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

…, CC Tseng, TC Jones, AD Kohler, GJ Ellames

文献索引：Spivey, Alan C.; Tseng, Chih-Chung; Jones, Teyrnon C.; Kohler, Andrew D.; Ellames, George J. Organic Letters, 2009 , vol. 11, # 20 p. 4760 - 4763

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被引用次数: 11

摘要

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/ ...