Imidazole thieno-benzothiepins

Details Imidazole thieno-benzothiepins Imidazole thieno-benzothiepins

1986-12-01

1988-03-08

Schwartz, Richard A.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549 12, C07D49504

Patent

active

047300540

ABSTRACT:
The present invention relates to imidazolyl thieno-benzothiepin derivatives of the Formula I: ##STR1## and acid addition salts thereof with pharmaceutically acceptable inorganic and organic acids, wherein R is a hydrogen or a chlorine atom. The invention also relates to processes for the preparation of these compounds. These compounds demonstrate substantial in vitro and in vivo antimycotic properties of the kind useful for the treatment of dermal and vaginal mycoses.
The new compounds can be prepared by reacting 4,9-dihydrothieno(2,3-c)-2-benzothiepin-4-ol or its 6-chloro derivative with imidazole or a reactive derivative thereof, such as 1,1'-carbonyl-diimidazole or 1,1'-thionyldiimidazole; or by first converting the respective thieno-benzothiepin-4-ol into its alkane- or arenesulfonate ester, followed by reaction with imidazole.

REFERENCES:
patent: 4169205 (1979-09-01), Hoehn
Derwent Abstract of Japan 56073073 6/17/81.

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