Technology Process of N1-(2-((4-fluoro-2-methylbenzyl)carbamoyl)-3-hydroxy-4-oxo-6,7,8,9-tetrahydro-7,10-ethanopyrimido[1,2-a]azepin-10(4H)-yl)-N2,N2-dimethyloxalamide
There total 9 articles about N1-(2-((4-fluoro-2-methylbenzyl)carbamoyl)-3-hydroxy-4-oxo-6,7,8,9-tetrahydro-7,10-ethanopyrimido[1,2-a]azepin-10(4H)-yl)-N2,N2-dimethyloxalamide which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
ethyl 10-(((benzyloxy)carbonyl)amino)-3-hydroxy-4-oxo-4,6,7,8,9,10-hexahydro-7,10-ethanopyrimido[1,2-a] azepine-2-carboxylate;
With
palladium 10% on activated carbon; hydrogen;
In
methanol;
for 18h;
N,N-dimethyloxamic acid;
With
dmap; N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate;
In
N,N-dimethyl-formamide;
at 20 ℃;
for 5h;
(4-fluoro-2-methylphenyl)methanamine;
With
triethylamine;
In
ethanol;
at 90 ℃;
DOI:10.1016/j.bmc.2020.115541
- Guidance literature:
-
Multi-step reaction with 7 steps
1.1: hydrogenchloride / water; tetrahydrofuran / 24 h / 20 °C
2.1: ammonium hydroxide / water; tetrahydrofuran / 72 h / 20 °C
2.2: 16 h / 0 - 20 °C
3.1: hydroxylamine / water; tetrahydrofuran / 5 h / Reflux
4.1: water / 24 h / 20 °C
5.1: 125 °C
6.1: potassium carbonate / N,N-dimethyl-formamide / 3 h / 90 °C
7.1: palladium 10% on activated carbon; hydrogen / methanol / 18 h
7.2: 5 h / 20 °C
7.3: 90 °C
With
hydrogenchloride; ammonium hydroxide; palladium 10% on activated carbon; hydrogen; hydroxylamine; potassium carbonate;
In
tetrahydrofuran; methanol; water; N,N-dimethyl-formamide;
DOI:10.1016/j.bmc.2020.115541