ranging between 50°C to 100°C.

7} A process as claimed in claim 1 a, can also be carried out without azeotropic removal of water.
8) A process as claimed in claim 1, wherein the radical
initiator catalyst used include substituted or
unsubstituted aromatic or aliphatic peroxides like
-benzoyl peroxide, di-tert-butyl hydroperoxide , lauryl
peroxide or AIBN.
Dated this 14th day of October, 2005

ABSTRACT OF THE INVENTION
The process for producing 2-[l-(hydroxymethyl)- cyclopropane]
acetic acid with steps of : a) reacting 1,1-
cyclopropanedimethanol with aldehydes or acetals of
aldehydes in solvents or without solvent using acidic catalyst at
elevated temperature with azeotropic removal of water to
form benzylidene acetal; b) opening of benzylidene acetal
with N-halo succinimide or 1,3-dihalo-5, 5-dimethyl hydantoine
using radical initiator in solvent at elevated temperature to
obtain (halomethyl) cyclopropanemethyl benzoate; and c)
conversion of 1-(halomethyl) cyclopropanemethyl
benzoate to 1-(benzoyloxymethyl)cyclopropane acetonitrile followed by hydrolysis under alkaline condition to obtain (hydroxymethyl) cyclopropane acetic acid.

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Patent Number

251546

Indian Patent Application Number

1293/MUM/2005

PG Journal Number

12/2012

Publication Date

23-Mar-2012

Grant Date

21-Mar-2012

Date of Filing

14-Oct-2005

Name of Patentee

CENTAUR CHEMICALS PRIVATE LIMITED

Applicant Address

CENTAUR HOUSE, SHANTINAGAR, VAKOLA, SANATACRUZ (E), MUMBAI 400 055.

Inventors:

#	Inventor's Name	Inventor's Address
1	ANIL MAHADEV NAIK	CENTAUR HOUSE, SHANTINAGAR, VAKOLA, SANATACRUZ (E), MUMBAI 400 055.
2	SHRIKANT DATTATRAYA SAWANT	CENTAUR HOUSE, SHANTINAGAR, VAKOLA, SANATACRUZ (E), MUMBAI 400 055.
3	SMITA GIRISH KAVISHWAR	CENTAUR HOUSE, SHANTINAGAR, VAKOLA, SANATACRUZ (E), MUMBAI 400 055.

PCT International Classification Number

C07C61/04

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA