Title:
ペリンドプリルおよびその塩の製法
Document Type and Number:
Japanese Patent JP4461027
Kind Code:
B2
Abstract:
A process for preparation of perindopril of formula (II) and salts thereof which is simple, safe, convenient and cost-effective. The process involves reaction of compound of formula (I), wherein X is chlorine or bromine with compound of formula (VII) wherein A signifies that the six-membered ring of the bicyclic system is either saturated or unsaturated to give compound of formula (VIII), wherein A is as defined above, followed by catalytic hydrogenation of the compound of formula (VIII) thus obtained to give the perindopril of formula (II). The above process for the manufacture of perindopril would specifically avoid the use of harmful chemicals like phosgene or costly coupling agents like dicyclohexylcarbodiimide and 1-hydroxybenxotriazole usually used for such manufacture. The process would also not require any intervention of a catalyst and does not require any alkaline or acidic reaction conditions. Importantly, the process provides for manufacture of perindopril with high stereoselectively giving perindopril (II) having (S)-configuration in all the five chiral centres of the molecule, conforming to pharmacoepeial specifications. The invention also relates to a method for preparation of the compound of formula (I) and also to a method for preparation of N-[(S)-1-carbethoxybutyl]-(S)-alanine of formula (III) used in the process.
Inventors:
Devashish Datta
Giriji Pal Shin
Himanche Madav Godbole
Rajender del Shen
Giriji Pal Shin
Himanche Madav Godbole
Rajender del Shen
Application Number:
JP2004568714A
Publication Date:
May 12, 2010
Filing Date:
February 28, 2003
Export Citation:
Assignee:
Réra Bora Toir Servier
International Classes:
C07K5/062; A61P9/12; C07C227/32; C07C227/34; C07C229/12; C07D209/42
Domestic Patent References:
| JP1110696A | ||||
| JP57165355A |
Attorney, Agent or Firm:
Hajime Tsukuni
Koshiro Tsukuda
Fusayuki Saito
Koshiro Tsukuda
Fusayuki Saito