Title of Invention

"A PROCESS FOR PREPARING AN ECTEINASCHIDIN COMPOUND"

Abstract The present invention relates to a process for preparing an ecteinascidin compounds, particularly ecteinascidin compound (ET-743). The present invention also relates to novel intermediates compounds which are used in process for preparing an ecteinascidin compound (ET-743).
Full Text




We Claim:
1. A process for preparing an ecteinascidin compound (ET-743), said process comprising the steps of:
(a) oxidising an a-aminelactone of formula (35) to the corresponding a-
ketolactone of formula (36) by transamination, in accordance with the
following scheme:
(Formula Removed)
(b) stereospecifically forming the spirotetrahydroisoquinoline
compound Et770 from the a-ketolactone of formula (36) by a Pictet-
Spengler reaction, in accordance with the following scheme:
(Formula Removed)
(c) replacing nitrile at C-21 of Et770 by hydroxy to give the final
compound Et743, in accordance with the following scheme:
(Formula Removed)
2. A process for preparing an ecteinascidin compound (ET743), said process comprising the steps of:
(a) stereospecifically forming the spirotetrahydroisoquinoline compound
Et770 from the a-ketolactone of formula (36) by a Pictet-Spengler
reaction, in accordance with the following scheme:
(Formula Removed)
(b) replacing nitrile at C-21 of Et770 by hydroxy to give the final
compound Et743, in accordance with the following scheme:
(Formula Removed)
3. An intermediate for the synthesis of an ecteinascidin compound (ET743), said intermediate being of the formula (35) or formula (36):
(Formula Removed)

Documents:

5255-DELNP-2007-Abstract-(11-04-2012).pdf

5255-DELNP-2007-Claims-(11-04-2012).pdf

5255-delnp-2007-Correspondence Others-(08-04-2011).pdf

5255-DELNP-2007-Correspondence Others-(11-04-2012).pdf

5255-delnp-2007-Correspondence-Others(16-05-2011).pdf

5255-delnp-2007-correspondence-others-1.pdf

5255-DELNP-2007-Form-1-(11-04-2012).pdf

5255-delnp-2007-Form-1-(16-05-2011).pdf

5255-delnp-2007-form-18.pdf

5255-DELNP-2007-Form-2-(11-04-2012).pdf

5255-DELNP-2007-Form-3-(11-04-2012).pdf

5255-DELNP-2007-GPA-(11-04-2012).pdf

5255-DELNP-2007-Petition-137-(11-04-2012)-1.pdf

5255-DELNP-2007-Petition-137-(11-04-2012).pdf


Patent Number 252542
Indian Patent Application Number 5255/DELNP/2007
PG Journal Number 21/2012
Publication Date 25-May-2012
Grant Date 21-May-2012
Date of Filing 06-Jul-2007
Name of Patentee PHARMA MAR,S.A.
Applicant Address CALLE DE LA CALERA, 3,POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
Inventors:
# Inventor's Name Inventor's Address
1 CUEVAS, CARMEN PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
2 PEREZ, MARTA PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
3 FRANCESCH, CAROLINA PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
4 FERNANDEZ, CAROLINA PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
5 CHICHARRO, JOSE LUIS PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
6 GALLEGO, PILAR PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
7 ZARZUELO, MARIA PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
8 MANZANARES, IGNACIO PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
9 MARTIN, MARIA JESUS PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
10 MUNT, SIMON PHARMA MAR,S.A., CALLE DE LA CALERA, 3, POLIGONO INDUSTRIAL DE TRES CANTOS, TRES CANTOS, E-28760 MADRID, SPAIN
PCT International Classification Number C07D 471/18
PCT International Application Number PCT/GB01/02120
PCT International Filing date 2002-10-09
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 PCT/GB01/02120 2002-10-09 PCT