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

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-hydrox...

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Published in中国化学：英文版 Vol. 29; no. 12; pp. 2581 - 2583
Main Author 李晓明 马欣 李万方 陶晓明 孟庆华 范为正 张兆国
Format Journal Article
LanguageEnglish
Published 2011
Subjects
os系统
不对称催化加氢
不对称氢化
合成
噻吩
增强剂
甲酸乙酯
苯
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Summary: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.
Bibliography: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.
T-588, asymmetric catalysis, hydrogenation, SunPhos
31-1547/O6
ISSN:1001-604X
1614-7065