p-Toluenesulfonic acid → (S)-1-cyclopropyl-3-(4-(4-(3-methylmorpholino)-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-2-yl)phenyl)urea

Participants

Reaction Conditions

Reaction Steps

To a stirred solution of (S)-tert-butyl 2-(4-(3-cyclopropylureido)phenyl)-4-(3-methylmorpholino)-5H-pyrrolo[3,4-d]pyrimidine-6(7H)-carboxylate (0.99 g, 1.99 mmol) in DCM (5 mL) was added TFA (2.5 mL) and stirred at room temperature (20° C.) overnight. The reaction mixture was diluted with methanol and adsorbed onto a mp-TsOH cartridge (2.5 g, 3 mmol/g). The cartridge was rinsed with MeOH (3 column volumes) and the product was eluted with 7M NH3 in MeOH. The basic fractions were concentrated in vacuo to leave a pale orange solid (0.46 g, 1.16 mmol, 58% yield).

Provenance & Evidence