Triethylamine → HCID 57635048, compound

Participants

Reaction Steps

A mixture of 0.047 g (0.0001 mole) of (rac)-4-[9-cyclopentyl-7-(2-hydroxy-ethyl)-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino]-3-methoxy-benzoic acid (I-49a), 0.043 g (0.00011 mole) of 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium-3-oxide hexafluorophosphate, 0.027 g (0.000023 mole) of 4-amino-1-methylpiperidine, 0.05 mL of triethylamine and 2 mL of dichloromethane was stirred at room temperature for 1.5 hours and then concentrated under reduced pressure. The residue purified by C18 reverse phase silica gel chromatography, eluting with an acetonitrile-water gradient (10:90-100:0) to give 0.0182 g of (rac)-4-[9-cyclopentyl-7-(2-hydroxy-ethyl)-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino]-3-methoxy-N-(1-methyl-piperidin-4-yl)-benzamide (I-49)

Provenance & Evidence