An Efficient Synthesis of 3-Substituted N -Glycoside Indoles Useful as Sodium-Dependent Glucose Transporter Inhibitors
Organic Process Research & Development(2012)
摘要
A practical synthesis of two N-glycoside indoles 1 and 2, identified as highly potent sodium-dependent glucose transporter (SGLT) inhibitors is described. Highlights of the synthetic process include a selective and quantitative Vilsmeier acylation and a high-yielding Grignard coupling reaction. The chemistry developed has been applied to prepare two separate SGLT inhibitors 1 and 2 for clinical evaluation without recourse to chromatography.
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关键词
indoles,glucose,inhibitors,synthesis,sodium-dependent
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