Process Development and Large-Scale Synthesis of MK-6186, a Non-Nucleoside Reverse Transcriptase Inhibitor for the Treatment of HIV

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• 作者：Adrian Goodyear ; Xin Linghu ; Brian Bishop ; Cheng Chen ; Ed Cleator ; Mark McLaughlin ; Faye J. Sheen ; Gavin W. Stewart ; Yingju Xu ; Jingjun Yin.
• 刊名：Organic Process Research & Development
• 出版年：2012
• 出版时间：April 20, 2012
• 年：2012
• 卷：16
• 期：4
• 页码：605-611
• 全文大小：303K
• 年卷期：v.16,no.4(April 20, 2012)
• ISSN：1520-586X

文摘

A new synthetic route has been developed to drug candidate 1, a second-generation NNRTI being developed as a potential treatment of HIV. Regiocontrol in a key alkylation step was achieved by selective N-alkylation of hydrazone 13. After a deprotection and cyclisation sequence, 1 was isolated in six steps in 35% overall yield from readily available starting materials.