反应详情

Under an Ar atmosphere, a catalytic amount of a Raney Ni solution in water was added to a solution of (R)—N2-(2-(2,4-dimethoxybenzylamino)-4-fluorophenyl)-N4-(8-fluorochroman-4-yl)-5-nitropyrimidine-2,4-diamine (21 mg) in THF. The flask was closed with a septum, evacuated under house vacuum and hydrogen added via balloon. The resulting suspension was stirred at RT for 2 hr, when the H2 balloon was removed, the mixture evacuated and filtered through a plug of celite, that was thoroughly rinsed with THF and MeOH, to yield (R)—N2-(2-(2,4-dimethoxybenzylamino)-4-fluorophenyl)-N4-(8-fluorochroman-4-yl)pyrimidine-2,4,5-triamine that was used directly.

1. customThe flask was closed with a septum
2. customevacuated under house vacuum and hydrogen
3. additionadded via balloon
4. customwhen the H2 balloon was removed
5. customthe mixture evacuated
6. filtrationfiltered through a plug of celite, that
7. washwas thoroughly rinsed with THF and MeOH