1,4-Dioxane hydrochloride → 3-(1-(2,3-difluoro-4-methoxyphenyl)-1H-tetrazol-5-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine, dihydrochloride salt

Participants

Role	Name	HCID	Charge
Reactant	1,4-Dioxane hydrochloride	HCID 20443148	—
Reactant	tert-butyl 4-(4-(6-amino-5-(1-(2,3-difluoro-4-methoxyphenyl)-1H-tetrazol-5-yl)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate	HCID 58293836	—
Product	3-(1-(2,3-difluoro-4-methoxyphenyl)-1H-tetrazol-5-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine, dihydrochloride salt	HCID 131730701	98.2%

Reaction Steps

Compound 1103 (3.0 g, 5.419 mmol) was treated with 4 M HCl/dioxane (50 mL, 200.0 mmol) for 1 hour at RT. The solvents were removed by vacuum evaporation to give 3-(1-(2,3-difluoro-4-methoxyphenyl)-1H-tetrazol-5-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine, dihydrochloride salt (Compound 12, 2.8 g, 98%) as a slightly yellow solid.

Provenance & Evidence

DOI	10.6084/m9.figshare.5104873.v1
Patent number	US08481524B2
Source dataset	uspto-grants-2013_07
ORD ID	ord-594ae4dbf4264d50b9f94e6c1b85cd12
Source note	uspto-grants-2013_07