Cesium carbonate → 6-[3-(2-Fluorobenzyl)-1H-pyrazolo[4,3-b]pyridin-1-yl]-1,3,5-triazine-2,4-diamine

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Reaction Steps

A solution of 100 mg (0.44 mmol) of 3-(2-fluorobenzyl)-1H-pyrazolo[4,3-b]pyridine from example 4A, 64 mg (0.44 mmol) of 6-chloro-1,3,5-triazine-2,4-diamine, 8.1 mg (0.009 mmol) of tris(di-benzylideneacetone)dipalladium, 13 mg (0.026 mmol) of dicyclohexyl(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphine (XPHOS) and 201 mg (0.62 mmol) of cesium carbonate in 3 ml of degassed toluene is heated at 90° C. for 20 h. It is then diluted with ethyl acetate and methanol, filtered and concentrated in vacuo. The residue is crystallized from methanol to result in 42 mg (28% of theory) of the title compound as pale yellow crystals.

Provenance & Evidence