Palladium-catalyzed heteroarylamination of ethyl 2-chloro-1-azaazulene-3-carboxylate and annulation of heteroarylamino-1-azaazulenes

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Abstract

The palladium catalyzed heteroarylamination of ethyl 2-chloro-1-azaazulene-3-carboxylate was achieved using a catalyst based on Pd2(dba)3 / Xantphos system. Treatment of ethyl 2-(heteroarylamino)-1-aza-azulene-3-carboxylates with a PPA-POCl3 mixture gave corresponding annulation products. 2-(2-Benzothiazolylamino)-1-azaazulene (3h) showed anticancer activity against HeLa S3 cells (IC50: 6.5 μM).

Journal

  • Heterocycles

    Heterocycles 79 (1), 319-324, 2009-04

    日本複素環化学研究所

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