To obtain the subject new compound, a specific dihydrobenzodioxepin compound, exhibiting selective antagonism against muscarine M3 receptors, and useful in dealing with urologic diseases including pollakisuria, incontinence of urine and labile bladder.
This new compound is a compound of the formula [D is (esterified) carboxyl or a group of the formula A-X-R5' (R5' is a cycloalkyl-alkyl or the like; A is a 1-5C alkylene; X is O, S, or the like); R1 and R2 are each H, a halogen, or the like; R3 and R4 are each H, an alkyl or the like], e.g. 3-amino-3-cyano-3,4-dihydro-2H-1,5-benzodioxepin. This compound of the formula is obtained by the following process: a benzoxepin compound is reacted with a carboxylic acid in the presence of dicyclohexylcarbodiimide or the like in an inert solvent at 0-120°C for 10 min to 10 h to form the corresponding amide compound, which is then reduced in the presence of lithium aluminum hydride or the like in an inert solvent at 0-120°C for 30 min to 10 h.
KATAYAMA KENICHI
IKEBE TSUGIO
FUJIO MASAKAZU
NAKAMURA MITSUHARU
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