反应详情

To 2-(1H-benzo[d]imidazol-5-yl)-5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridine (100 mg, 0.271 mmol) was added acetonitrile (2.7 mL) before 7-methyl-1,5,7-triazabicyclo(4.4.0)dec-5-ene (1.949 μL, 0.014 mmol) and ethyl acrylate (36.2 μL, 0.326 mmol) were added and stirred at ambient temperature for 2 h to give a 2:1 mixture of regioisomers. Ethyl 3-(5-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)-1H-benzo[d]imidazol-1-yl)propanoate was obtained after regioisomer separation via SFC (Column: ChiralPak AD-H; Mobile Phase: 50:50 liquid CO2/isopropanol with 0.2% isopropylamine). MS (ESI) m/z: Calculated: 468.2; Observed: 469.2 (M++H).

1. additionwere added
2. customto give
3. additiona 2:1 mixture of regioisomers