1, 2, 5-Thiadizole 1-oxide and 1, 1-dioxide derivatives. A new class of potent histamine H2-receptor antagonists

…, M Brown, RA Partyka, RR Crenshaw

Index: Algieri, Aldo A.; Luke, George M.; Standridge, Robert T.; Brown, Myron; Partyka, Richard A.; Crenshaw, R. R. Journal of Medicinal Chemistry, 1982 , vol. 25, # 3 p. 210 - 212

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Citation Number: 45

Abstract

with the monoxide 1 at reflux temperature gave the dioxide 2, mp 187-191" C after recrystallization from MeOH, in 46% and 70% yields, respectively. The dioxide 2 may also be prepared by the method of Wen et al.'O Alternatively, the monoxide 1 was more readily prepared in 87% yield directly from dimethyl oxaldiimidate and thionyl chloride with 2 equiv of pyridine. Compound 1 or 2 then was treated sequentially in methanol at 0-5 OC with the ...