Benzenesulfonic acid, 4-methyl-, compd. with pyridine (1:1) → HCID 59023735, compound

Participants

Reaction Conditions

Reaction Steps

PPTS (0.019 g, 0.075 mmol) was added to a mixture of 4-{7-[(E)-4-(tetrahydro-pyran-2-yloxy)-but-1-enyl]-1H-indazol-5-ylamino}-pyrimidine-2-amine (prepared from Example #N.2.7 reacted with trans-2-[3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)allyoxy]-tetrahydropyran using general procedure F, 0.037 g, 0.100 mmol) in MeOH (3.0 mL). The reaction mixture was stirred at about 25° C. for about 5 hours. The reaction mixture was diluted with EtOAc (5 mL) and was washed with aqueous Na2CO3 solution (5 mL). The organic portion was evaporated under reduced pressure to afford (E)-4-[5-(2-amino-pyrimidin-4-ylamino)-1H-indazol-7-yl]-but-3-en-1-ol (0.015 g, 0.051 mmol) as an off white solid; RP-HPLC (Table 1, Method e) Rt 0.62 min; m/z: (M+H)+ 297.0.

Provenance & Evidence