Hydrochloric Acid → Saxagliptin hydrochloride

Participants

Reaction Steps

Saxagliptin monohydrate, form H-1 (2 g) was suspended in 15 ml of 1-butanol and a solution of 0.591 ml of conc. HCl in 15 ml of n-butylacetate (“BuOAc”) was added dropwise. The obtained suspension was analyzed by PXRD and polymorphically pure form Z was found to have been obtained. The suspension was stirred at room temperature for 30 min and then for additional 30 min in an ice bath. The suspension was then filtered, yielding 1.879 g of Saxagliptin HCl. PXRD is shown in FIG. 12.

Provenance & Evidence