Multi-step reaction with 8 steps
1: 92.2 percent / N-methylmorpholine, 1-hydroxybenzotriazole (HOBt), dicyclohexylcarbodiimide (DCC) / CH2Cl2 / 22 h / 0 - 20 °C
2: 4 N HCl / dioxane / 1 h / Ambient temperature
3: N-methylmorpholine, 1-hydroxybenzotriazole (HOBt), dicyclohexylcarbodiimide (DCC) / CH2Cl2 / 22 h / 0 - 20 °C
4: 4 N HCl / dioxane / 1 h / Ambient temperature
5: N-methylmorpholine, 1-hydroxybenzotriazole (HOBt), dicyclohexylcarbodiimide (DCC) / CH2Cl2 / 22 h / 0 - 20 °C
6: 4 N HCl / dioxane / 1 h / Ambient temperature
7: N-methylmorpholine, 1-hydroxybenzotriazole (HOBt), dicyclohexylcarbodiimide (DCC) / CH2Cl2 / 22 h / 0 - 20 °C
8: 92 percent / H2 / 10percent Pd/C / 2-methyl-propan-2-ol / 7 h
With
4-methyl-morpholine; hydrogenchloride; hydrogen; benzotriazol-1-ol; dicyclohexyl-carbodiimide;
palladium on activated charcoal;
In
1,4-dioxane; dichloromethane; tert-butyl alcohol;
DOI:10.1021/jm00138a013