Addition of benzylic and allylic organozinc and Grignard reagents to resin-bound imines to provide alpha-branched secondary amines bearing a wide variety of functional groups. Utility in the synthesis of beta-3 adrenergic receptor agonists |
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| Authors: | Wu Gang Cai Zhen-Wei Bednarz Mark S Kocy Octavian R Gavai Ashvinikumar V Godfrey Jollie D Washburn William N Poss Michael A Sher Philip M |
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| Institution: | Bristol-Myers Squibb Pharmaceutical Research Institute, P O Box 5400, Princeton, New Jersey 08543, USA. |
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| Abstract: | Benzylic and allylic organozinc and Grignard reagents have been added to resin-bound imines to provide alpha-branched secondary amines. Many functional groups, including electrophilic groups, were compatible with this methodology. Three modules--a resin-bound primary amine, an aromatic aldehyde, and the organometallic--were independently varied to produce a combinatorial library of alpha-branched secondary amines designed as beta-3 adrenergic receptor agonists. |
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