苯并噻二嗪取代的四嗪酸的高效不对称固相合成：丙型肝炎病毒RNA依赖性RNA聚合酶的有效抑制剂。
An efficient, asymmetric solid-phase synthesis of benzothiadiazine-substituted tetramic acids: potent inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
作者信息
Evans Karen A, Chai Deping, Graybill Todd L, Burton George, Sarisky Robert T, Lin-Goerke Juili, Johnston Victor K, Rivero Ralph A
机构信息
Department of Discovery Research, GlaxoSmithKline Pharmaceuticals, Collegeville, PA 19426-0989, USA.
出版信息
Bioorg Med Chem Lett. 2006 Apr 15;16(8):2205-8. doi: 10.1016/j.bmcl.2006.01.034. Epub 2006 Feb 7.
An efficient, asymmetric solid-phase synthesis of benzothiadiazine-substituted tetramic acids is reported. Starting from commercially available chiral Fmoc-protected alpha-amino acids loaded onto Wang resin, Fmoc removal, reductive amination followed by amide bond formation, and base-catalyzed cyclization with simultaneous cleavage from the resin provided the desired products. Compounds described are potent inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
报道了一种高效的、不对称的固相合成苯并噻二嗪取代四嗪酸的方法。从负载在王树脂上的市售手性Fmoc保护的α-氨基酸开始，通过Fmoc去除、还原胺化随后形成酰胺键，以及碱催化环化并同时从树脂上裂解，得到了所需产物。所描述的化合物是丙型肝炎病毒RNA依赖性RNA聚合酶的有效抑制剂。
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