A Convenient Synthesis of Centperazine, an Antifilarial Candidate Drug
✍ Scribed by Sengupta, Sreela ;Sahu, Devi Prasad ;Chatterjee, Sunil Krishna
- Publisher
- John Wiley and Sons
- Year
- 1993
- Tongue
- English
- Weight
- 279 KB
- Volume
- 1993
- Category
- Article
- ISSN
- 0947-3440
No coin nor oath required. For personal study only.
✦ Synopsis
Abstract
7‐Ethyl‐octahydro‐2‐methyl‐6__H__‐pyrazino[1,2‐c]pyrimidin‐6‐one (centperazine) (1), an antifilarial candidate drug, currently undergoing phase II clinical trials, has been synthesized by a more economically viable alternative route. Condensation of N,N′‐dibenzylethylenediamine (2) with 3,4‐dibromobutyronitrile (3) gives 2‐(1,4‐dibenzyl‐2‐piperazinyl)acetonitrile (4), which, on catalytic reduction, debenzylation, cyclocarbamation and N‐alkylation yields the target molecule 1 in 10.1% overall yield.
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