Multi-step reaction with 6 steps
1: O-benzotriazol-1-yl-N,N,N',N'-tetramethyluronium hexafluorophosphate (HBTU), N-methylmorpholine (NMM) / tetrahydrofuran / 6 h / Ambient temperature
2: trifluoroacetic acid (TFA) / CH2Cl2 / 2 h / Ambient temperature
3: 1.)2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT), N-methylmorpholine (NMM), 2.) N-methylmorpholine (NMM) / 1.) CH2Cl2, 0 deg C, 3 h, 2.) CH2Cl2, RT, 12 h
4: trifluoroacetic acid (TFA) / CH2Cl2 / 2 h / Ambient temperature
5: NaHCO3 / CH2Cl2; H2O
6: aq. Na2CO3 / CH2Cl2 / 2 h
With
4-methyl-morpholine; 2-chloro-4,6-dimethoxy-1 ,3,5-triazine; sodium hydrogencarbonate; sodium carbonate; O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; trifluoroacetic acid;
In
tetrahydrofuran; dichloromethane; water;
DOI:10.1021/jm00101a017