(N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide

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Chemical Name:(N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide
CAS No.:1202759-10-1
Molecular Formula:C₂₄H₂₄F₂N₆O₃
Molecular Weight:482.49
Hs Code.:

Synonyms:(N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide

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Chemical Property of (N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide

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Technology Process of (N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide

There total 13 articles about (N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide 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:

: 40216-83-9
L-4-hydroxyproline methyl ester hydrochloride

: 1202759-10-1
(N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide

Guidance literature:: Multi-step reaction with 10 steps

1.1: triethylamine / dichloromethane / 5 h / 20 °C

2.1: 1H-imidazole / N,N-dimethyl-formamide / 16 h

3.1: lithium aluminium tetrahydride / tetrahydrofuran / 0.25 h / -20 °C

4.1: di-isopropyl azodicarboxylate; triethylamine; triphenylphosphine / tetrahydrofuran / 0 - 20 °C / Inert atmosphere

5.1: hydrogen / palladium on activated carbon / methanol / 16 h / 20 °C

6.1: caesium carbonate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl / palladium diacetate / toluene / 16 h / 110 °C / Inert atmosphere

7.1: hydrogen / palladium on activated carbon / methanol / 16 h / 20 °C

8.1: di-tert-butyl dicarbonate / 1-methyl-pyrrolidin-2-one / 1 h / 20 °C

8.2: 1.5 h / 0 °C

9.1: hydrogen fluoride / water / 0 - 20 °C

10.1: trifluoroacetic acid / dichloromethane / 0 - 20 °C

10.2: 0 °C

With 1H-imidazole; lithium aluminium tetrahydride; di-tert-butyl dicarbonate; di-isopropyl azodicarboxylate; hydrogen fluoride; hydrogen; caesium carbonate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; triethylamine; triphenylphosphine; trifluoroacetic acid; palladium on activated carbon; palladium diacetate; In tetrahydrofuran; 1-methyl-pyrrolidin-2-one; methanol; dichloromethane; water; N,N-dimethyl-formamide; toluene;

Reference yield:

: 1202760-81-3
C₂₉H₃₂F₂N₆O₅

: 1202759-10-1
(N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide

Guidance literature:: C₂₉H₃₂F₂N₆O₅; With trifluoroacetic acid; In dichloromethane; at 0 - 20 ℃;

With sodium hydrogencarbonate; In dichloromethane; at 0 ℃;

Reference yield:

: 403-19-0
2-fluoro-4-nitrophenol

: 1202759-10-1
(N-(3-(5-fluoro-2-(3-fluoro-4-((2S,4R)-4-hydroxypyrrolidin-2-yl)methoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide

Guidance literature:: Multi-step reaction with 7 steps

1.1: di-isopropyl azodicarboxylate; triethylamine; triphenylphosphine / tetrahydrofuran / 0 - 20 °C / Inert atmosphere

2.1: hydrogen / palladium on activated carbon / methanol / 16 h / 20 °C

3.1: caesium carbonate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl / palladium diacetate / toluene / 16 h / 110 °C / Inert atmosphere

4.1: hydrogen / palladium on activated carbon / methanol / 16 h / 20 °C

5.1: di-tert-butyl dicarbonate / 1-methyl-pyrrolidin-2-one / 1 h / 20 °C

5.2: 1.5 h / 0 °C

6.1: hydrogen fluoride / water / 0 - 20 °C

7.1: trifluoroacetic acid / dichloromethane / 0 - 20 °C

7.2: 0 °C

With di-tert-butyl dicarbonate; di-isopropyl azodicarboxylate; hydrogen fluoride; hydrogen; caesium carbonate; 2,2'-bis-(diphenylphosphino)-1,1'-binaphthyl; triethylamine; triphenylphosphine; trifluoroacetic acid; palladium on activated carbon; palladium diacetate; In tetrahydrofuran; 1-methyl-pyrrolidin-2-one; methanol; dichloromethane; water; toluene;