ISSN:
0170-2041
Keywords:
Centperazine
;
Antifilarial drug
;
6H-Pyrazino[1,2-c]pyrimidines
;
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
7-Ethyl-octahydro-2-methyl-6H-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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/jlac.199319930171
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