Technology Process of (4S,7S,10aS)-methyl 4-((2R,5R)-2,5-dibenzyl-6-((S)-1-(3-methoxy-3-oxopropyl)-2-oxoazepan-3-ylamino)-6-oxohexanamido)-5-oxooctahydro-2H-pyrido[2,1-b][1,3]thiazepine-7-carboxylate
There total 7 articles about (4S,7S,10aS)-methyl 4-((2R,5R)-2,5-dibenzyl-6-((S)-1-(3-methoxy-3-oxopropyl)-2-oxoazepan-3-ylamino)-6-oxohexanamido)-5-oxooctahydro-2H-pyrido[2,1-b][1,3]thiazepine-7-carboxylate which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine;
In
N,N-dimethyl-formamide;
at 20 ℃;
- Guidance literature:
-
Multi-step reaction with 4 steps
1.1: sodium hydrogencarbonate / tetrahydrofuran / 18 h / 20 °C
2.1: lithium hexamethyldisilazane / tetrahydrofuran / 1 h / 20 °C
2.2: 0 - 20 °C
3.1: hydrogenchloride / 1,4-dioxane / 3 h / 20 °C
4.1: N-ethyl-N,N-diisopropylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
With
hydrogenchloride; sodium hydrogencarbonate; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine; lithium hexamethyldisilazane;
In
tetrahydrofuran; 1,4-dioxane; N,N-dimethyl-formamide;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: pivaloyl chloride; 4-methyl-morpholine / tetrahydrofuran / 0.5 h / 0 - 20 °C
1.2: 2.75 h / -78 - 20 °C
2.1: sodium hexamethyldisilazane / tetrahydrofuran / 0.33 h / -78 °C
2.2: 3 h / 20 °C
3.1: hydrogen / palladium 10% on activated carbon / methanol / 3 h
4.1: dihydrogen peroxide; lithium hydroxide monohydrate / water; tetrahydrofuran / 0.67 h / 0 °C
4.2: pH < 2
5.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane; N,N-dimethyl-formamide / 24 h / 20 °C
5.2: 3 h / 20 °C
6.1: N-ethyl-N,N-diisopropylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
With
4-methyl-morpholine; lithium hydroxide monohydrate; hydrogen; dihydrogen peroxide; sodium hexamethyldisilazane; pivaloyl chloride; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine;
palladium 10% on activated carbon;
In
tetrahydrofuran; methanol; dichloromethane; water; N,N-dimethyl-formamide;
