An improved synthesis of anticancer benzothiopyranoindazoles. An efficient large??scale β??aminoethylation procedure

…, AB Giordani, OP Goel, DR Johnson…

文献索引：Beylin; Colbry; Giordani; Goel; Johnson; Leeds; Leja; Lewis; Lustgarten; Showalter; Sercel; Reily; Uhlendorf; Zisek Journal of Heterocyclic Chemistry, 1991 , vol. 28, # 2 p. 517 - 527

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被引用次数: 8

摘要

Abstract Improved processes for the synthesis of bulk quantities of the benzothiopyranoindazole clinical agent CI-958 and A-ring congeners is reported. The process chosen for scale-up operations achieves β-aminoethylation of an anilino precursor via a three-step sequence (acylation, reduction, deprotection) starting from N-(trityl) glycine. Detailed analytical data are reported for the target compounds and most intermediates, ...