Synthesis of substituted benzoimidazole derivatives as potent and selective histamine-3 receptor antagonists

ORGN 821

Tim Grieme, timothy.grieme@abbott.com1, Yi-Yin Ku, yiyin.ku@abbott.com1, Yu-Ming Pu1, Marlon Cowart2, and Timothy A. Esbenshade2. (1) D-R450, Process Chemistry, Abbott Laboratories, 1401 Sheridan Rd, North Chicago, IL 60064, (2) Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, R4MN, AP9A, 100 Abbott Park Road, Abbott Park, IL 60064-6123
The benzoimidazole core was synthesized from inexpensive and readily available starting materials in 3 chemical steps.  The process proceeded through a Michael addition of the amine functionality with ethyl acrylate before cyclization to give the benzoimidazole core.  The benzoimidazole core was then derivatized by a Suzuki cross coupling reaction with a variety of aryl and heteroaryls. 

 

Combinatorial, Parallel and Process Chemistry, Heterocycles, Aromatics, New Reactions and Methodology
8:00 PM-10:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster

Division of Organic Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007