3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol

Base Information

Chemical Name:3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol
CAS No.:934660-98-7
Molecular Formula:C₁₈H₁₇F₃IN₃O₂
Molecular Weight:491.252
Hs Code.:

Synonyms:3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol

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Chemical Property of 3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol

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Technology Process of 3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol

There total 10 articles about 3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol 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:

: 934665-86-8
3-[(1R)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol hydrochloride

: 20445-33-4,39637-99-5
(R)-methoxytrifluoromethylphenylacetyl chloride

: 934660-98-7
3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol

: 934660-99-8
3-[(1R)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol

: 1035349-42-8
(2S)-N-{(1R)-1-[1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)-3-hydroxyazetidin-3-yl]ethyl}-3,3,3-trifluoro-2-(methyloxy)-2-phenylpropanamide

: C₂₈H₂₄F₆IN₃O₄

Guidance literature:: With N-ethyl-N,N-diisopropylamine; In dichloromethane; at 20 ℃; for 0.25h;

Reference yield:

: 1373446-70-8
1,1-dimethylethyl {(1S)-1-[1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)-3-hydroxyazetidin-3-yl]ethyl}carbamate

: 934660-98-7
3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol

Guidance literature:: With hydrogenchloride; In 1,4-dioxane; methanol; at 55 ℃; for 2h;
DOI:10.1021/ml300049d

Reference yield:

: 1373446-60-6
phenylmethyl 3-hydroxy-3-[(1R)-1-hydroxyethyl]azetidine-1-carboxylate

: 934660-98-7
3-[(1S)-1-aminoethyl]-1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol

Guidance literature:: Multi-step reaction with 7 steps

1.1: pyridine; thionyl chloride / dichloromethane / 1 h / 20 °C / Cooling with ice; Reflux

1.2: 2 h / 20 °C / Cooling with ice

2.1: sodium azide / diethyl ether; N,N-dimethyl-formamide / 1.5 h / 60 °C

2.2: 22 h / 20 °C

3.1: triphenylphosphine / tetrahydrofuran; water / 1 h / 70 °C

4.1: tetrahydrofuran / 2 h / 20 °C

5.1: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 760.05 Torr

6.1: N-ethyl-N,N-diisopropylamine / tetrahydrofuran / 20 °C

7.1: hydrogenchloride / 1,4-dioxane; methanol / 2 h / 55 °C

With pyridine; hydrogenchloride; thionyl chloride; sodium azide; palladium 10% on activated carbon; hydrogen; N-ethyl-N,N-diisopropylamine; triphenylphosphine; In tetrahydrofuran; 1,4-dioxane; methanol; diethyl ether; dichloromethane; water; N,N-dimethyl-formamide;
DOI:10.1021/ml300049d