Diisopropylethylamine → HCID 117859714, compound

Participants

Reaction Steps

A mixture of 70 mg of 7-[(2,6-difluorobenzyl)oxy]-2,5-dimethylpyrazolo[1,5-a]pyridine-3-carboxylic acid (75% purity, 0.118 mmol) from Example 4A, 66 mg of HATU (0.174 mmol) and 0.083 ml (0.474 mmol) of N,N-diisopropylethylamine in 0.7 ml of DMF was stirred at RT for 10 min. This reaction mixture was added to a solution of 53 mg (0.236 mmol) of rac-4-(methylsulphanyl)butane-1,2-diamine dihydrochloride in 0.14 ml of DMF at 0° C. and the mixture was stirred for 60 min. The reaction mixture was admixed with water and acetonitrile and purified by means of preparative HPLC (RP18 column, eluent:acetonitrile/water gradient with addition of 0.05% formic acid). 40 mg of the target compound were obtained (54% of theory).

Provenance & Evidence