3,3-Difluoropiperidine hydrochloride (CAS number 496807-97-7) is a hydrochloride salt of piperidine with two fluoride substituents at 3-position. As a piperidine derivative, 3,3-difluoropiperidine hydrochloride is a ubiquitous building block in pharmaceutical active ingredients (APIs). 3,3-Difluoropiperidine hydrochloride can attach to molecular scaffolds effortlessly through amination. This fluorinated piperidine building block improves the potency of an agonist of apelin receptor with effective concentration EC50 from 162 nM to 6.5 nM. The presence of 3,3-difluoropiperidine has an enhanced selectivity of estrogen positive breast cancer (1600 folds selectivity).
Molecular functionalization with 3,3-difluoropiperidine hydrochloride is also used as a 19F NMR probe without requiring deuterated solvents or internal standards.