Semi-synthesis of taxol by technological improvement
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TQ460.31

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    Abstract:

    The C-13 side-chain precursor (4R,5S)-2,4-diphenyl-4,5-dihydroxazole-5- carboxylic acid was prepared from Cinnamic acid via epoxidation of C=C double bond with Oxone,benzyl protection, Ritter reaction, hydrolyzation, and resolution with (+)-Quinidine. Thus by linking it to 7-TES-Baccatin Ⅲ, taxol could be synthesized. The yield is 4.5% in the overall steps. Some intermediates and the target product were identified by means of 1H-NMR, 13C-NMR and MS.

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History
  • Received:October 26,2012
  • Revised:January 27,2013
  • Adopted:January 31,2013
  • Online: May 03,2013
  • Published: