Technology Process of (2R,4R)-4-[(5-acetyl-2H-pyrazole-3-carbonyl)amino]-5-biphenyl-4-yl-2-hydroxypentanoic acid trifluoroacetate
There total 9 articles about (2R,4R)-4-[(5-acetyl-2H-pyrazole-3-carbonyl)amino]-5-biphenyl-4-yl-2-hydroxypentanoic acid trifluoroacetate which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
(2R,4R)-4-[(5-acetyl-2H-pyrazole-3-carbonyl)amino]-5-biphenyl-4-yl-2-hydroxypentanoic acid ethyl ester trifluoroacetate;
With
water; sodium hydroxide;
In
ethanol;
for 1h;
With
acetic acid;
In
ethanol;
trifluoroacetic acid;
- Guidance literature:
-
Multi-step reaction with 8 steps
1.1: acetic acid / dichloromethane / 0.5 h / -5 °C / Inert atmosphere
1.2: 3 h / -5 °C
2.1: toluene / 3 h / Inert atmosphere; Reflux
3.1: hydrogenchloride / ethyl acetate / 3 h / 20 °C
4.1: n-butyllithium / tetrahydrofuran; hexanes / 0.5 h / -78 °C
4.2: 1 h / -78 °C
5.1: sodium hexamethyldisilazane / tetrahydrofuran / 0.33 h / -78 °C / Inert atmosphere
5.2: 0.5 h
6.1: hydrogenchloride / water / 20 h / 90 - 95 °C
7.1: N-ethyl-N,N-diisopropylamine; HATU / N,N-dimethyl-formamide / 1 h
8.1: sodium hydroxide; water / ethanol / 1 h
With
hydrogenchloride; n-butyllithium; water; sodium hexamethyldisilazane; acetic acid; N-ethyl-N,N-diisopropylamine; HATU; sodium hydroxide;
In
tetrahydrofuran; hexanes; ethanol; dichloromethane; water; ethyl acetate; N,N-dimethyl-formamide; toluene;
- Guidance literature:
-
Multi-step reaction with 9 steps
1.1: dmap; dicyclohexyl-carbodiimide / dichloromethane / -5 °C / Inert atmosphere
2.1: acetic acid / dichloromethane / 0.5 h / -5 °C / Inert atmosphere
2.2: 3 h / -5 °C
3.1: toluene / 3 h / Inert atmosphere; Reflux
4.1: lithium hexamethyldisilazane / tetrahydrofuran / 3.25 h / -65 °C / Inert atmosphere
4.2: 2 h / -35 °C
5.1: dmap; triethylamine / dichloromethane / 0.5 h / 0 °C / Inert atmosphere
5.2: 2.25 h / 0 °C
6.1: potassium carbonate / 20 h / 20 °C / Inert atmosphere
7.1: acetyl chloride / ethanol / 3 h / 25 °C
8.1: N-ethyl-N,N-diisopropylamine; HATU / N,N-dimethyl-formamide / 1 h
9.1: sodium hydroxide; water / ethanol / 1 h
With
dmap; water; potassium carbonate; acetic acid; triethylamine; N-ethyl-N,N-diisopropylamine; acetyl chloride; dicyclohexyl-carbodiimide; HATU; sodium hydroxide; lithium hexamethyldisilazane;
In
tetrahydrofuran; ethanol; dichloromethane; N,N-dimethyl-formamide; toluene;