| 摘要 |
CNS active 9-(subst. alkylidene)-thiaxanthenes Title cpds. of formula (I) (where D is a divalent > 2C aliphatic residue subst. by a secondary or tertiary amino group which may be hydroxy- or amino- subst., and where the aromatic nuclei may be substd. by alkyl, CF3, aralkyl, aryl, alkoxy, aralkoxy, aryloxy, alkylthio, aralkylthio, arylthio, halogen, acyl, amino, OH or COOH) having e.g. narcosis-potentiating, adrenolytic, sedative, antihistamine, antiemetic, antipyretic, local anaesthetic or hypothermic activity are prepd. by reacting a corr. thiaxanthone (in which any acyl substituent is protected by ketalization, any amino substituent by acylation and any hydroxy or carboxy substituent by esterification) with a >2C aliphatic organometallic cpd. subst. by an ether group, hydrolysing the reaction product, removing any protecting groups, simultaneously dehydrating the product and cleaving off the ether group by reacting with a halogen-releasing cpd. (pref. HBr or POCl3), and reacting the product with an opt. hydroxy- or amino-substd. primary or secondary amine. |
