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A Convenient Synthesis of Centperazine, an Antifilarial Candidate Drug (1993)

Sengupta, Sreela ; Sahu, Devi Prasad ; Chatterjee, Sunil Krishna

Weinheim : Wiley-Blackwell

Liebigs Annalen 1993 (1993), S. 437-439

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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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