Multi-step reaction with 8 steps
1: dicyclohexylcarbodiimide / from 0 deg C to r.t.
2: 65 percent / N-methyl-morpholine / Ambient temperature
3: 1.) dicyclohexylcarbodiimide; 2.) N-hydroxysuccinimide 3.) N-methyl-morpholine / 1.) DMF; 2.) 30 min at 0 deg C; 3.) r.t.
4: 84 percent / H2O2, NaOH / dimethylformamide; H2O / 0.33 h / pH:10.5
5: 1.) N-hydroxybenzotriazole, dicyclohexylcarbodiimide 2.) N-methylmorpholine / 1.) 0 deg C, DMF, 30 min.; 2.) room temp.
6: 64 percent / H2 / 5percent Pd/C / dimethylformamide / 8 h
7: 33 percent / N-methyl-morpholine, N-hydroxybenzotriazole / dimethylformamide / from 0 deg C to r.t.
8: 81 percent / dimethyl sulphide, NaOH, H2O2 / dimethylformamide; H2O / 2 h / pH: 10.5
With
4-methyl-morpholine; sodium hydroxide; 1-hydroxy-pyrrolidine-2,5-dione; dimethylsulfide; hydrogen; dihydrogen peroxide; benzotriazol-1-ol; dicyclohexyl-carbodiimide;
palladium on activated charcoal;
In
water; N,N-dimethyl-formamide;
DOI:10.1016/S0040-4020(01)97641-0