Diisopropylethylamine → 2-[1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5,5-dimethyl-4-[2-(trifluoromethyl)morpholin-4-yl]-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one

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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 put in 4 ml of absolute NMP, and 924 mg (4.82 mmol) of 2-(trifluoromethyl)morpholine and 623 mg (4.82 mmol) of N,N-diisopropyl ethylamine were added. The mixture was heated in the microwave at 150° C. for 5 h. The reaction solution was filtered and purified by preparative HPLC (eluent: acetonitrile/water with 0.1% formic acid, gradient 20:80→100:0). 60 mg (46% of theor.) of the target compound was obtained.

Provenance & Evidence