Development of a Pilot-Plant Process for a Nevirapine Analogue HIV NNRT Inhibitor

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• 作者：Carl A. Busacca ; Mike Cerreta ; Yong Dong ; Magnus C. Eriksson ; Vittorio Farina ; XuWu Feng ; Ji-Young Kim ; Jon C. Lorenz ; Max Sarvestani ; Robert Simpson ; Rich Varsolona ; Jana Vitous ; Scot J. Campbell ; Ma
• 刊名：Organic Process Research & Development
• 出版年：2008
• 出版时间：July 2008
• 年：2008
• 卷：12
• 期：4
• 页码：603-613
• 全文大小：266K
• 年卷期：v.12,no.4(July 2008)
• ISSN：1520-586X

文摘

The pilot-plant synthesis of nevirapine analogue 1 is described. The compound was prepared in eight steps from substituted pyridine raw materials and 4-hydroxyquinoline. The key transformation involves a novel one-pot conversion of an arylhalide to arylacetic acid under palladium catalysis, followed by regioselective reduction via in situ generated BH₃/THF to the arylethanol intermediate 2. All stages were carried out on 10−150-kg scale.