1,4-Dioxane hydrochloride → 3-(5-(Azetidin-3-yloxy)pyridin-2-ylamino)-5-bromo-1-methylpyridin-2(1H)-one Hydrochloride

https://huagongshe.com/reaction/1021939

Participants

Role	Name	HCID	Charge
Reactant	1,4-Dioxane hydrochloride	HCID 20443148	—
Reactant	tert-Butyl 3-(6-(5-Bromo-1-methyl-2-oxo-1,2-dihydropyridin-3-ylamino)pyridin-3-yloxy)azetidine-1-carboxylate	HCID 58043697	—
Solvent	Methanol	HCID 887	—
Product	3-(5-(Azetidin-3-yloxy)pyridin-2-ylamino)-5-bromo-1-methylpyridin-2(1H)-one Hydrochloride	HCID 86661248	100%

Reaction Conditions

Temperature	80 °C

Reaction Steps

A mixture of 206d (1.46 g, 3.2 mmol) and HCl/1,4-dioxane (3.2 mL, 4M, 12.8 mmol) in methanol (20 mL) was heated at 80° C. for 1 h. The mixture was then concentrated under reduced pressure to afford 206e (1.24 g, 99%). MS-ESI: [M+H]+ 351.

Provenance & Evidence

DOI	10.6084/m9.figshare.5104873.v1
Patent number	US08716274B2
Source dataset	uspto-grants-2014_05
ORD ID	ord-0bf62ef4404f463c8373e15e5f11d165
Source note	uspto-grants-2014_05