Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
A Novel Preparation and Reaction of 2, 1-Benzisothiazole Derivatives
OSAMI AKIYASUSHI NAKAGAWAKENZO SIRAKAWA
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1972 Volume 20 Issue 11 Pages 2372-2376

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Abstract
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.
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© The Pharmaceutical Society of Japan
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