1-Methylpyrrolidine → 1-{6-[(2-{[7-(2,4-Dichlorophenyl)imidazo[1,2-c]pyrimidin-5-yl]amino}ethyl)amino]pyridin-3-yl}ethanone

Participants

Role	Name	HCID	Charge
Reactant	1-Methylpyrrolidine	HCID 8454	—
Reactant	Diisopropylethylamine	HCID 81531	—
Reactant	1-(6-Chloropyridin-3-yl)ethan-1-one	HCID 2779698	—
Reactant	N-[7-(2,4-Dichlorophenyl)imidazo[1,2-c]pyrimidin-5-yl]ethane-1,2-diamine trifluoroacetate	HCID 68710578	—
Product	1-{6-[(2-{[7-(2,4-Dichlorophenyl)imidazo[1,2-c]pyrimidin-5-yl]amino}ethyl)amino]pyridin-3-yl}ethanone	HCID 59313028	—

Reaction Conditions

Temperature	130 °C

Reaction Steps

50 mg (0.155 mmol) of the amine (Example 8A) are introduced into 3 ml of dry N-methylpyrrolidine, 48.3 mg (0.31 mmol) of 1-(6-chloropyridin-3-yl)ethanone and 40.1 mg (0.31 mmol) of DIPEA are added, and the mixture is heated in a microwave at 130° C. for 1.5 h. Purification by preparative HPLC results in 11 mg (15% of theory) of the product as a solid.

Provenance & Evidence

DOI	10.6084/m9.figshare.5104873.v1
Patent number	US08273752B2
Source dataset	uspto-grants-2012_09
ORD ID	ord-f4b20586e2e74ba2aab9f931cb7e9b5b
Source note	uspto-grants-2012_09