| 新型苯并吡喃类FSH拮抗剂的合成 |
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| 引用本文： | 王志涛,吕兰亭,任二勇,王旭东,张瑞,毛龙飞,姜玉钦.新型苯并吡喃类FSH拮抗剂的合成[J].合成化学,2017,25(10). |
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| 作者姓名： | 王志涛 吕兰亭 任二勇 王旭东 张瑞 毛龙飞 姜玉钦 |
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| 作者单位： | 1. 天方药业有限公司,河南驻马店,463000;2. 河南师范大学化学化工学院,河南省手性醇类药物工程技术研究中心,河南新乡 453007 |
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| 基金项目： | 河南省杰出青年创新人才项目 |
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| 摘 要： | 以2-溴-4,5-二甲氧基苄溴为起始原料,依次经取代、Sonogoshira偶联、水解、酰化和氧化反应合成了新型FSH拮抗剂——(R)-N-1-羟基-3-(1H-吲哚-3-基)丙烷-2-基]-3-异丙氧基-8,9-二甲氧基-6H-苯并c]苯并吡喃-2-甲酰胺,总收率16.8%,其结构经~1H NMR和MS(ESI)确证。
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| 关 键 词： | 2-溴-4 5-二甲氧基苄溴 FSH拮抗剂 (R)-N-(1-羟基-3-(1H-吲哚-3-基)丙烷-2-基)-3-异丙氧基-8 9-二甲氧基-6H-苯并[c]苯并吡喃-2-甲酰胺 药物合成 |
Synthesis of A Novel FSH Antagonist of Benzopyrans |
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| WANG Zhi-tao,L&#; Lan-ting,REN Er-yong,WANG Xu-dong,ZHANG Rui,MAO Long-fei,JIANG Yu-qin.Synthesis of A Novel FSH Antagonist of Benzopyrans[J].Chinese Journal of Synthetic Chemistry,2017,25(10). |
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| Authors: | WANG Zhi-tao L&#; Lan-ting REN Er-yong WANG Xu-dong ZHANG Rui MAO Long-fei JIANG Yu-qin |
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| Institution: | WANG Zhi-tao,Lü Lan-ting,REN Er-yong,WANG Xu-dong,ZHANG Rui,MAO Long-fei,JIANG Yu-qin |
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| Abstract: | A FSH inhibitor, (R)-N-1-hydroxy-3-(1H-indol-3-yl)propan-2-yl]-3-isopropoxy-8,9-di-methoxy-6H-benzoc]chromene-2-carboxamide with the total yield of 16.8%, was synthesized by re-action of substitution , Sonogoshira coupling , hydrolysis and oxidation reaction , using 2-bromo-4 ,5-di-methoxybenzyl as the starting material .The structure was confirmed by 1 H NMR and MS( ESI) . |
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| Keywords: | 2-bromo-4 5-dimethoxybenzyl bromide FSH antagonist ( R)-N-[1-hydroxy-3-(1H-in-dol-3-yl) propan-2-yl]-3-isopropoxy-8 9-dimethoxy-6H-benzo[ c] chromene-2-carboxamide drug syn-thesis |
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