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Synfacts 2006(9): 0875-0875
DOI: 10.1055/s-2006-942056
DOI: 10.1055/s-2006-942056
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York
Synthesis of Torcetrapib
D. B. Damon, R. W. Dugger, S. E. Hubbs, J. M. Scott, R. W. Scott*
Pfizer Chemical Research and Development, Groton, USA
Further Information
Publication History
Publication Date:
23 August 2006 (online)
Significance
Torcetrapib, the least euphonic drug candidate in living memory, is in clinical trials for the treatment of atherosclerosis because it inhibits cholesteryl ester transfer protein. The six-step synthesis from the commercial enantiopure amine B (37% overall) features a large-scale Pd-catalyzed Buchwald N-arylation as the key step.