Technology Process of D-glycero-Pentonic acid, 2,3-dideoxy-3-[[N-[2-(1,1-diMethylethyl)phenyl]-2-oxoglycyl-L-alanyl]aMino]-5-O-(2,3,5,6-tetrafluorophenyl)-, 1,1-diMethylethyl ester, (4ξ)- (9CI)
There total 9 articles about D-glycero-Pentonic acid, 2,3-dideoxy-3-[[N-[2-(1,1-diMethylethyl)phenyl]-2-oxoglycyl-L-alanyl]aMino]-5-O-(2,3,5,6-tetrafluorophenyl)-, 1,1-diMethylethyl ester, (4ξ)- (9CI) which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
(3S)-3-(alaninyl)amino-5-(2′,3′,5′,6′-tetrafluorophenoxy)-4-hydroxypentanoic acid tert-butyl ester;
With
benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride;
In
dichloromethane;
at 0 ℃;
for 0.166667h;
2-((2-(tert-butyl)phenyl)amino)-2-oxoacetic acid;
With
4-methyl-morpholine;
In
dichloromethane;
at 20 ℃;
for 16h;
DOI:10.1021/jm050307e
- Guidance literature:
-
Multi-step reaction with 4 steps
1.1: KF / dimethylformamide / 4 h / 20 °C
2.1: 0.142 g / NaBH4 / methanol; tetrahydrofuran / 1 h / 0 °C
3.1: H2 / Pd/C / methanol / 2 h / 760 Torr
4.1: hydroxybenzotriazole hydrate; 1-ethyl-3-(3',3'-dimethyl-1'-aminopropyl)carbodiimide*HCl / CH2Cl2 / 0.17 h / 0 °C
4.2: N-methylmorpholine / CH2Cl2 / 16 h / 20 °C
With
potassium fluoride; sodium tetrahydroborate; hydrogen; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride;
palladium on activated charcoal;
In
tetrahydrofuran; methanol; dichloromethane; N,N-dimethyl-formamide;
DOI:10.1021/jm050307e
- Guidance literature:
-
Multi-step reaction with 3 steps
1.1: 0.142 g / NaBH4 / methanol; tetrahydrofuran / 1 h / 0 °C
2.1: H2 / Pd/C / methanol / 2 h / 760 Torr
3.1: hydroxybenzotriazole hydrate; 1-ethyl-3-(3',3'-dimethyl-1'-aminopropyl)carbodiimide*HCl / CH2Cl2 / 0.17 h / 0 °C
3.2: N-methylmorpholine / CH2Cl2 / 16 h / 20 °C
With
sodium tetrahydroborate; hydrogen; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride;
palladium on activated charcoal;
In
tetrahydrofuran; methanol; dichloromethane;
DOI:10.1021/jm050307e
