Hydrochloric Acid → HCID 68813499, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-chloro-2-[2-(3-cyclopropylisoxazol-5-yl]pyrrolidin-1-yl]-6-methoxymethylpyrimidine (Method 19) (250 mg, 0.746 mmol), 3-amino-5-methyl-1H-pyrazole (109 mg, 1.2 mmol) and hydrogen chloride (0.56 ml of a 4M solution in dioxane, 2.24 mmol) in NMP (5 ml) was heated at 120° C. for 18 hours. The mixture was allowed to cool then directly applied to an isolute SCX2 ion exchange column. The column was eluted with DCM/methanol (4:1) to remove neutrals and then with 7M methanolic ammonia to elute the product. The partially purified product was then purified by chromatography on silica gel eluting with DCM/methanol (100:0 increasing in polarity to 95:5). The product was triturated with diethyl ether/DCM and the solid product collected by filtration to give the title compound (100 mg, 34%) as a white solid.

Provenance & Evidence