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    • 1. 发明授权
    • Methods of synthesis of certain hydroxamic acid compounds
    • 合成某些异羟肟酸化合物的方法
    • US08642809B2
    • 2014-02-04
    • US12678594
    • 2008-09-23
    • Helge A. ReischPeter LeemingPrasad S. Raje
    • Helge A. ReischPeter LeemingPrasad S. Raje
    • C07C303/00
    • C07C303/40C07C311/21
    • The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD101 and Belinostat®, comprising, for example, the steps of: (SAF) sulfonamide formation; (PURC) optional purification; (AAA) alkenyl-acid addition, comprising: either (i): the steps of, in order: (ACAEA) alkenyl-carboxylic acid ester addition; (PURE) optional purification; and (CAD) carboxylic acid deprotection; or (ii): the step of: (ACAA) alkenyl-carboxylic acid addition; (PURF) optional purification; (HAF) hydroxamic acid formation; and (PURG) optional purification.
    • 本发明涉及化学合成的一般领域,更具体地涉及合成某些异羟肟酸化合物,特别是(E)-N-羟基-3-(3-苯基氨磺酰基 - 苯基) - 丙烯酰胺的方法, 也称为PXD101和Belinostat,包括例如以下步骤:(SAF)磺酰胺的形成; (PURC)可选净化; (AAA)烯基酸添加,包括:(i):以下步骤:按顺序:(ACAEA)烯基 - 羧酸酯添加; (PURE)可选净化; 和(CAD)羧酸脱保护; 或(ii):步骤:(ACAA)烯基 - 羧酸添加; (PURF)可选净化; (HAF)异羟肟酸形成; 和(PURG)可选纯化。