Technology Process of 1-(7-cyclopropyl-2,7-diazaspiro[4.4]nonan-2-yl)-2-(2-(4-methoxy-2,6-dimethylphenylsulfonyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-1-yl)ethanone
There total 10 articles about 1-(7-cyclopropyl-2,7-diazaspiro[4.4]nonan-2-yl)-2-(2-(4-methoxy-2,6-dimethylphenylsulfonyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-1-yl)ethanone which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine;
In
dichloromethane;
at 0 - 20 ℃;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: 1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride / dichloromethane / 20 °C
2.1: polyphosphoric acid / 5 h / 90 °C
3.1: hydrogen / palladium on activated charcoal / ethanol / 20 °C / 1500.15 Torr
4.1: triethylamine / dichloromethane / 20 °C
5.1: water; sodium hydroxide / tetrahydrofuran; methanol / 3 h / 20 °C
5.2: 0 °C
6.1: 1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 20 °C
With
1-hydroxy-7-aza-benzotriazole; water; hydrogen; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; N-ethyl-N,N-diisopropylamine; sodium hydroxide;
palladium on activated charcoal;
In
tetrahydrofuran; methanol; ethanol; dichloromethane;
- Guidance literature:
-
Multi-step reaction with 3 steps
1: sodium cyanoborohydride; acetic acid / methanol / 4 h / Molecular sieve; Reflux
2: hydrogen / palladium 10% on activated carbon / ethanol / 20 °C / 2250.23 Torr / Inert atmosphere
3: 1-hydroxy-7-aza-benzotriazole; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 20 °C
With
1-hydroxy-7-aza-benzotriazole; hydrogen; sodium cyanoborohydride; acetic acid; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine;
palladium 10% on activated carbon;
In
methanol; ethanol; dichloromethane;