Development of an Alternate Synthesis for a Key JAK2 Inhibitor Intermediate via Sequential C鈥揌 Bond Functionalization
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- 作者：Alison N. Campbell ; Kevin P. Cole ; Joseph R. Martinelli ; Scott A. May ; David Mitchell ; Patrick M. Pollock ; Kevin A. Sullivan
- 刊名：Organic Process Research & Development
- 出版年：2013
- 出版时间：February 15, 2013
- 年：2013
- 卷：17
- 期：2
- 页码：273-281
- 全文大小：366K
- 年卷期：v.17,no.2(February 15, 2013)
- ISSN：1520-586X
文摘
The development of an alternative synthetic route to a functionalized imidazopyridazine which strategically streamlines the synthesis and avoids a number of problematic reagents is described. Key to the success of this alternative route is the use of two C鈥揌 functionalization reactions: a Pd-catalyzed direct benzylation reaction to functionalize a C鈥揌 bond with a substituted benzyl group and a V-catalyzed NMO addition reaction to install a benzylic morpholine moiety.