1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 118890590, compound

Participants

Reaction Steps

To a solution of N-(azepan-3-yl)-N-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine (200 mg, 0.5 mmol), in DMF (4 mL) was added EDCI (144 mg, 0.75 mmol), HOBt (101 mg, 0.75 mmol), 2-(3,5-dichlorophenylamino)acetic acid (109 mg, 0.5 mmol) and DIEA (129 mg, 1.0 mmol) at 0° C. The reaction mixture was stirred at rt overnight and diluted with EtOAc (100 mL) and washed with water (50 mL). The aqueous layer was extracted with the EtOAc (50 mL), the combined organic layer was dried over Na2SO4 and evaporated in vacuo to give a residue that was subjected to flash column chromatography using 0-4% MeOH in CH2Cl2 as an eluent to give (235 mg, 77%) of the titled compound. LC-MS: m/z [M+1]=601.

Provenance & Evidence