NEW MATERIAL:The compound of formula 1 (R1 and R2 are H or lower alkyl; n is 0W2).
EXAMPLE: 3-Amino-5-ethoxycarbonylmethyl-2,3-dihydro-1,5-benzothiazepin-4( 5H )- one.
USE: Remedy for hypertension and circulatory diseases. It has angiotensinase-inhibiting and hypotensive activities.
PREPARATION: The compound of formula 1 can be prepared by (1) reacting the compound of formula 2 with the compound of formula 3 (X is Br, Cl or I) in the presence of a proper dechlorination agent such as sodium, sodium hydride, potassium hydride, etc. at a temperature between room temperature and the boiling point of the reaction mixture for 0.5W3hr to obtain the compound of formula 4 (R3 is lower alkyl), (2) optionally converting the compound of formula 4 to the compound of formula 5 by hydrolysis, etc., and (3) reacting the compound of formula 4 or the compound of formula 5 with the compound of formula 6 in the presence of a proper reducing agent.
FUKAZAWA NOBUYUKI
IIZUKA HAJIME
NISHINA TAKASHI
SHIRAKAWA ISAO
| JPS59205372A | 1984-11-20 | |||
| JPS59167577A | 1984-09-21 |