2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide

Base Information

Chemical Name:2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide
CAS No.:1026929-28-1
Molecular Formula:C₁₉H₁₈F₃N₅O₂
Molecular Weight:405.379
Hs Code.:

Synonyms:2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide

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Chemical Property of 2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide

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Technology Process of 2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide

There total 3 articles about 2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield:

: 446-32-2
4-fluoroanthranilic acid

: 127000-91-3
(2R,3R)-3-Amino-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol

: 1026929-28-1
2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide

Guidance literature:: With benzotriazol-1-ol; triethylamine; dicyclohexyl-carbodiimide; In N,N-dimethyl-formamide; for 18h; Ambient temperature;
DOI:10.1021/jm9707277

Reference yield:

: 126917-48-4
(2R,3R)-3-Azido-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol

: 1026929-28-1
2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide

Guidance literature:: Multi-step reaction with 2 steps

1: palladium on activated charcoal; hydrogen / methanol / 4 h / 20 °C

2: N-ethyl-N,N-diisopropylamine; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate / N,N-dimethyl-formamide / 2 h / 20 °C

With palladium on activated charcoal; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; hydrogen; N-ethyl-N,N-diisopropylamine; In methanol; N,N-dimethyl-formamide;
DOI:10.1016/j.bmcl.2020.126951

Reference yield:

: 132507-89-2,132507-94-9,135270-05-2,135270-11-0,135272-36-5,133775-25-4
(2R,3R)-2-(2,4-Difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2,3-butanediol

: 1026929-28-1
2-Amino-N-[(1R,2R)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl]-4-fluoro-benzamide

Guidance literature:: Multi-step reaction with 4 steps

1.1: triethylamine; methanesulfonyl chloride / dichloromethane / 0.5 h / 0 °C

1.2: 2 h / 0 °C

2.1: sodium azide; ammonium chloride / N,N-dimethyl-formamide / 8 h / 100 °C

3.1: palladium on activated charcoal; hydrogen / methanol / 4 h / 20 °C

4.1: N-ethyl-N,N-diisopropylamine; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate / N,N-dimethyl-formamide / 2 h / 20 °C

With sodium azide; palladium on activated charcoal; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; hydrogen; ammonium chloride; methanesulfonyl chloride; triethylamine; N-ethyl-N,N-diisopropylamine; In methanol; dichloromethane; N,N-dimethyl-formamide;
DOI:10.1016/j.bmcl.2020.126951