A Reductive Amination/Lactamization Procedure Using Borohydride Reagents

Ahmed F. Abdel-Magid; Bruce D. Harris; Cynthia A. Maryanoff

doi:10.1055/s-1994-22747

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Synlett 1994; 1994(1): 81-83
DOI: 10.1055/s-1994-22747

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A Reductive Amination/Lactamization Procedure Using Borohydride Reagents

Ahmed F. Abdel-Magid^* , Bruce D. Harris, Cynthia A. Maryanoff

^*The R. W. Johnson Pharmaceutical Research Institute, Chemical Development Department, Spring House, PA 19477, USA

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Publication Date:
22 March 2002 (online)

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We report a procedure for tandem reductive aminationlactamization of aldehydes or ketones with aminoesters or ketoesters with primary amines under mild conditions (NaBH(OAc)₃/1,2-dichloroethane or NaBH₄/ MeOH).

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