N-(2-{(1S,2S)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl}ethyl)-1-(4-methoxybenzyl)-3-methyl-1H-indazol-5-amine → N-(2-{(1S,2S)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl}ethyl)-3-methyl-1H-indazol-5-amine

Participants

Reaction Conditions

Reaction Steps

N-(2-{(1S,2S)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl}ethyl)-1-(4-methoxybenzyl)-3-methyl-1H-indazol-5-amine (22 mg, 0.041 mmol) from step 3 of this example was dissolved in TFA (200 uL) and stirred at 75° C. for 4.5 hours. The volatiles were removed in vacuum. The residue was then dissolved in MeOH, and the volatiles removed in vacuum. The residue was then dissolved in DCM, and the volatiles removed in vacuum. The product was purified by chromatography on KPNH2™ SiO2 (Biotage) eluting with 5% acetone:DCM to give the titled compound. LRMS calc: 410.20; obs: 411.05 (M+1). Compounds reported in Table 8 are prepared by a general procedure analogous to that described in step 3, Example 48 above.

Provenance & Evidence