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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

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✦ 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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