New Synthetic Route to a Dipeptidyl Peptidase-4 Inhibitor
Autor: | Stephane Caron, Danny Lafrance |
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Rok vydání: | 2012 |
Předmět: | |
Zdroj: | Organic Process Research & Development. 16:409-414 |
ISSN: | 1520-586X 1083-6160 |
Popis: | A new synthetic route to a dipeptidyl peptidase-4 (DPP4) inhibitor was developed and demonstrated on a multigram scale. This approach takes advantage of the cheap and readily available Boc-trans-4-hydroxy-l-proline methyl ester as starting material which was derivatized through an SN2 reaction. Several leaving groups were studied, and the nosylate group showed superiority over other derivatives. Formation of an amide using the most costly starting material, 3,3-difluoropyrrolidine, was performed late in the synthesis to minimize its economical impact on the overall cost of the API. |
Databáze: | OpenAIRE |
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