Hydrochloric Acid → (RS)-S-[4-({5-bromo-4-[(1R,2R)-2-hydroxy-1-methylpropoxy]pyrimidin-2-yl}amino)-2-methoxyphenyl]-S-methyl Sulfoximide

Participants

Reaction Steps

220 mg (1.1 mmol) of (RS)-S-(4-amino-2-methoxyphenyl)-S-methyl sulfoximide and 280 mg (1.0 mmol) of (2R,3R)-3-[(5-bromo-2-chloropyrimidin-4-yl)oxy]-butan-2-ol in 10 ml of acetonitrile are mixed with 0.28 ml of a 4N solution of HCl in dioxane and stirred under reflux overnight. It is mixed with 1 ml of a solution of n-butanol/methanol (9:1) and stirred under reflux for another 5 days. The batch is concentrated by evaporation, and the residue is purified by chromatography (DCM/ethanol 8:2). 36 mg (0.1 mmol, corresponding to 8% of theory) of the product is obtained.

Provenance & Evidence