Reversible carboxamide-mediated internal activation at C(6) of 2-chloro-4-anilino-1H-pyrrolo[2,3-d]pyrimidines |
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| Authors: | Chamberlain Stanley D Gerding Roseanne M Lei Huangshu Moorthy Ganesh Patnaik Samarjit Redman Anikó M Stevens Kirk L Wilson Joseph W Yang Bin Shotwell J Brad |
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| Institution: | GlaxoSmithKline, Oncology R&D, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. |
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| Abstract: | A synthetic route to bisanilino-1H-pyrrolo2,3-d]pyrimidines has been discovered, wherein the C(6)-chloride reactivity is necessarily enhanced via reversible acid-catalyzed internal activation of the pyrimidine ring by a C(1')-carboxamide moiety. Subsequent selective nucleophilic displacements at C(6) and C(1') constitute a one-pot tandem protocol for the rapid assembly of bisanilino-1H-pyrrolo2,3-d]pyrimidines. |
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