Telescoped Approach to Aryl Hydroxymethylation in the Synthesis of a Key Pharmaceutical Intermediate
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- 作者：Catherine N. Slattery ; Rebecca E. Deasy ; Anita R. Maguire ; Michael E. Kopach ; Utpal K. Singh ; Mark D. Argentine ; William G. Trankle ; Roger Brian Scherer ; Humphrey Moynihan
- 刊名：The Journal of Organic Chemistry
- 出版年：2013
- 出版时间：June 21, 2013
- 年：2013
- 卷：78
- 期：12
- 页码：5955-5963
- 全文大小：329K
- 年卷期：v.78,no.12(June 21, 2013)
- ISSN：1520-6904
文摘
An efficient synthetic approach leading to introduction of the hydroxymethyl group to an aryl moiety via combination of the Bouveault formylation and hydride reduction has been optimized using a rational, mechanistic-based approach. This approach enabled telescoping of the two steps into a single efficient process, readily amenable to scaleup.