NEW MATERIAL:The compound of formula I (R1WR3 are H, halogen, lower alkyl, lower alkoxy or OH; R4 is lower alkyl, lower alkylaminoalkyl or morpholinoalkyl) or its acid addition salt.
EXAMPLE: 2-(4-Hydroxyphenyl)-5-( 2-morpholinoethyl )-2,3-dihydro-1,5- benzothiazepine-3,4(5H)-dione hydrochloride.
USE: A drug having weak toxicity and excellent pharmacological activities such as analgesic, antipyretic or antiarrhythmic activities.
PREPARATION: The compound of formula I can be produced in high yield, by reacting 2-phenylmethylidene or 2-(substituted-phenyl)methylidene-4-substituted-2H- 1,4-benzothiazin-3(4H)-one of formula II with trimethyl halogen, H2O2 and water in an inert solvent under cooling or at room temperature for several tens minutes or several hours.
MITSUMORI NAOMICHI
UNEDA TAKASHI
SASAO YASUTAKA
TAKATANI MASAHIRO
Next Patent: 1,5-BENZOTHIAZEPINE DERIVATIVE AND ITS PREPARATION