Multi-step reaction with 8 steps
1: 59 percent / triethylamine / methanol / 2 h / Heating
2: 97 percent / m-chloroperoxybenzoic acid / CH2Cl2 / 1 h
3: HCl / ethanol / Ambient temperature
4: 1-hydroxybenzotriazole monohydrate (HOBt), N-methylmorpholine, 1-<3-(dimethylamino)propyl>-3-ethylcarbodiimide hydrochloride / dimethylformamide / -23 - 20 °C
5: HCl / ethanol / Ambient temperature
6: 1-hydroxybenzotriazole monohydrate (HOBt), N-methylmorpholine, 1-<3-(dimethylamino)propyl>-3-ethylcarbodiimide hydrochloride / dimethylformamide / -23 - 20 °C
7: HCl / ethanol / Ambient temperature
8: N-hydroxysuccinimide, N-methylmorpholine / dimethylformamide / 1.) 0 deg C, 2 h, 2.) RT, overnight
With
4-methyl-morpholine; hydrogenchloride; 1-hydroxy-pyrrolidine-2,5-dione; 1-hydroxybenzotriazol-hydrate; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; 3-chloro-benzenecarboperoxoic acid;
In
methanol; ethanol; dichloromethane; N,N-dimethyl-formamide;
DOI:10.1021/jm00394a035