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。
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.
出处
《现代药物与临床》
CAS
2013年第2期123-125,共3页
Drugs & Clinic
关键词
盐酸坦索罗辛
不对称合成
氯磺化、胺解、烃化、氢解
tamsulosin hydrochloride
asymmetric synthesis
chlorosulfonation
amination
alkylation
hydrogenolysis
