Expeditious synthesis of ramipril: An angiotensin converting enzyme (ACE) inhibitor

被引:5
|
作者
Malakondaiah, Golla China [1 ]
Gurav, V. M. [1 ]
Reddy, Lekkala Amarnath
Babu, Karrothu Srihari
Bhaskar, Bolugoddu Vijaya
Reddy, Padi Pratap
Bhattacharya, Apurba
Anand, Ramasamy Vijaya
机构
[1] Dr Reddys Labs Ltd, Ctr Excellence, IPDO, Bachupalli 500072, Andhra Pradesh, India
关键词
boric acid; esterification; L-(+)-mandelic acid; ramipril; resolution;
D O I
10.1080/00397910801989238
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We document an efficient and cost-effective synthesis of ramipril 1 utilizing (i) an environmentally benign process for the esterification of racemic 2-aza-bicyclo-[3.3.0]-octane-3-carboxylic acid hydrochloride 2 using boric acid as a catalyst and (ii) a robust resolution process for the synthesis of 3a by means of inexpensive and recyclable L-(+)-mandelic acid as key steps.
引用
收藏
页码:1737 / 1744
页数:8
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