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Thursday, August 27 • 2:00pm - 2:40pm
[0196] Old Methods to New Targets: Accessing Highly Functionalized Heterocycles for Drug Development

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The development of a practical and efficient synthesis of an investigational drug candidate will be described.  A Vilsmeier-Haak quinolinone synthesis was first developed to support the initial multi-kilo manufactures.  Alternative chemistry based on a highly selective Friedlander cyclization was later discovered to provide efficient access to the key quinolinone intermediate. Development of subsequent transformations to access the target molecule including development of a  challenging Negishi coupling and selective oxime hydrogenation will also be described.  The process development ultimately provided access to the non-racemic drug candidate in 5-step chiral process with a 47% overall yield

Invited Lecturers
avatar for Christopher Borths

Christopher Borths

Senior Scientist, Amgen
Senior ScientistAmgenMarch 2010 – Present (5 years 1 month)ScientistAmgenAugust 2004 – March 2010 (5 years 8 months)EducationCaltech  Ph.D., Chemistry  2000 – 2004University of California, Berkeley  M.S., Chemistry  1998 – 2000University of Kentucky  B.S... Read More →

Thursday August 27, 2015 2:00pm - 2:40pm
MCC Theater