反应详情

温度

0 °C

120 mg (0.29 mmol) of trans-3-{4-[methyl-(4-trifluoromethyl-benzenesulfonyl)-amino]-cyclohexyloxy}-propionic acid in 3 mL of CH2Cl2 were treated with 0.057 mL (0.44 mmol, 1.5 eq) of N,N,N′-trimethylethylenediamine and 0.48 mL (0.36 mmol, 1.5 eq) of NMM. The solution was cooled to 0° C. and 73.0 mg (0.38 mmol, 1.3 eq) of EDCI and 9 mg (0.06 mmol, 0.2 eq) of HOBT were added. The mixture was stirred at RT for 2 days, partitioned between CH2Cl2 and a saturated aqueous solution of NaHCO3. The organic phase was washed with brine, dried over Na2SO4 and evaporated. Column chromatography with CH2Cl2:MeOH 9:1 gave 118 mg (82%) of trans-N-(2-dimethylamino-ethyl)-N-methyl-3-{4-[methyl-(4-trifluoromethyl-benzenesulfonyl)-amino]-cyclohexyloxy}-propionamide as colorless oil, MS: 494 (MH+).

1. custompartitioned between CH2Cl2
2. washThe organic phase was washed with brine
3. dry with materialdried over Na2SO4
4. customevaporated