755037-03-7

  • Product Name:Regorafenib int
  • Molecular Formula:C21H15ClF4N4O3
  • Purity:99%
  • Molecular Weight:482.822
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Product Details

Reputable Manufacturer Supply High Purity 99% Regorafenib int  755037-03-7 with Low Price

  • Molecular Formula:C21H15ClF4N4O3
  • Molecular Weight:482.822
  • Melting Point:206.0 to 210.0 °C 
  • Boiling Point:513.4 °C at 760 mmHg 
  • PKA:12.04±0.70(Predicted) 
  • Flash Point:264.3 °C 
  • PSA:92.35000 
  • Density:1.491 g/cm3 
  • LogP:6.22570 

755037-03-7 Relevant articles

Synthesis method of regorafenib

-

Paragraph 0029-0031, (2021/04/21)

The invention provides a synthesis metho...

Interrupted aza-Wittig reactions using iminophosphoranes to synthesize 11C-carbonyls

Ismailani, Uzair S.,Munch, Maxime,Mair, Braeden A.,Rotstein, Benjamin H.

supporting information, p. 5266 - 5269 (2021/06/06)

A direct CO2-fixation methodology couple...

Preparation method of regorafenib

-

Paragraph 0025-0040, (2021/05/29)

The invention relates to a preparation m...

Regorafenib analogues and their ferrocenic counterparts: Synthesis and biological evaluation

Wilde, Myron,Arzur, Danielle,Baratte, Blandine,Lefebvre, Dorian,Robert, Thomas,Roisnel, Thierry,Le Jossic-Corcos, Catherine,Bach, Stéphane,Corcos, Laurent,Erb, William

supporting information, p. 19723 - 19733 (2020/12/04)

Approved by the FDA in 2012, regorafenib...

755037-03-7 Process route

4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide
757251-39-1

4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide

4-chloro-3-(trifluoromethyl)phenyl isocyanate
327-78-6

4-chloro-3-(trifluoromethyl)phenyl isocyanate

regorafenib
755037-03-7

regorafenib

Conditions
Conditions Yield
In ethyl acetate; at 20 ℃; for 1.5h;
94.5%
In dichloromethane; at 0 - 20 ℃; for 16h; Inert atmosphere;
90%
In dichloromethane; for 24h;
87%
In acetone; at 40 ℃; for 5h;
85%
In tetrahydrofuran; toluene; at 27 ℃; for 4.5h;
74.9%
In tetrahydrofuran; at 30 ℃; for 12h;
73.46%
In dichloromethane; at 0 - 25 ℃; for 3h;
67.2%
In toluene; at 20 ℃; for 72h;
47%
In toluene; at 20 ℃; for 72h;
47%
In toluene; at 20 ℃; for 72h;
47%
In toluene; at 20 ℃; for 72h;
47%
In toluene; at 20 ℃; for 72h;
47%
In ethyl acetate; at 20 - 45 ℃; for 1.5h;
 
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide; 4-chloro-3-(trifluoromethyl)phenyl isocyanate; In tetrahydrofuran; toluene; at 20 ℃; for 4.5h;
With acetyl chloride; In tetrahydrofuran; methanol; toluene; for 2.25h;
 
In dichloromethane; at 0 - 5 ℃; for 4h; Inert atmosphere;
350 g
In acetone; at 25 - 30 ℃;
5.5 g
In ethyl acetate; at 20 ℃; for 0.5h;
 
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide; 4-chloro-3-(trifluoromethyl)phenyl isocyanate; In tetrahydrofuran; at 25 ℃; for 4h; Inert atmosphere;
With hydrogenchloride; In water; at 25 ℃; for 4h;
 
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide; In dichloromethane; at 25 - 30 ℃; Inert atmosphere;
4-chloro-3-(trifluoromethyl)phenyl isocyanate; In dichloromethane; at 0 - 30 ℃;
 
In tetrahydrofuran; at 20 ℃; for 5h;
86.7 g
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide; 4-chloro-3-(trifluoromethyl)phenyl isocyanate; With acetic acid; In tetrahydrofuran; toluene; at 20 ℃; for 4.5h;
With acetyl chloride; In tetrahydrofuran; methanol; for 2.25h;
With water; sodium hydroxide; In acetone; at 40 ℃; for 0.5h;
31.5 g
In dichloromethane; ethyl acetate; at 20 ℃; for 18h; Inert atmosphere; Schlenk technique;
169 mg
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide
757251-39-1

4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide

Methyl 4-methyl-3-oxopentanoate
42558-54-3

Methyl 4-methyl-3-oxopentanoate

4-chloro-3-trifluoromethyl-aniline
320-51-4

4-chloro-3-trifluoromethyl-aniline

regorafenib
755037-03-7

regorafenib

Conditions
Conditions Yield
With dmap; In N,N-dimethyl-formamide; at 140 ℃; for 4h; Temperature; Green chemistry;
96.8%

755037-03-7 Upstream products

  • 757251-39-1
    757251-39-1

    4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide

  • 327-78-6
    327-78-6

    4-chloro-3-(trifluoromethyl)phenyl isocyanate

  • 399-95-1
    399-95-1

    4-amino-3-fluorophenol

  • 1338722-52-3
    1338722-52-3

    C12H16FNO

755037-03-7 Downstream products

  • 835621-08-4
    835621-08-4

    4-{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide mesylate

  • 835621-09-5
    835621-09-5

    4-{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide phenylsulfonate

  • 835621-07-3
    835621-07-3

    4-{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide hydrochloride

  • 1019206-88-2
    1019206-88-2

    4-[4({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide monohydrate

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