| 摘要 |
1386027 Derivatives of thienochromene and dihydrothiapyranochromene L S HARRIS H G PARS J C SHEEHAN nd R K RAZDAN 20 Dec 1972 [27 Dec 1971] 58870/72 Heading C2C The invention comprises compounds of formula and their acid addition salts, wherein m, n are each 0-3 but m + n = 2 or 3; R 1 is C 1-6 alkyl; R 2 is alkyl or cycloalkyl-C 1-6 -alkyl; R 3 is -CO(CH 2 ) 1-8 -Z and Z is morpholino, thiamorpholino, piperazino, 4-C 1-6 -alkylpiperazino or N(CH 2 ) 3-9 . In examples, these compounds are prepared by reacting together the corresponding phenol (R 3 =H : II), HO 2 C(CH 2 ) 1-8 Z and dicyclohexylcarbodiimide. II are prepared by reacting an appropriate oxo-compound (R 1 R 1 C=O : C, R 3 =H) with R 1 MgBr, and ring- -closing the thus-formed 2-(dialkylmethyloldihydrothienyl) - 5 - R 2 - resorcinot (or its dihydrothiapyranyl analogue) with p-TSOH or HBr. Starting materials also prepared are 2- and 5- carbomethoxy - 3 - oxotetrahydrothiophene and 2-carbomethoxy-3-oxotetrahydrothiapyran. Therapeutic compositions for oral or intraperitoneal administration comprise compounds of the above formula, which have tranquilizing activity. |
