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Synlett 1999; 1999(12): 1957-1959
DOI: 10.1055/s-1999-2987
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Two Efficient N-Acylation Methods Mediated by Solid-Supported Reagents for Weakly Nucleophilic Heterocyclic Amines

Kyungjin Kim* , Kang Le
  • *Roche Research Center, Hoffmann-La Roche, Inc., Nutley, NJ 07110-1199, USA; Fax + 1-9 73-2 35-60 84; E-mail: kyungjin.kim@roche.com
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Publication Date:
31 December 1999 (online)

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Two efficient acylation methods utilizing solid-supported reagents have been developed for weakly nucleophilic heterocyclic amines. The novel approaches by chemoselective purification and polymeric-supported reagents facilitate library synthesis of diverse heterocyclic amides that are found in several pharmacophores.

acylation - amide - chemoselective purification - combinatorial chemistry - solid-supported reagents

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