A highly enantioselective aza-Friedel-Crafts alkylation of indoles with cyclic aryl alpha-ketimino esters catalyzed by a chiral phosphoric acid has been developed, the corresponding alpha,alpha-disubstituted unnatural alpha-amino ester derivatives were obtained in moderate to high yields (67-85%) with high enantioselectivities (up to 93% ee) under mild reaction conditions. (C) 2016 Published by Elsevier Ltd.
机构:
Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China
Univ Chinese Acad Sci, Beijing 100049, Peoples R ChinaSun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
Ding, Yu-Yang
Xu, Deng-Feng
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Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R ChinaSun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
Xu, Deng-Feng
Meng, Shan-Shui
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Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R ChinaSun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
Meng, Shan-Shui
Li, Yang
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Dalian Univ Technol, Sch Petr & Chem Engn, Stat Key Lab Fine Chem, Panjin 124000, Peoples R ChinaSun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
Li, Yang
Zhao, Jun-Ling
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Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R ChinaSun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
机构:
Jilin Med Univ, Dept Pharm, Changchun 132013, Jilin, Peoples R China
Acad Mil Med Sci, Inst Mil Vet Sci, Changchun, Jilin, Peoples R ChinaJilin Med Univ, Dept Pharm, Changchun 132013, Jilin, Peoples R China
Li, Ya Wei
Wang, Li Ming
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Jilin Med Univ, Dept Pharm, Changchun 132013, Jilin, Peoples R ChinaJilin Med Univ, Dept Pharm, Changchun 132013, Jilin, Peoples R China
Wang, Li Ming
Jin, Ying
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Jilin Med Univ, Dept Pharm, Changchun 132013, Jilin, Peoples R ChinaJilin Med Univ, Dept Pharm, Changchun 132013, Jilin, Peoples R China
Jin, Ying
Chang, Sheng
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Jilin Med Univ, Dept Pharm, Changchun 132013, Jilin, Peoples R ChinaJilin Med Univ, Dept Pharm, Changchun 132013, Jilin, Peoples R China