Dimethylformamide → N-(1-isobutoxyethoxy) 2-[5-(naphthalene-2-sulfonyl)-hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]-pyrimidine-5-carboxamide

Participants

Reaction Steps

To a solution of 2-[5-(naphthalene-2-sulfonyl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-pyrimidine-5-carboxylic acid (0.266 g, 0.71 mmol) in DMF (2 ml) was added EDCl (0.204 g, 1.06 mmol), HOBt (0.171 g, 1.1 mmol), intermediate D (1 ml, 7 mmol) and DIPEA (2 ml, 11 mmol). The reaction was stirred for 24 h, then loaded directly onto a silica gel column. The product was eluted with 2% MeOH/DCM to 5% MeOH/DCM to yield the title compound (0.255 g, 66%). This was carried onto the next step without characterisation.

Provenance & Evidence