483368-24-7Relevant academic research and scientific papers
Development of a practical large-scale synthesis of denagliptin tosylate
Patterson, Daniel E.,Powers, Jeremiah D.,Leblanc, Michael,Sharkey, Tyler,Boehler, Emily,Mam, Erwin,Osterhout, Martin H.
scheme or table, p. 900 - 906 (2010/04/22)
A large-scale synthesis of denagliptin tosylate has been developed. The efficiency of the synthesis has been improved from the initially scaled route by changing the order of steps (performing a dehydration at a late stage). The key step of the synthesis is a single-step peptide coupling/dehydration, mediated by n-propanephosphonic acid cyclic anhydride. The challenges of developing this synthesis into a robust and practical manufacturing route are described.
(2S,4S)-4-FLUORO-1-[4-FLUORO-BETA-(4-FLUOROPHENYL)-L-PHENYLALANYL]-2-PYRROLIDINECARBONITRILE P-TOLUENESULFONIC ACID SALT AND ANHYDROUS CRYSTALLINE FORMS THEREOF
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Page/Page column 17-18, (2008/06/13)
The present invention includes anhydrous crystalline forms of (2S,4S)-4-fluoro-1-[4-fluoro-β-(4-fluorophenyl)-L-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt.
