4-Methylmorpholine → HCID 57382978, compound

Participants

Reaction Conditions

Reaction Steps

3-{[2-(1-pyrrolidinyl)ethyl]oxy}benzoic acid D38 (200 mg) and 2-chloro-4,6-dimethoxy-1,3,5-triazine (171 mg, 0.98 mmol) was dissolved under argon in MeCN (20 ml) and cooled down to 0° C. Then N-methylmorpholine (0.3 ml) was added and the mixture was stirred at 0° C. for 2 hours. To this mixture was added 1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinamine hydrochloride D11 (240 mg) in small portions, afterwards the reaction was then warmed up to room temperature. After stirring for 16 hours, the reaction was filtered and concentrated to give crude product. This product was purified by prep-HPLC (A 0.01% NH4HCO3/Water, B: ACN, 0˜8 min 25-50%, 50%˜60% 8-12 min, 60%˜95% 12-15 min, 95˜95% 15-18 min) to give 50 mg of white solid of desired product E43. LCMS [MH+] [email protected] min (5 min run)

Provenance & Evidence