Title of Invention

A NOVEL PROCESS FOR PREPARATION OF MALEIC ACID SALT OF QUINAPRIL BENZYL ESTER

Abstract

PROCESS FOR PREPARATION OF BENZYL ESTER MALEATE SALT OF QUINAPRIL A process for preparation of a novel crystalline form of quinapril hydrochloride of formula(I). A process for preparation of amorphous form of quinapril hydrochloride, of high purity and conforming to pharmacopoeial specifications, by the use of the novel crystalline quinapril hydrochloride as an intermediate. The said process involves adjusting the pH of a solution of the benzyl ester maleate salt of quinapril of formula(V) between 7.5-8.5 in a mixture of water and an organic solvent to obtain free base compound of formula(V); subjecting the free base of compound (V) thus obtained to catalytic hydrogenation in an alcoholic solvent in the presence of concentrated hydrochloric acid or hydrogen chloride dissolved in an alcoholic solvent and in the presence of catalytic amounts of Pd/C to obtain a residue containing formula(I); crystallization of the said residue by evaporating the alcoholic solvent from a nitrolkane solvent to give crystalline quinapril hydrochloride, associated with a solvent of the nitroalkane solvent, and drying the crystalline quinapril hydrochloride nitroalkane solvate at a temperature between 40 and 45 degree/C under vacuum to give pure quinapril hydrochloride of formula(I).

Full Text

FORM-2 THE PATENTS ACT, 1970 (39 OF 1970) COMPLETE SPECIFICATION (See Section 10; rule 13) 1. TITLE OF INVENTION A NOVEL PROCESS FOR PREPARATION OF MALEIC ACID SALT OF QUINAPRIL BENZYAL ESTER LUPIN LIMITED 159, CST Road, Kalina, Santa Cruz (East) Mumbai - 400 098 Maharashtra, India An Indian Company The following specification particularly describes the nature of the invention and the manner in which it is to be performed.

Documents:

1320-mum-2004-abstract(10-12-2004).pdf

1320-mum-2004-abstract(16-12-2004).doc

1320-MUM-2004-ABSTRACT(GRANTED)-(1-1-2008).pdf

1320-MUM-2004-CLAIMS(10-12-2004).pdf

1320-mum-2004-claims(granted)(16-12-2004).doc

1320-MUM-2004-CLAIMS(GRANTED)-(1-1-2008).pdf

1320-mum-2004-claims(granted)-(10-12-2004).pdf

1320-mum-2004-correspondence(31-10-2007).pdf

1320-MUM-2004-CORRESPONDENCE(IPO)-(4-2-2008).pdf

1320-mum-2004-correspondence-ipo-(21-1-2007).pdf

1320-MUM-2004-DESCRIPTION(COMPLETE)-(10-12-2004).pdf

1320-MUM-2004-DESCRIPTION(GRANTED)-(1-1-2008).pdf

1320-mum-2004-drawing(10-12-2004).pdf

1320-MUM-2004-DRAWING(GRANTED)-(1-1-2008).pdf

1320-mum-2004-form 1(10-12-2004).pdf

1320-MUM-2004-FORM 1(31-2-2005).pdf

1320-mum-2004-form 18(24-02-2005).pdf

1320-MUM-2004-FORM 2(COMPLETE)-(10-12-2004).pdf

1320-mum-2004-form 2(granted)(16-12-2004).doc

1320-MUM-2004-FORM 2(GRANTED)-(1-1-2008).pdf

1320-mum-2004-form 2(granted)-(10-12-2004).pdf

1320-MUM-2004-FORM 2(TITLE PAGE)-(10-12-2004).pdf

1320-MUM-2004-FORM 2(TITLE PAGE)-(GRANTED)-(1-1-2008).pdf

1320-mum-2004-form 3(09-12-2004).pdf

1320-MUM-2004-FORM 3(10-12-2004).pdf

1320-mum-2004-form pct-ipea-409(10-12-2004).pdf

1320-mum-2004-form pct-isa-210(10-12-2004).pdf

1320-mum-2004-power of attorney(10-12-2004).pdf

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