目的 研究鹽酸坦索羅辛的合成方法。方法 以4-甲氧基苯丙酮和(R)-1-苯乙胺為起始原料，先進(jìn)行不對(duì)稱(chēng)合成制備2-[(R)-1-(4-甲氧基苯基)]丙基-N-[(R)-1-苯乙基]胺鹽酸鹽，再經(jīng)過(guò)氯磺化、胺解、烴化、氫解和成鹽合成鹽酸坦索羅辛。結(jié)果 該合成工藝鹽酸坦索羅辛的總收率為26%。結(jié)論 該合成方法步驟短，易于操作。

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.