反应详情

温度

75 °C

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.

1. customThe volatiles were removed in vacuum
2. dissolutionThe residue was then dissolved in MeOH
3. customthe volatiles removed in vacuum
4. dissolutionThe residue was then dissolved in DCM
5. customthe volatiles removed in vacuum
6. customThe product was purified by chromatography on KPNH2™ SiO2 (Biotage)
7. washeluting with 5% acetone