磷酸二酯酶抑制剂西地那非的合成 |
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引用本文: | 宁奇,张秀平.磷酸二酯酶抑制剂西地那非的合成[J].中国医药工业杂志,2000,31(4):145-147. |
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作者姓名: | 宁奇 张秀平 |
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作者单位: | 上海医药工业研究院!上海200437 |
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摘 要: | 以2-戊酮为原料,经酶酮综合、肼解环合、甲基化、水解、硝化、酰胺化、铁粉还原、酰胺化、环合、氯磺酰化、磺酰胺化等11步反应合成西地那非。经工艺改进,我步收率有较大提高,总收率为14.2%。
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关 键 词: | 磷酸二酯酶Ⅴ型抑制剂 西地那非 合成 |
修稿时间: | 1999-12-28 |
Synthesis of Sildenafil |
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Authors: | NING Qi ZHANG Xiu Ping |
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Affiliation: | NING Qi,ZHANG Xiu Ping * |
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Abstract: | Sildenafil was synthesized from 2 pentanone via Claisen condensation,hydrazinolytic cyclization,methylation,hydrolysis,nitration,amidation,reduction,2 ethoxybenzoyl chloride acylation,oxidative cyclization,chlorosulfonation, N methylpiperazine condensation.Some reaction conditions had been improved and the total yield raised to 14.2% by using the cheaper reagents. |
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Keywords: | phosphodiesterase V inhibitor sildenafil synthesis |
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