Diisopropylethylamine → HCID 46190327, compound

Participants

Reaction Steps

61 mg 1-methyl-piperidine-4-carboxylic acid are dissolved in 1 ml N,N-dimethylformamide and combined with 137 mg O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium-tetrafluoroborate (TBTU) and 138 μl N,N-diisopropyl-ethylamine (DIEA). The mixture is stirred for 20 minutes, then 150 mg 1-methyl-7-piperazin-1-ylmethyl-1H-indole-2-carboxylic acid(5-tert-butyl-3-methanesulphonylamino-2-methoxy-phenyl)-amide are added and the mixture is stirred for 12 hours. Then it is divided between water and ethyl acetate and the aqueous phase is extracted twice with ethyl acetate. The combined organic phases are washed with saturated aqueous sodium chloride solution and dried on magnesium sulphate. Then the solvents are eliminated in vacuo and the residue is chromatographed on silica gel with dichloromethane/(methanol/ammonia 9:1) 99:1 to 90:10.

Provenance & Evidence