Technology Process of [15α-{4-[(3,4-dihydroxybenzyl)amino]-4-oxobutyl}-17-oxoestra-1(10),2,4-trien-3-yl]boronic acid
There total 4 articles about [15α-{4-[(3,4-dihydroxybenzyl)amino]-4-oxobutyl}-17-oxoestra-1(10),2,4-trien-3-yl]boronic acid which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
4-(15α-{3-[boronic acid]}estronyl)-butanoic acid;
With
benzotriazol-1-ol;
In
dichloromethane;
at 20 ℃;
3,4-dihydroxybenzylamine;
In
dichloromethane; acetonitrile;
at 20 ℃;
for 48h;
- Guidance literature:
-
Multi-step reaction with 4 steps
1.1: 2,6-dimethylpyridine / dichloromethane / 18 h / 0 - 20 °C
2.1: potassium acetate / Pd(dppf)Cl2*2DCM / 1,4-dioxane; dimethyl sulfoxide / 20 h / 100 °C
3.1: lithium hydroxide / tetrahydrofuran; water / 24 h / 20 °C / Alkaline aqueous solution
3.2: 1 h / 20 °C / Acidic aqueous solution
4.1: benzotriazol-1-ol / dichloromethane; acetonitrile / 24 h / 20 °C
4.2: 24 h / 20 °C
With
2,6-dimethylpyridine; lithium hydroxide; potassium acetate; benzotriazol-1-ol;
Pd(dppf)Cl2*2DCM;
In
tetrahydrofuran; 1,4-dioxane; dichloromethane; water; dimethyl sulfoxide; acetonitrile;
- Guidance literature:
-
Multi-step reaction with 3 steps
1.1: potassium acetate / Pd(dppf)Cl2*2DCM / 1,4-dioxane; dimethyl sulfoxide / 20 h / 100 °C
2.1: lithium hydroxide / tetrahydrofuran; water / 24 h / 20 °C / Alkaline aqueous solution
2.2: 1 h / 20 °C / Acidic aqueous solution
3.1: benzotriazol-1-ol / dichloromethane; acetonitrile / 24 h / 20 °C
3.2: 24 h / 20 °C
With
lithium hydroxide; potassium acetate; benzotriazol-1-ol;
Pd(dppf)Cl2*2DCM;
In
tetrahydrofuran; 1,4-dioxane; dichloromethane; water; dimethyl sulfoxide; acetonitrile;