METHOD FOR PRODUCING 4,4,7-TRIFLUORO-1,2,3,4-TETRAHYDRO-5H-1-BENZAZEPINE COMPOUND AND INTERMEDIATE USED IN THE METHOD

摘要

The present invention provides a method for producing a 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound which has an superior agonistic activity to an arginine vasopressin V2 receptor and is useful as an active ingredient for a pharmaceutical composition for preventing and/or treating urinary frequency, urinary incontinence, enuresis, central diabetes insipidus, nocturia, nocturnal enuresis, or the like; and useful intermediates for use in the methods. The production method of the present invention is suitable for the industrial production of a medicament, because of a smaller number of steps, a higher yield, and a lower cost, as compared with the methods in the related art.

主权项

1. A method for producing a compound of the formula (1) shown in the reaction scheme below, comprising:
a step of reacting a compound of the formula (5) with thionyl chloride (4) to produce a compound of the formula (3); and a step of amidating the compound of the formula (3) by reacting with 2-aminoethanol (2): (in the formula, Me represents methyl).