NEW MATERIAL:The compound of formula I[R1 is phenyl or p-methoxyphenyl; R2 is H or CH3; R3 is p-methoxyphenetyl, 3-(p-fluorobenzoyl)-propyl, cyclopropylmethyl or group of formula II] or its pharmacologically permissible salt.
EXAMPLE: 5-[3-(p-Fluorobenzoyl)propyl]-1,2,3,4,5,6-hexahydro-1-(p-methoxy-phenyl)- 2-methyl-2,5-benzodiazocine.
USE: A nervous system agent useful as an analgesic, antitussive, antipyretic and sedative (hypnotic).
PROCESS: The compound of formulaIcan be prepared by substituting the 5-position of the compound of formula III with R1 by conventional method such as acid chloride process, carboxylic acid process, alkyl halogenide process, etc., and if necessary, methylating the 2-position of the product by conventional process. The reaction may be carried out using proper protecting groups.
MIURA KENJI
BABA YUTAKA
IWATA NORIYUKI
FUKUI AKIRA
HORI MIKIO
FUJIMURA HAJIME
SUENAGA EIICHI
| US3499806A | 1970-03-10 |