Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Nonsteroidal Antiinflammatory Agents. IV. Syntheses of Pyridobenzoxepin, Pyridobenzothiepin and Their Acetic Acid Derivatives
HIROAKI TAGAWASHIRO KUBOFUMIYOSHI ISHIKAWA
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Keywords: cyclization
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1981 Volume 29 Issue 12 Pages 3515-3521

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Abstract
As part of a search for new antiinflammatory agents, some new tricyclic compounds and their acetic acid derivatives were prepared. Pyrido [2, 3-c] [1] benzoxepin-5 (11H)-one (4a) and pyrido [3, 2-c] [1] benzoxepin-11 (5H)-one (10a) and their thiepin analogs (4b, 10b) were synthesized by cyclization of the corresponding pyridinecarboxylic acid derivatives (3a, 3b, 9a and 9b) with polyphosphoric acid (PPA). The acetic acid derivatives (12a-b) of 4a-b were prepared via methyl derivatives (14a-b) of 4a-b. Their antiinflammatory activities were less potent than those of the corresponding dibenz [b, e] oxepin- and dibenz-[b, e] thiepinacetic acids.
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© The Pharmaceutical Society of Japan
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