3-Methyl-2-ketopiperazine → 2-[1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5,5-dimethyl-4-(2-methyl-3-oxopiperazin-1-yl)-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one

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 550 mg (4.82 mmol) of 3-methylpiperazin-2-one was added. The mixture was heated in the microwave for 3 h at 150° C. and for 3 h at 220° C. After cooling, the reaction mixture was purified by preparative HPLC (eluent: acetonitrile/water, gradient 20:80→100:0). 61 mg (purity 100%, 50% of theor.) of the target compound was obtained.

Provenance & Evidence