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[摘要]
目的 研究盐酸坦索罗辛的合成方法。方法 以4-甲氧基苯丙酮和(R)-1-苯乙胺为起始原料,先进行不对称合成制备2-[(R)-1-(4-甲氧基苯基)]丙基-N-[(R)-1-苯乙基]胺盐酸盐,再经过氯磺化、胺解、烃化、氢解和成盐合成盐酸坦索罗辛。结果 该合成工艺盐酸坦索罗辛的总收率为26%。结论 该合成方法步骤短,易于操作。
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[Abstract]
Objective To study the synthesis of tamsulosin hydrochloride. Methods (R)-1-(4-Methoxyphenyl)-N-[(R)-1-phenylethyl] propan-2-amine hydrochloride was synthesized from 4-methoxyphenylacetone and (R)-1-phenylethanamine by asymmetric synthesis firstly, then tamsulosin hydrochloride was prepared by chlorosulfonation, amination, alkylation, hydrogenolysis, and salification. Results The total yield of tamsulosin hydrochloride was 26% by this synthetic technology. Conclusion The route of this synthetic method is short and easy to operate.
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