(Rs)-s-(4-amino-2-bromphenyl)-n-(ethoxycarbonyl)-s-methylsulfoximide → (Rs)-s-{2-bromo-4-[(4-{[(r)-1-(hydroxymethyl)propyl]amino}-5-(3-thienyl)pyrimidine-2-yl)amino]phenyl}-n-(ethoxycarbonyl)-s-methylsulfoximide

Participants

Reaction Steps

In the reaction of (R)-2-(2-chloro-5-thiophen-3-yl-pyrimidine-4-ylamino)-butan-1-ol (426 mg, 1.5 mmol) with (RS)—S-(4-amino-2-bromphenyl)-N-(ethoxycarbonyl)-S-methylsulfoximide (404 mg, 1.3 mmol) according to procedure 5b, the desired product is obtained in 30% yield (214 mg) after chromatographic purification (silica gel, dichloromethane/ethanol (0%-15% ethanol)).

Provenance & Evidence