抗胆碱药——9-羟基-噻吨-9-羧酸氨基烃酯类化合物的合成

SYNTHESIS OF AMINO-ALKYL-9-HYDROXY-THIOXANTHENE-9-CARBOXYLATES AS ANTICHO?INERGIC AGENTS

本文报道了9-羟基-噻吨-9-羧酸氨基烃酯类化合物的合成.主要中间体9-羟基-噻吨-9-羧酸系分别采用文献方法合成,还设计由噻吨酮与金属钠和CO_2一步反应而得.在所合成9个氨基烃酯类化合物中,经初步药理实验表明,多数化合物均有不同程度的抗胆碱作用.其中化合物Ⅵ-1的抗槟榔碱震颤作用与阿托品相当,但抗流涎作用和扩瞳作用比阿托品弱.

A series of amino-alkyl-9-hydroxy-thioxanthene-9-carboxylates was synthesized.The main intermediate,9-hydroxy-thioxanthene-9-carboxylic acid,was designed and synthesized by treating the thioxanthone with metallic sodium and CO_2 in THF.New method is better and simpler than the referential one.The IR,~2HNMR and MS spectra and elemental analyses of all compounds are consistent with their structures.Preliminary pharmacological experiments showed that some of these compounds exhibited anticholinergic activities in mice.Among them,the antitremor activity of compound Ⅵ-1 was equal to that of atropine,but its antisalivatic and mydriatic activities were weaker than that of atropine.