Technology Process of (R)-2-(3-(5-(5-(3,4-dimethylpiperazin-1-yl)pyridin-2-ylamino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-5-fluoro-2-(hydroxymethyl)-phenyl)-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1(2H)-one
There total 21 articles about (R)-2-(3-(5-(5-(3,4-dimethylpiperazin-1-yl)pyridin-2-ylamino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-5-fluoro-2-(hydroxymethyl)-phenyl)-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1(2H)-one which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
lithium hydroxide monohydrate; water;
In
tetrahydrofuran; isopropyl alcohol;
at 30 ℃;
for 2h;
- Guidance literature:
-
Multi-step reaction with 6 steps
1: sodium tetrahydroborate; ethanol / 4 h / 10 °C
2: triethylamine / dichloromethane / 16 h / 20 °C
3: tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; caesium carbonate / 1,4-dioxane / 16 h / 100 °C / Inert atmosphere
4: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 15 h / 100 °C / Inert atmosphere
5: sodium acetate; potassium phosphate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 2 h / 110 °C
6: water; lithium hydroxide monohydrate / isopropyl alcohol; tetrahydrofuran / 2 h / 30 °C
With
(1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium tetrahydroborate; potassium phosphate; tris-(dibenzylideneacetone)dipalladium(0); lithium hydroxide monohydrate; ethanol; water; potassium acetate; sodium acetate; caesium carbonate; triethylamine; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene;
In
tetrahydrofuran; 1,4-dioxane; dichloromethane; isopropyl alcohol;
- Guidance literature:
-
Multi-step reaction with 7 steps
1.1: isopropylmagnesium chloride / toluene; ethyl acetate / 2 h / -35 - -25 °C
1.2: 3 h / 10 - 20 °C
2.1: sodium tetrahydroborate; ethanol / 4 h / 10 °C
3.1: triethylamine / dichloromethane / 16 h / 20 °C
4.1: tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; caesium carbonate / 1,4-dioxane / 16 h / 100 °C / Inert atmosphere
5.1: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 15 h / 100 °C / Inert atmosphere
6.1: sodium acetate; potassium phosphate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 2 h / 110 °C
7.1: water; lithium hydroxide monohydrate / isopropyl alcohol; tetrahydrofuran / 2 h / 30 °C
With
(1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium tetrahydroborate; potassium phosphate; tris-(dibenzylideneacetone)dipalladium(0); lithium hydroxide monohydrate; ethanol; water; isopropylmagnesium chloride; potassium acetate; sodium acetate; caesium carbonate; triethylamine; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene;
In
tetrahydrofuran; 1,4-dioxane; dichloromethane; ethyl acetate; isopropyl alcohol; toluene;