Technology Process of PL-225B
There total 10 articles about PL-225B which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
(S)-ethyl 7-amino-5-chloro-3-(2-(phenoxymethyl)morpholinosulfonyl)-1H-indole-2-carboxylate; N-ethoxycarbonyl-4-piperidone;
In
dichloromethane;
at 20 ℃;
for 20h;
With
trifluoroacetic acid;
In
dichloromethane;
for 0.166667h;
With
sodium tris(acetoxy)borohydride;
In
dichloromethane;
for 1.5h;
- Guidance literature:
-
Multi-step reaction with 7 steps
1.1: potassium hydroxide / ethanol; water / 0 - 10 °C / Industry scale
1.2: 0.5 h / -5 - 0 °C
2.1: Polyphosphoric acid (PPA) / 110 °C
3.1: acetic anhydride; sulfuric acid / 0 - 20 °C
3.2: 0 - 20 °C
4.1: oxalyl dichloride / N,N-dimethyl-formamide / dichloromethane / 12 h / 10 °C
5.1: triethylamine / dichloromethane / 4 h
6.1: ammonium chloride; iron / ethanol / 80 - 85 °C
7.1: dichloromethane / 20 h / 20 °C
7.2: 0.17 h
7.3: 1.5 h
With
oxalyl dichloride; sulfuric acid; acetic anhydride; iron; ammonium chloride; triethylamine; potassium hydroxide;
N,N-dimethyl-formamide;
In
ethanol; dichloromethane; water;
- Guidance literature:
-
Multi-step reaction with 5 steps
1.1: sodium hydroxide / water / 0.17 h / 10 - 20 °C
1.2: 15 h / 45 - 50 °C
2.1: ammonium formate / palladium 10% on activated carbon / 1 h / 20 °C / Reflux; Cooling with dry ice
3.1: triethylamine / dichloromethane / 4 h
4.1: ammonium chloride; iron / ethanol / 80 - 85 °C
5.1: dichloromethane / 20 h / 20 °C
5.2: 0.17 h
5.3: 1.5 h
With
ammonium formate; iron; ammonium chloride; triethylamine; sodium hydroxide;
palladium 10% on activated carbon;
In
ethanol; dichloromethane; water;
