A Facile Total Synthesis for Large-Scale Production of Imatinib Base

作者:Kompella Amala*; Adibhatla Bhujanga Rao Kalisatya; Muddasani Pulla Reddy; Rachakonda Sreenivas; Gampa Venugopala Krishna; Dubey Pramod Kumar
来源:Organic Process Research & Development, 2012, 16(11): 1794-1804.
DOI:10.1021/op300212u

摘要

An efficient, economic process has been developed for the production of imatinib with 99.99% purity and 50% overall yield from four steps. Formation and control of all possible impurities is described. The synthesis comprises the condensation of N-(5-amino-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidineamine with 4-(4-methylpiperazinomethyl)benzoyl chloride in isopropyl alcohol solvent in the presence of potassium carbonate to yield imatinib base.

  • 出版日期2012-11