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替仑西平是新的选择性抗胆碱药,正开发治疗消化性溃疡,与其它传统抗胆碱药相比,本品优先作用于M_1受体,且较哌仑西平作用强,作用持续时间长,生物利用度高,故建议本品一日服药1次。合成 1,2-二氨基苯(Ⅰ)与四氢5-甲基-4氧代-3-噻吩乙酸甲酯(Ⅱ)在甲苯中缩合成三环物(Ⅲ),Ⅲ脱氢生成Ⅳ,Ⅳ在二噁烷中在K_2CO_3存在下与氯乙酰氯生成Ⅴ,最后与N-甲基哌嗪生成本品的盐酸盐。
Telen Xapine is a new selective anticholinergic drugs, is developing the treatment of peptic ulcer, compared with other traditional anticholinergics, this product preferentially acts on the M 1 receptor, and stronger than pirenzepine, the role of long duration, high bioavailability Therefore, it is recommended that this product be taken once a day. Synthesis of 1,2-diaminobenzene (Ⅰ) and tetrahydro-5-methyl-4-oxo-3-thiopheneacetic acid methyl ester (Ⅱ) is condensed into tricyclo (Ⅲ) Ⅳ in dioxane in the presence of K_2CO_3 with chloroacetyl chloride generated Ⅴ, and finally with N-methyl piperazine hydrochloride generated hydrochloride.