Thiomorpholine 1,1-dioxide → HCID 71285780, compound

Participants

Reaction Conditions

Reaction Steps

Under argon atmosphere, 200 mg (purity 62%, 0.24 mmol) of 2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-iodo-5,5-dimethyl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one (example 15A) was suspended in 4 ml of absolute 1-methyl-2-pyrrolidone and 652 mg (4.82 mmol) of thiomorpholine-1,1-dioxide was added. The mixture was heated in the microwave for 3 h at 150° C. and 1 h at 200° C. After cooling, the reaction mixture was purified by preparative HPLC (eluent: acetonitrile/water with 0.1% formic acid, gradient 20:80→100:0). 72 mg (57% of theor.) of the target compound was obtained.

Provenance & Evidence