1-Hydroxybenzotriazole → HCID 69512524, compound

Participants

Reaction Steps

HATU (65 mg, 0.17 mmol) was added to a solution of {3′-[(cyclopropylamino)carbonyl}-6′-methyl-biphen-4-yl}carboxylic acid (50 mg, 0.17 mmol) in DMF (2 ml). After 5 minutes HOBT (23 mg, 0.17 mmol), 2-amino-N-methylacetamide (0.17 mmol) and DIPEA (0.087 ml, 0.51 mmol) were added and the reaction mixture stirred at room temperature under nitrogen for 18 hours. The DMF was removed in vacuo and the residue partitioned between DCM (5 ml) and aqueous sodium carbonate solution (1M, 5 ml). The organic phase was purified by SPE cartridge (Si, 5 g) eluting in turn with DCM, chloroform, ether, ethyl acetate, acetonitrile, acetone, ethanol, DCM:ethanol:ammonia (40:8:1, 20:8:1 and 10:8:1). The product fractions were concentrated in vacuo to give N3-cyclopropyl-N4′{[(methylamino)carbonyl]methyl}-6-methyl-1,1′-biphenyl-3,4′-dicarboxamide.

Provenance & Evidence