| abstract |
1468497 Esters of 1-acylpiperazine-4-carboxylic acids RHONE - POULENC INDUSTRIES 6 Nov 1975 [7 Nov 1974 4 Sept 1975 (3)] 46103/75 Heading C2C The invention comprises compounds of formula wherein the pyrroline ring, R 1 and R 2 together form an optionally substituted isoindoline, 6,7- dihydro - 5H - pyrrolo[3,4 - b]pyrazine, 2,3,6,7- tetrahydro - 5H - 1,4 - oxathiino[2,3 - c]pyrrole or 2,3,6,7 - tetrahydro - 5H - 1,4 - dithiino[2,3- c]pyrrole nucleus; Het is pyrid-2-yl, quinol-2-yl or 1,8-naphthyridin-2-yl, and may be substituted; Z is O or S; and R is H or a substituent (as defined in the Specification). In examples, the bicyclic dicarboxylic acid imide is partially reduced to the bicyclic hydroxylactam which is either esterified with a 1-acylpiperazine-4-carbonyl chloride to give (I), or converted to the bicyclic phenoxycarbonyloxy-lactam; the latter is reacted either with a 1-acylpiperazine to give (I), or with piperazine to give the unacylated analogue of (I) which may then be acylated. Starting materials also prepared are 2-amino- 7-chloroquinoline and pyrazinedicarboxylic acid mono-(5-chloropyridyl)amide. Therapeutic compositions having tranquillizing, anticonvulsant, decontracturant and hypnotic activity comprise compounds of the above formula, and may be administered orally, parenterally or rectally. |