反应详情

2-[2-(3-Trifluoromethyl-4,5,6,7-tetrahydroindazol-1-yl)-acetylamino]-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid (25 mg, 0.059 mmol) was dissolved in a solution of DCM (1 mL) and DMF (0.2 mL). O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (27 mg, 0.070 mmol) was added, followed by N-(2-aminoethyl)-N-methyl carbamic acid tert-butyl ester (12 mg, 0.070 mmol) and N,N-diisopropylethylamine (12.2 μL, 0.070 mmol). The resultant mixture was stirred at RT overnight. The solvent was removed under reduced pressure, and the residue obtained purified by preparative reverse phase HPLC. The resulting residue was dissolved in a solution of DCM (0.5 mL) and TFA (0.5 mL) and stirred at RT for 30 min, before concentration in vacuo. The residue obtained was purified by preparative reverse phase HPLC to yield the title compound as a TFA salt (15 mg, 0.025, 42%).

1. customThe solvent was removed under reduced pressure
2. customthe residue obtained
3. custompurified by preparative reverse phase HPLC
4. dissolutionThe resulting residue was dissolved in a solution of DCM (0.5 mL) and TFA (0.5 mL)
5. customThe residue obtained
6. customwas purified by preparative reverse phase HPLC