反应详情

To a mixture of 2-(1-(5-methyl-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)ethyl)-1-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-4-carboxylic acid (20 mg, 0.051 mmol, Intermediate-47, single enantiomer), ammonium chloride (8.1 mg, 0.15 mmol), and N,N-diisopropylethylamine in MeCN (2.0 mL) is added HBTU (23 mg, 0.061 mmol) at rt. The reaction mixture is stirred at rt for 1 hour. After removal of the solvent, the residue is filtered through a short column of NH-gel eluting with EtOAc and volatiles are removed. The residue is purified by preparative LC-MS to give 10.2 mg (50% yield) of the title compound.

1. customAfter removal of the solvent
2. filtrationthe residue is filtered through a short column of NH-gel
3. washeluting with EtOAc and volatiles
4. customare removed
5. customThe residue is purified by preparative LC-MS