Patent ID: 8748631
Filing Date: 2014-06-10
Classification: C07C,C07D

Abstract:
1. A method for making saxagliptin hydrochloride monohydrate comprising: combining (S)-(+)-p-toluenesulfinamide Ti(OEt) wherein R is alkyl or aryl, treating the resulting compound with NaCN, KCN, trimethylsilyl cyanide (TMSCN) or Et treating the resulting compound with phthalic anhydride to obtain treating the resulting compound with acid to obtain treating the resulting compound with KMnO coupling the resulting compound with methanoproline nitrile using hydroxybenzotriazole (HOBT), 1-ethyl-3-[3-dimethylaminopropyl]carbodiimide hydrochloride (EDC HCl) or N,N-diisopropylethylamine (DIPEA) to obtain treating the resulting compound with methyl amine and hydrochloric acid.