A novel asymmetric synthetic strategy to prepare 4-aryl-dihydroisoquinolinones has been developed through a highly regioselective Friedel-Crafts alkylation of benzylamine derivatives with (alpha R)-alpha-bromo arylacetates and subsequent facile lactamization. In addition, an efficient asymmetric synthesis of 2-aryl morpholinones is demonstrated with 2-aminoethanol derivatives using the same convenient substitution-lactamization protocol. (C) 2019 Elsevier Ltd. All rights reserved.
机构:
Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
Gonzalez, Ana Z.
Eksterowicz, John
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Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
Eksterowicz, John
Bartberger, Michael D.
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Amgen Inc, Dept Therapeut Discovery, Thousand Oaks, CA 91320 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
Bartberger, Michael D.
Beck, Hilary P.
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Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
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Canon, Jude
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Amgen Inc, Dept Oncol Res, Thousand Oaks, CA 91320 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
Canon, Jude
Chen, Ada
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Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
Chen, Ada
Chow, David
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Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
Chow, David
Duquette, Jason
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Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
Duquette, Jason
Fox, Brian M.
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Fox, Brian M.
Fu, Jiasheng
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Fu, Jiasheng
Huang, Xin
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Houze, Jonathan B.
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Houze, Jonathan B.
Jin, Lixia
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Li, Yihong
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Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
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Li, Zhihong
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Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
Li, Zhihong
Ling, Yun
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Ling, Yun
Lo, Mei-Chu
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Osgood, Tao
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Univ Lille Nord France, F-59000 Lille, France
ENSCL, CCM CCCF, F-59652 Villeneuve Dascq, FranceUniv Lille Nord France, F-59000 Lille, France
Keldenich, Jerome
Denicourt-Nowicki, Audrey
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Univ Lille Nord France, F-59000 Lille, France
ENSCL, CCM CCCF, F-59652 Villeneuve Dascq, FranceUniv Lille Nord France, F-59000 Lille, France
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Michon, Christophe
Agbossou-Niedercorn, Francine
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Univ Lille Nord France, F-59000 Lille, France
CNRS, UCCS UMR 8181, F-59655 Villeneuve Dascq, France
ENSCL, CCM CCCF, F-59652 Villeneuve Dascq, FranceUniv Lille Nord France, F-59000 Lille, France
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Amgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USAAmgen Inc, Dept Therapeut Discovery, 1120 Vet Blvd, San Francisco, CA 94080 USA
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机构:
Univ Lille Nord France, F-59000 Lille, France
ENSCL, CCM CCCF, F-59652 Villeneuve Dascq, FranceUniv Lille Nord France, F-59000 Lille, France
Keldenich, Jerome
Denicourt-Nowicki, Audrey
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Univ Lille Nord France, F-59000 Lille, France
ENSCL, CCM CCCF, F-59652 Villeneuve Dascq, FranceUniv Lille Nord France, F-59000 Lille, France
Denicourt-Nowicki, Audrey
Michon, Christophe
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Univ Lille Nord France, F-59000 Lille, France
CNRS, UCCS UMR 8181, F-59655 Villeneuve Dascq, France
ENSCL, CCM CCCF, F-59652 Villeneuve Dascq, FranceUniv Lille Nord France, F-59000 Lille, France
Michon, Christophe
Agbossou-Niedercorn, Francine
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Univ Lille Nord France, F-59000 Lille, France
CNRS, UCCS UMR 8181, F-59655 Villeneuve Dascq, France
ENSCL, CCM CCCF, F-59652 Villeneuve Dascq, FranceUniv Lille Nord France, F-59000 Lille, France