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Sunday, 25 September 2016

A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives

Image result for A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives








A highly efficient and green method has been developed for the rapid preparation of highly functionalized isoxazolopyridin-3-amine derivatives in excellent yields. This process has a broad substrate scope, is operationally simple, and generally requires no chromatographic purification. In addition, the process is scalable and significantly greener than current alternatives with a PMI of 18 and water as the reaction solvent.



Graphical abstract: A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives


Image result for A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives

Image result for A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives









































Image result for A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives











Image result for A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives


Image result for A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives



A rapid preparation of highly functionalized isoxazolopyridin-3-amine and other heterocyclic fused aminoisoxazole derivatives


A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives

Wensheng Yu,*a   Paul G. Bulgerb and   Kevin M. Maloney*b  

*
Corresponding authors
a
Discovery Chemistry, Merck Research Laboratories, 126 E. Lincoln Avenue, Rahway, USA
E-mail: wensheng.yu@merck.com
b
Process Chemistry, Merck Research Laboratories, 126 E. Lincoln Avenue, Rahway, USA
Green Chem., 2016,18, 4941-4946

DOI: 10.1039/C6GC01125J















http://pubs.rsc.org/en/Content/ArticleLanding/2016/GC/C6GC01125J?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract


Wensheng Yu


Wensheng Yu

Associate Principal Scientist at Merck



Image result for Paul G. Bulger merck

Paul G. Bulger was born in London, England, in 1978. He received his undergraduate M.Chem degree in 2000 from the University of Oxford, completing his Part II project under the supervision of Dr. Mark G. Moloney. He remained at Oxford for his graduate studies, obtaining his D. Phil. in chemistry in 2003 for research conducted under the supervision of Professor Sir Jack E. Baldwin. After an enjoyable three-year stint as a postdoctoral researcher in Professor K. C. Nicolaou's group at The Scripps Research Institute, he joined the Process Research Department of Merck & Co., Inc. in the fall of 2006.






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Kevin Maloney

Sr Research Chemist at Merck Sharp & Dohme


Experience


Sr Research Chemist

Merck
 – Present (9 years)

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