Document Type and Number:
Japanese Patent JPS4994691
Kind Code:
A
Abstract:
1453828 Thiaxanthene derivatives KEFALAS AS 28 Nov 1973 [8 Dec 1972] 56910/72 Heading C2C The invention comprises compounds of formula and their addition salts with pharmaceutically acceptable acids, wherein X is Cl, CF 3 or SO 2 NMe 2 ; Z is >CHCH 2 - or >C : CH-; and Y is >NH, >NMe, >NCH 2 CH 2 OH or > CHCH 2 CH 2 OH, and the esters of these alcohols with C 1-17 alkanoic acids. In examples, these compounds are prepared by (1) reducing the unsaturated to the saturated compounds; (2) reacting the analogues having the side-chain terminated by: CH 2 , Cl or NMe 2 with (3) forming the compound where Y is by reacting that where Y is >NH with ethylene oxide; (4) esterifying the alcohols; (5) reacting a 9-Li derivative of a 9-unsubstituted 3-fluorothioxanthene (which is derived from the corresponding thiaxanthone) with (6) splitting the corresponding methyl ether of the desired alcohol. Analogues of the compounds (I) having a 5- or 6-Cl or CF 3 substituent instead of 6-F are also disclosed. Starting materials and intermediates otherwise described are 1-(3-chloropropyl)-4-(2-methoxyethyl)piperazine, and those of formulµ R2 (-OH)CH 2 CH : CH 2 and R2 : O, where R is 3-FC 6 H 4 , R1 is 2-chloro(or trifluoromethyl)-6- fluorothiaxanth-9-ylidene, and R2 is 2-dimethylsulphamoyl-6-fluorothiaxanth-9-ylidene. Therapeutic compositions having neuroleptic activity comprise compounds of the above formula, and may be administered orally or parenterally.
Application Number:
JP13625673A
Publication Date:
September 09, 1974
Filing Date:
December 07, 1973
Export Citation:
International Classes:
C07D335/20; A61K31/38; A61K31/395; A61K31/54; A61K31/5415; A61P25/00; C07D279/28; C07D295/088; C07D335/12; C07D337/14; C07D409/06; (IPC1-7): C07D99/06