A method for parallel solid-phase synthesis of iodinated analogues of the CB1 receptor inverse agonist rimonabant.

نویسندگان

  • Alan C Spivey
  • Chih-Chung Tseng
  • Teyrnon C Jones
  • Andrew D Kohler
  • George J Ellames
چکیده

A method for the parallel solid-phase synthesis (SPS) of iodinated analogues of Sanofi-Aventis' type 1 cannabinoid (CB1) receptor inverse agonist rimonabant (acomplia) has been developed. The method allows the synthesis of a range of C3 amide/hydrazide derivatives from a resin-bound C3 ester precursor. The C-Ge linkage to the Hypogel-200 resin is stable to the diversification conditions but allows ipso-iododegermylative cleavage using NaI/NCS even for the products containing the oxidatively labile hydrazide moiety.

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عنوان ژورنال:
  • Organic letters

دوره 11 20  شماره 

صفحات  -

تاریخ انتشار 2009