反应详情

Methyl 13-cyclohexyl-6-formyl-6,7-dihydro-5H-indolo[2,1-a][2]benzazepine-10-carboxylate was dissolved in MeOH (0.04 M), HOAc (5 eq.) and tert-butyl[(3-{methyl[2-(methylamino)ethyl]amino}propyl)sulfonyl]carbamate (2 eq. Example 15, steps 1-3) were added followed by Et3N (3 eq.) and the mixture was stirred for 5 min. NaCNBH3 (2 eq.) was added and the mixture was stirred for 18 h. All volatiles were evaporated and the residual material was dissolved in EtOAc. The solution was extracted with sat. aq. NaHCO3, water and brine. After drying over Na2SO4 all volatiles were evaporated in vacuo and the compound was used without purification in the next reaction. (ES) m/z 697 (M+H)+.

1. stirringthe mixture was stirred for 18 h
2. customAll volatiles were evaporated
3. dissolutionthe residual material was dissolved in EtOAc
4. extractionThe solution was extracted with sat. aq. NaHCO3, water and brine
5. dry with materialAfter drying over Na2SO4 all volatiles
6. customwere evaporated in vacuo
7. customthe compound was used without purification in the next reaction