Technology Process of methyl 3-[(2R,5R)-5-(5-fluoro-pyridin-2-yloxymethyl)-2-methyl-piperidine-1-carbonyl]-4-[1,2,3]triazol-2-yl-benzoate
There total 13 articles about methyl 3-[(2R,5R)-5-(5-fluoro-pyridin-2-yloxymethyl)-2-methyl-piperidine-1-carbonyl]-4-[1,2,3]triazol-2-yl-benzoate which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
triethylamine;
palladium diacetate; 1,3-bis-(diphenylphosphino)propane;
In
dimethyl sulfoxide;
at 80 ℃;
- Guidance literature:
-
Multi-step reaction with 6 steps
1: triethylamine / dichloromethane / 22 °C
2: ethanol; hexane / Resolution of racemate
3: PS-triphenylphosphine; di-isopropyl azodicarboxylate / dichloromethane
4: hydrogen / 10 % Pd(OH)2/C / ethanol / 0.67 h / 22 °C / 760.05 Torr
5: 1-hydroxy-7-aza-benzotriazole; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; triethylamine / N,N-dimethyl-formamide / 4 h / 50 °C
6: triethylamine / palladium diacetate; 1,3-bis-(diphenylphosphino)propane / dimethyl sulfoxide / 80 °C
With
1-hydroxy-7-aza-benzotriazole; PS-triphenylphosphine; di-isopropyl azodicarboxylate; hydrogen; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; triethylamine;
palladium diacetate; 10 % Pd(OH)2/C; 1,3-bis-(diphenylphosphino)propane;
In
ethanol; hexane; dichloromethane; dimethyl sulfoxide; N,N-dimethyl-formamide;
- Guidance literature:
-
Multi-step reaction with 7 steps
1: tetrahydrofuran / 1 h
2: triethylamine / dichloromethane / 3 h
3: pyridine / dichloromethane / 19 h / 0 - 20 °C
4: 1-methyl-pyrrolidin-2-one; caesium carbonate / 26 h / 60 °C
5: trifluoroacetic acid / dichloromethane / 3.5 h / -2 - 20 °C / Cooling with iso-propanol/ice bath
6: 1-hydroxy-7-aza-benzotriazole; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; triethylamine / N,N-dimethyl-formamide / 4 h / 50 °C
7: triethylamine / palladium diacetate; 1,3-bis-(diphenylphosphino)propane / dimethyl sulfoxide / 80 °C
With
pyridine; 1-methyl-pyrrolidin-2-one; 1-hydroxy-7-aza-benzotriazole; caesium carbonate; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; triethylamine; trifluoroacetic acid;
palladium diacetate; 1,3-bis-(diphenylphosphino)propane;
In
tetrahydrofuran; dichloromethane; dimethyl sulfoxide; N,N-dimethyl-formamide;
