| 摘要 |
1424572 3,4-Dihydrocarbostyril derivatives OTSUKA PHARMACEUTICAL CO Ltd 22 Jan 1973 [13 April 1972 (2) 14 Sept 1972 (3) 2 Dec 1972 21 Dec 1972] 34170/75 Divided out of 1424571 Heading C2C The invention comprises 3,4-dihydrocarbostyril derivatives of Formula (I) in which R<SP>1</SP> is hydrogen, a C 1 -C 4 alkyl group, an aralkyl group or a C 2 -C 4 alkenyl group and Z represents (a) or (b) -CHOH-CH 2 X where X is a halogen atom. They may be prepared by reacting a 5-, 6-, 7- or 8-hydroxy-3,4-dihydrocarbostyril derivative of Formula II with an epihalohydrin of Formula III in the presence of a basic compound. The compounds of Formula II may be prepared by reacting a 3,4,5,6,7,8-hexahydrocarbostyril-5- one of Formula VI with a brominating agent to get an 8- (or 6-) -bromo derivative and heating this to remove bromine and dehydrogenate the ring. The proportion of the two products having groups (a) and (b) obtained depends on the reaction conditions. The compounds in which Z is the group (b) may also be prepared by reacting a compound of Formula (VI) above with a compound of formula CH 2 OH.CHOH.CH 2 X (X is a halogen) in the presence of a brominating agent. |
