Practical Synthesis of A Benzophenone-Based NNRT Inhibitor of HIV-1
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- 作者：Xiao-jun Wang ; Li Zhang ; Xiufeng Sun ; Heewon Lee ; Dhileepkumar Krishnamurthy ; Jeff A. O鈥橫eara ; Serge Landry ; Christiane Yoakim ; Bruno Simoneau ; Nathan K. Yee ; Chris H. Senanayake
- 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：561-566
- 全文大小：282K
- 年卷期：v.16,no.4(April 20, 2012)
- ISSN：1520-586X
文摘
A convergent synthesis of NNRTI 1 is described. The key step involves a direct coupling of acid chloride 4 with Grignard reagent 11 in the presence of bis[2-(N,N-dimethylamino)ethyl] ether that moderates the reactivity of the Grignard reagent to give benzophenone 7. An efficient 2-step process for the preparation of 2-fluoro-3-methyl-4-aminobenzoic acid (3) is also described.