Practical synthesis of gemcitabine, an anticancer agent

ORGN 83

Wen-sen Li, wensen_li@pharmaessentia.com1, Craig N. Zimmerman, czimmerman@molecularinsight.com2, and Yungshung Wein1. (1) New product development, Pharmaessentia Corp, 13 floor, No. 3, YangQu St., NanKang Dist, Taipei, Taiwan, (2) Chemistry, Molecular Insight Pharmaceuticals, 160 Second Street, Cambridge, MA 02142
Gemcitabine, an effective anticancer agent that is marketed by the Eli Lilly Company, and has been a challenging synthetic target for the producers of active pharmaceutical ingredients and generic drug manufacturerss. Due to its structural complexity, the development of a practical, freedom-to-operate process for its production has been not realized. Pharmaessentia has instituted a non-chromatographic method to efficiently isolate the major desired Reformatsky product in the synthetic route. The early separation/purification of the Reformatsky product increases the efficiency and eases the synthetic process. The details of this improved synthesis of gemcitabine will be described.

 

Physical Organic Chemistry, Combinatorial and Process Chemistry, New Reactions and Methodology, Peptides, Proteins and Amino Acids
8:00 PM-10:00 PM, Sunday, April 6, 2008 Morial Convention Center -- Hall A, Poster

Division of Organic Chemistry

The 235th ACS National Meeting, New Orleans, LA, April 6-10, 2008