A Scalable Synthesis of a Hydroxamic Acid LpxC Inhibitor
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- 作者：ZhongBo Fei ; Weiyong Kong ; Huaimin Wang ; Jianbiao Peng ; Feng Sun ; Yueyan Yin ; Joginder Bajwa ; Xinglong Jiang
- 刊名：Organic Process Research & Development
- 出版年：2012
- 出版时间：August 17, 2012
- 年：2012
- 卷：16
- 期：8
- 页码：1436-1441
- 全文大小：291K
- 年卷期：v.16,no.8(August 17, 2012)
- ISSN：1520-586X
文摘
A short and scalable synthesis of chiral hydroxamic acid 1, a LpxC inhibitor, is described. This work discloses a novel diastereoselective addition of 2-nitropropane-generated lithium salt to tert-butanesulfinimine. Moreover, the impurity profiles of reactions giving oily products and practical means of purifying these products are discussed in detail.