Technology Process of (1aRS,7bSR)-5-[2-((R)-1-ethylpyrrolidin-3-ylmethyl)-4-fluombenzenesulfonyl-amino]-1,1a,2,7b-tetrahydrocyclopropa[c]chromene-4-catboxylic acid
There total 28 articles about (1aRS,7bSR)-5-[2-((R)-1-ethylpyrrolidin-3-ylmethyl)-4-fluombenzenesulfonyl-amino]-1,1a,2,7b-tetrahydrocyclopropa[c]chromene-4-catboxylic acid which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
methyl (1aS,7bR)-5-[2-((R)-1-ethylpyrrolidin-3-ylmethyl)-4-fluoro-benzenesulfonylamino]-1,1a,2,7b-tetrahydrocyclopropa[c]chromene-4-carboxylate;
With
water; lithium hydroxide;
In
1,4-dioxane;
at 85 ℃;
With
formic acid;
In
methanol;
With
citric acid;
In
1,4-dioxane; water;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: (1R,2R)-trans-2-aminocyclohexanol hydrochloride; sodium hexamethyldisilazane / nickel(I) iodide / isopropyl alcohol / 0.08 h / 40 °C / Sealed tube; Inert atmosphere
1.2: 70 °C
2.1: trifluoroacetic acid / dichloromethane / 1 h / 20 °C
3.1: potassium carbonate / acetonitrile / 2.5 h / 20 °C
4.1: chlorosulfonic acid / 1,2-dichloro-ethane / 2 h / 20 °C
5.1: dichloromethane; pyridine / 20 °C
6.1: water; lithium hydroxide / 1,4-dioxane / 85 °C
With
chlorosulfonic acid; water; sodium hexamethyldisilazane; potassium carbonate; (1R,2R)-trans-2-aminocyclohexanol hydrochloride; trifluoroacetic acid; lithium hydroxide;
nickel(I) iodide;
In
1,4-dioxane; pyridine; dichloromethane; 1,2-dichloro-ethane; isopropyl alcohol; acetonitrile;
- Guidance literature:
-
Multi-step reaction with 7 steps
1.1: 1H-imidazole; triphenylphosphine; iodine / 1,4-dioxane; diethyl ether / 20 °C / Cooling with ice
1.2: 20 °C
2.1: (1R,2R)-trans-2-aminocyclohexanol hydrochloride; sodium hexamethyldisilazane / nickel(I) iodide / isopropyl alcohol / 0.08 h / 40 °C / Sealed tube; Inert atmosphere
2.2: 70 °C
3.1: trifluoroacetic acid / dichloromethane / 1 h / 20 °C
4.1: potassium carbonate / acetonitrile / 2.5 h / 20 °C
5.1: chlorosulfonic acid / 1,2-dichloro-ethane / 2 h / 20 °C
6.1: dichloromethane; pyridine / 20 °C
7.1: water; lithium hydroxide / 1,4-dioxane / 85 °C
With
1H-imidazole; chlorosulfonic acid; water; iodine; sodium hexamethyldisilazane; potassium carbonate; triphenylphosphine; (1R,2R)-trans-2-aminocyclohexanol hydrochloride; trifluoroacetic acid; lithium hydroxide;
nickel(I) iodide;
In
1,4-dioxane; pyridine; diethyl ether; dichloromethane; 1,2-dichloro-ethane; isopropyl alcohol; acetonitrile;