A method for parallel solid-phase synthesis of iodinated analogues of the CB1 receptor inverse agonist rimonabant.
A method for parallel solid-phase synthesis of iodinated analogues of the CB1 receptor inverse agonist rimonabant.
复制标题
CB1受体反向激动剂利莫那班的碘化类似物的平行固相合成方法。
DOI：
10.1021/ol902038y
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发表时间：
2009
期刊：
影响因子：
5.2
通讯作者：
Spivey AC
中科院分区：
文献类型：
--
作者：
Spivey AC
建立了一种平行固相合成赛诺菲-安万特1型大麻素受体逆激动剂利莫那班（acomplia）碘化类似物的方法。该方法允许从树脂结合的C3酯前体合成一系列C3酰胺/肼衍生物。在多样化条件下，与Hypogel-200树脂的C−Ge连接是稳定的，但即使对于含有氧化不稳定的酰肼部分的产物，也允许使用NaI/NCS进行siso -碘脱菌裂解。
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 allowsipso-iododegermylative cleavage using NaI/NCS even for the products containing the oxidatively labile hydrazide moiety.