1,5-Benzothiazepine derivatives and production thereof

Details 1,5-Benzothiazepine derivatives and production thereof 1,5-Benzothiazepine derivatives and production thereof

1983-10-07

1984-12-25

Bond, Robert T.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424275, C07D28102

Patent

active

044902921

ABSTRACT:
Novel 1,5-benzothiazepine derivatives having the formula; ##STR1## (wherein R.sub.1, R.sub.2 and R.sub.3 each denotes hydrogen, a halogen, a lower alkyl group, a lower alkoxy group or a hydroxy group; R.sub.4 denotes a lower alkyl group, an allyl group, a lower alkoxyalkyl group, a lower alkyl group substituted with a hydroxy group or a halogen, a lower alkylaminoalkyl group or a morpholino lower alkyl group; X denotes a halogen or hydrogen) are produced from corresponding 1,4-benzothiazine by a ring expansion reaction with trimethylhalosilane, hydrogen peroxide and water. The derivatives have analgesic, antipyretic and antiarrythmic activities.

REFERENCES:
patent: 4416819 (1983-11-01), Nagao et al.
Maki et al., "J. Chem. Soc.", Chemical Communications, (1983), pp. 450-451.

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