盐酸坦索罗辛的合成 |
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引用本文: | 何训贵,王元,吴建才.盐酸坦索罗辛的合成[J].中国医药工业杂志,2011,42(8):565-568. |
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作者姓名: | 何训贵 王元 吴建才 |
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作者单位: | 药源药物化学(上海)有限公司,上海,201203 |
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基金项目: | 上海市科学委员会资助,资助课题编号为09QB1404300 |
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摘 要: | 以4-甲氧基苯丙酮为原料,依次经过(R)-苯乙胺诱导的还原胺化、氯乙酰化、氯磺化和氨化反应制得N-(R)-2-(4-甲氧基-3-氨基磺酰基苯基)-1-甲基乙基]-N-(R)-(1-苯乙基)-氯乙酰胺,再经烷基化、还原和催化脱苄等反应制得盐酸坦索罗辛,总收率约15%.
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关 键 词: | 坦索罗辛 良性前列腺增生 α-肾上腺素受体拮抗剂 合成 |
Synthesis of Tamsulosin Hydrochloride |
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Authors: | HE Xungui WANG Yuan WU Jiancai |
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Affiliation: | HE Xungui,WANG Yuan,WU Jiancai (2Y-Chem.,Ltd.,Shanghai 201203) |
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Abstract: | Tamsulosin hydrochloride was synthesized from 4-methoxyphenylacetone by reductive amination with chiral induction of(R) -phenethylamine,chloracetylation,chlorosulfonation and amination to give N-(R) -2-(4-methoxy -3-aminosulfonylphenyl)-1-methylethyl]-N-(R)-(1-phenylethyl)-chloroacetamide,which was subjected to alkylation,reduction and catalytic debenzylation with an overall yield of 15%. |
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