Technology Process of (2S,4S)-N-((1R,2S)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide hydrochloride
There total 6 articles about (2S,4S)-N-((1R,2S)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide hydrochloride which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
(2S,4S)-tert-butyl-2-((1R,2S)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropylcarbamoyl)-4-phenylpyrrolidine-1-carboxylate;
With
trifluoroacetic acid;
In
dichloromethane;
at 20 ℃;
for 0.5h;
With
hydrogenchloride;
In
diethyl ether; dichloromethane;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: tert-butyl methyl ether; toluene / 20 °C / Heating / reflux
2.1: esperase 8.0L / water; dimethyl sulfoxide / 90 h / 40 °C / pH 8.5 / Heps*Na buffer; Enzymatic reaction; Resolution of racemate
3.1: 1,1'-carbonyldiimidazole / tetrahydrofuran / 0.83 h / Heating / reflux
3.2: 20 h / 20 °C
4.1: trifluoroacetic acid / dichloromethane / 1.5 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 14 h
6.1: trifluoroacetic acid / dichloromethane / 0.5 h / 20 °C
With
esperase 8.0L; N-ethyl-N,N-diisopropylamine; HATU; 1,1'-carbonyldiimidazole; trifluoroacetic acid;
In
tetrahydrofuran; dichloromethane; tert-butyl methyl ether; water; dimethyl sulfoxide; toluene;
- Guidance literature:
-
Multi-step reaction with 5 steps
1.1: esperase 8.0L / water; dimethyl sulfoxide / 90 h / 40 °C / pH 8.5 / Heps*Na buffer; Enzymatic reaction; Resolution of racemate
2.1: 1,1'-carbonyldiimidazole / tetrahydrofuran / 0.83 h / Heating / reflux
2.2: 20 h / 20 °C
3.1: trifluoroacetic acid / dichloromethane / 1.5 h / 20 °C
4.1: N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 14 h
5.1: trifluoroacetic acid / dichloromethane / 0.5 h / 20 °C
With
esperase 8.0L; N-ethyl-N,N-diisopropylamine; HATU; 1,1'-carbonyldiimidazole; trifluoroacetic acid;
In
tetrahydrofuran; dichloromethane; water; dimethyl sulfoxide;