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Catalytic Asymmetric Hydrogenation of Ethyl 2-（Benzo[b]thiophen-5-yl）-2-oxoacetate with Ru-SunPhos in the Formal Synthesis of T-588

ISSN号：1001-604X
期刊名称：《中国化学：英文版》
分类：O621.254[理学—有机化学;理学—化学] S379.5[农业科学—农产品加工;农业科学—农艺学]
作者机构：[1]School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China, [2]Shanghai Isntitute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China
相关基金：Project supported by the National Natural Science Foundation of China （No. 20872090）.

作者：李晓明[1], 马欣[1], 李万方[1], 陶晓明[1], 孟庆华[1], 范为正[1], 张兆国[1,2]

关键词：不对称催化加氢, 甲酸乙酯, 噻吩, 合成, 苯, 不对称氢化, OS系统, 增强剂, T-588, asymmetric catalysis, hydrogenation, SunPhos

中文摘要：

乙醇 2- 的催化不对称的加氢的申请(benzo [b ] thiophen-5-yl ) 为认知 enhancer T-588 的正式合成的 -2-oxoacetate 被描述。加氢作为添加剂与 HCl 在 Ru-SunPhos 系统的催化作用下面被进行。乙醇 2-(benzo [b ] thiophen-5-yl )-2-hydroxy-acetate 与 98.6% ee 被获得，它能容易在简单再结晶以后被升级到 99.5% ee 并且在 T-588 的合成用作关键中介。

英文摘要：

Application of catalytic asymmetric hydrogenation of ethyl 2-（benzo[b]thiophen-5-yl）-2-oxoacetate for the formal synthesis of cognitive enhancer T-588 is described. The hydrogenation was conducted under the catalysis of Ru-SunPhos system with HC1 as additive. Ethyl 2-（benzo[b]thiophen-5-yl）-2-hydroxy-acetate was obtained with 98.6% ee, which could be easily upgraded to 99.5% ee after a simple recrystallization and served as the key intermediate in the synthesis of T-588.

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