| 摘要 |
<p>New benzopyran esters of formula (I) and their acid addn. salts. In formula (I), R is H or 1-6C alkyl; R1 is 1-6C alkyl; R2 is 1-20C alkyl; R3 is a gp. of formula (Ia) in which m is 0-8 and R4 is H or 1-6C alkyl; and n is 3-7. Specific cpds. (I) include 4,4-dimethyl-9-/4-(homopiperidino)-butyryloxy/-7-(3-methyl-2-octy- l)-1,2,3,4-tetrahydrocyclopenta c 1 benzopyran. In an example, (I) is prepd. by reacting 4,4-dimethyl-9-hydroxy-7-(3-methyl-2-octyl)-1,2,3,4-tetrahydrocyc- lopenta c 1 benzopyran (1.7 g.) with 4-homopiperidinobutyric acid hydrochloride (1.10 g.) in CH2Cl2 (200 ml.) in the presence of dicyclohexylcarbodiimide (1.13 g.). The prod. is isolated as the hydrochloride (1.7 g; m.pt. 147-9 degrees. (I) are useful as analgesics, minor tranquillisers and anticonvulsants. When tested in the tail-flick and hit-plate tests, (I) show analgesic activity at doses of 20-40 mg./kg. p.o. and 10-20 mg./kg. i.p. In mice, (I) show minor tranquilliser activity at doses of 5-40 mg./kg. i.p.; activity is seen in dogs at 1-5 mg./kg. Anticonvulsant activity is observed in mice at doses of 1-5 mg./kg. p.o. and in rates at 5-10 mg./kg. p.o.</p> |
