泰必乐(tiapride)系含烷砜基邻茴香酰胺的衍生物,其WHO的非专利商品名为Tiapridal;化学名为N-(2-二乙胺基乙基)-2-甲氧基-5甲砜基苯甲酰胺。结构式如下: 胺类抗精神病药舒必利(sulpiride)、索托必利(sultopride)之后,于最近发现的新型神经精神安定药,自1974年上市以来,国外已经广泛应用。鉴于国内尚无泰必乐产品,作者于1980年开始研制。综合文献报道,泰必乐是以2-甲氧基-5-甲砜基苯甲酸为主要中间体,其合成路线有几种图1。 Tiapride is an alkylsulfone-o-anisan derivative known by the WHO under the trade name Tiapridal. The chemical name is N- (2-diethylaminoethyl) -2-methoxy- 5 methyl sulfone benzamide. The structural formula is as follows: Amine antipsychotic sulpiride, sultopride, the recently discovered new neuropsychic stabilizer, since its listing in 1974, has been widely used abroad. In view of the fact that there are no products in Thailand, the author started the research in 1980. According to the comprehensive literature, Tropicel is 2-methoxy-5-methylsulfonyl benzoic acid as the main intermediates, the synthesis of several routes Figure 1.