Réaction #166527

Équation de réaction

N-(3-ethyl-1-((6-(((2R,3S)-3-hydroxypyrrolidin-2-yl)methoxy)pyridin-2-yl)methyl)-1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide

HCHO

NaBH(OAc)3

→

final product

Rendement 77.7%

N-(3-ethyl-1-((6-(((2R,3S)-3-hydroxy-1-methylpyrrolidin-2-yl)methoxy)pyridin-2-yl)methyl)-1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide

Rendement 77.7%

Solvants

MeOH

Conditions de réaction

Traitement

1. 1
   Concentrationconcentrated under reduced pressure
2. 2
   Autrepurified by silica gel chromatography (DCM/MeOH/NH4OH 10:1:0.1)

Mode opératoire

To N-(3-ethyl-1-((6-(((2R,3S)-3-hydroxypyrrolidin-2-yl)methoxy)pyridin-2-yl)methyl)-1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide (5 mg, 0.0098 mmol; prepared as in Example 36) in MeOH (1 mL) was added HCHO as a 35% aqueous solution (16 mg, 0.20 mmol) and NaBH(OAc)3 (10 mg, 0.049 mmol). The reaction mixture was stirred for 30 minutes, concentrated under reduced pressure and purified by silica gel chromatography (DCM/MeOH/NH4OH 10:1:0.1) to provide the final product (4 mg). MS (ES+APCI) m/z=526 (M+H).

Source