Document Type and Number:
Japanese Patent JPS4881898
Kind Code:
A
Abstract:
1416934 Quinobenzoxa(or thia)zepines E R SQUIBB & SONS Inc 18 Jan 1973 [31 Jan 1972] 2695/73 Heading C2C Novel compounds of Formula I or II in which each of X and Y is C 1-8 alkyl, cycloalkyl, C 1-8 alkylthio, C 1-8 alkoxy, halogen, CF 3 , CN, NC or di-(C 1-8 alkyl)sulphamoyl, A is O or S, each of R1 and R2 is H, C 1-8 alkyl, aralkyl or alkenyl or NR1 R2 represents a heterocyclic group of Formula IV in which X1 is NR4 , S or CH 2 , r is 1, 2 or 3, each of R3 and R4 is H, C 1-8 alkyl, hydroxy-C 1-8 alkyl, C 1-8 alkanoyloxy-C 1-8 alkyl, hydroxy-C 1-8 alkoxy-C 1-8 alkyl, amino-C 1-8 alkyl, C 1-8 alkylamino-C 1-8 alkyl, di-(C 1-8 alkyl)amino-C 1-8 alkyl or di-(C 1-8 alkyl)amino-C 1-8 alkoxy-C 1-8 alkyl, n is 0, 1 or 2, n1 is 0, 1 or 2 and n11 is 1 to 10, and pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of Formula VII or VIII (i) with a base and then with a compound of formula Hal(CH 2 ) n11 NR1 R2 , or (ii) with a chlorinating agent and then with a compound of formula HO(CH 2 ) n11 NR1 R2 , or (iii) with a base and then successively with a compound of formula Hal(CH 2 ) n11 Hal1 (in which Hal and Hal1 are different and are I, Br, Cl or F) and with a compound of formula HNR1 R2 . Starting materials of Formula VII and VIII are prepared by cyclization of compounds of Formula III followed by reduction of the resulting ketones, the compounds produced depending on the nature and position of X and Y. 5,11 - Dihydro - 7 - trifluoromethyl - dibenz- [b,e][1,4]oxazepine - 5 - propionic acid is prepared by reacting 5,11-dihydro-7-trifluoromethyl - dibenz [b,e][1,4]oxazepine with acrylonitrile to give 7 - trifluoromethyl - 5,11 - dihydrodibenz[b,e][1,4]oxazepine- 5 - propionitrile, reacting this with methanolic hydrogen chloride to form methyl 5,11-dihydro-7-trifluoromethyldibez[b,e][1,4]oxazepine - 5 - propionate and saponifying this to the free acid. 7-Chloro-5,11- dihydro - dibenz[b,e][1,4]oxazepine - 5 - propionic acid and 7 - chloro - 5,11 - dihydro - dibenz- [b,e][1,4]thiazepine-5-propionic acid are similarly prepared via the corresponding intermediates. Pharmaceutical compositions having CNS stimulant or depressant activity or anti-inflammatory activity, for oral or parenteral administration, comprise a compound of the invention together with a pharmaceutical carrier. The compounds of the invention may also be used as the active ingredients in disinfectant compositions.
Application Number:
JP1283073A
Publication Date:
November 01, 1973
Filing Date:
January 31, 1973
Export Citation:
International Classes:
C07D267/18; C07D281/14; C07D498/06; C07D513/04; C07D513/06; (IPC1-7): C07D87/54