Optimization of the Synthetic Process of INCB024360 as IDO1 Inhibitor
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O626;O625.6

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    Abstract:

    3-amino-4-amino oximidofurazan was obtained from the malononitrile through the one pot method of four-step consecutive reaction, which was diazotized by the Sandmeyer raction to get 3-amino-4-acid chloride oximidofurazan. Then, it was converted into 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide(INCB024360) via the substitution with 3-chloro-4-fluoro aniline with the overall yield increased from 10.0% to 43.1% and the HPLC purity of 99.6% in the best synthetic process. The structures were characterized by 1H NMR, 13C NMR, MS.

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History
  • Received:March 09,2015
  • Revised:May 12,2015
  • Adopted:May 25,2015
  • Online: August 12,2015
  • Published:
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