| 摘要 |
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 R<SP>2</SP>(-OH)CH 2 CH : CH 2 and R<SP>2</SP> : O, where R is 3-FC 6 H 4 , R<SP>1</SP> is 2-chloro(or trifluoromethyl)-6- fluorothiaxanth-9-ylidene, and R<SP>2</SP> 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. |
