A Novel Preparation and Reaction of 2, 1-Benzisothiazole Derivatives

Autor:	Osami Aki, Yasushi Nakagawa, Kenzo Sirakawa
Rok vydání:	1972
Předmět:	chemistry.chemical_element Phosphorus pentasulfide General Chemistry General Medicine Alkylation Sulfur chemistry.chemical_compound chemistry Derivative (finance) Drug Discovery Imidazole Organic chemistry Lewis acids and bases Glycine ethyl ester
Zdroj:	Chemical and Pharmaceutical Bulletin. 20:2372-2376
ISSN:	1347-5223 0009-2363
DOI:	10.1248/cpb.20.2372
Popis:	2, 1-Benzisoxazole derivatives were converted into 2, 1-benzisothiazoles simply by fusing with phosphorus pentasulfide in imidazole. 1-Alkyl-2, 1-benzisothiazolium salts, prepared by alkylation of 2, 1-benzisothiazoles with trialkyl orthoformates in the presence of Lewis acids, were shown to react with amines to afford 2, 1-benzisothiazoline derivatives and with glycine ethyl ester to form a 1, 4-benzodiazepin-2-one derivative by the extrusion of the sulfur atom.
Databáze:	OpenAIRE
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