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850140-72-6

Basic Information
CAS No.: 850140-72-6
Name: Afatinib
Molecular Structure:
Molecular Structure of 850140-72-6 (Afatinib)
Formula: C24H25ClFN5O3
Molecular Weight: 485.93800
Synonyms: BIBW 2992;
EINECS:
Density: 1.38g/cm3
Melting Point: 100 - 102 °C
Boiling Point: 676.917°C at 760 mmHg
Flash Point: 363.186°C
Solubility:
Appearance: Off-White Solid
Hazard Symbols:
Risk Codes:
Safety:
Transport Information:
PSA: 88.61000
LogP: 4.53590
Synthetic route

6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

(E)-4-(dimethylamino)-2-butenoic acid hydrochloride

850140-72-6

afatinib

Conditions
ConditionsYield
Stage #1: (E)-4-(dimethylamino)-2-butenoic acid hydrochloride With thionyl chloride In 1-methyl-pyrrolidin-2-one at -5 - 0℃; for 0.333333h;
Stage #2: 6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline In 1-methyl-pyrrolidin-2-one at -5 - 0℃; for 0.25h;
95%
With Bromoform; triethylamine; triphenylphosphine In dichloromethane at 25℃; for 1h; Reagent/catalyst; Temperature;93%
Stage #1: (E)-4-(dimethylamino)-2-butenoic acid hydrochloride With thionyl chloride In 1-methyl-pyrrolidin-2-one; ethyl acetate at 5℃;
Stage #2: 6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline In 1-methyl-pyrrolidin-2-one; ethyl acetate at 0℃; Temperature;
87.4%
Stage #1: (E)-4-(dimethylamino)-2-butenoic acid hydrochloride With thionyl chloride In N,N-dimethyl acetamide at -20 - -15℃;
Stage #2: 6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline In N,N-dimethyl acetamide; water at -25 - -20℃;
48 g
Stage #1: (E)-4-(dimethylamino)-2-butenoic acid hydrochloride With thionyl chloride In N,N-dimethyl acetamide at -20 - -10℃;
Stage #2: 6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline In N,N-dimethyl acetamide at -25 - -20℃; for 0.166667h;
Stage #3: In water Alkaline conditions;
1413945-87-5

dimethylaminoacetaldehyde-hydrogen sulphite adduct

850140-72-6

afatinib

Conditions
ConditionsYield
Stage #1: (S)-diethyl 2-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-ylamino)-2-oxoethylphosphonate With lithium chloride In ethanol at -5℃;
Stage #2: dimethylaminoacetaldehyde-hydrogen sulphite adduct With potassium hydroxide In ethanol; water for 1h;
91%

C36H36ClFN5O5P

850140-72-6

afatinib

Conditions
ConditionsYield
With sodium hydride In N,N-dimethyl-formamide at 20℃; for 1h; Temperature; Solvent;87.3%

6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

1056149-69-9

(2E)-(N,N-dimethylamino)-2-butenoyl chloride

850140-72-6

afatinib

Conditions
ConditionsYield
With piperidine In tetrahydrofuran at 5 - 40℃; for 9h; Temperature; Reagent/catalyst; Solvent;86.1%

6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

212776-19-7

(E)-4-(dimethylamino)-2-butenoic acid methyl ester

850140-72-6

afatinib

Conditions
ConditionsYield
Stage #1: 6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline With trimethylaluminum In hexane; dichloromethane at 20℃; for 2h;
Stage #2: (E)-4-(dimethylamino)-2-butenoic acid methyl ester In hexane; dichloromethane at 60℃; for 5h; Solvent;
98%

2-dimethylamino-1-hydroxyethanesulfonic acid sodium salt

C26H31ClFN4O6P

850140-72-6

afatinib

Conditions
ConditionsYield
Stage #1: C26H31ClFN4O6P With lithium chloride; potassium hydroxide In ethanol; water at -5 - 10℃; for 2h; Horner-Wadsworth-Emmons Olefination; Inert atmosphere;
Stage #2: 2-dimethylamino-1-hydroxyethanesulfonic acid sodium salt In ethanol; water at 0 - 18℃; for 7h; Solvent; Reagent/catalyst; Temperature;
91.7%

C20H18ClF2N5O

86087-23-2

(S)-3-hydroxytetyrahydrofurane

850140-72-6

afatinib

Conditions
ConditionsYield
With potassium tert-butylate In tert-butyl alcohol at 50℃; for 1h; Reagent/catalyst; Solvent;89%
3616-56-6

dimethylaminoacetaldehyde diethyl acetal

diethyl ((4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazoline-6-ylcarbamoyl)methyl)phosphonate

850140-72-6

afatinib

Conditions
ConditionsYield
Stage #1: dimethylaminoacetaldehyde diethyl acetal With hydrogenchloride In water at 30 - 35℃; for 8.3h; Large scale;
Stage #2: diethyl ((4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazoline-6-ylcarbamoyl)methyl)phosphonate With lithium chloride; potassium hydroxide In water at -7 - -5℃; for 2h; Large scale;
78%

6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

1055943-40-2

trans-4-dimethylamino crotonic acid chloride hydrochloride salt

850140-72-6

afatinib

Conditions
ConditionsYield
In tetrahydrofuran at 0 - 5℃;97.5%
In 1-methyl-pyrrolidin-2-one; water at -5 - 0℃; for 0.5 - 0.75h;87%
In 1-methyl-pyrrolidin-2-one at -5 - 0℃;14.1 g
618061-76-0

(S)-diethyl 2-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-ylamino)-2-oxoethylphosphonate

2-dimethylamino-1-hydroxyethanesulfonic acid sodium salt

850140-72-6

afatinib

Conditions
ConditionsYield
With lithium chloride; potassium hydroxide In ethanol; water at -10℃; for 2h;60%

(E)-4-(dimethylamino)but-3-enamide

C18H14ClFIN3O2

850140-72-6

afatinib

Conditions
ConditionsYield
With potassium phosphate; copper(l) iodide; (R,R)-N,N'-dimethyl-1,2-diaminocyclohexane In 1,4-dioxane at 110℃; for 48h; Ullmann-Goldberg Substitution; Inert atmosphere;56%
618061-76-0

(S)-diethyl 2-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-ylamino)-2-oxoethylphosphonate

3616-56-6

dimethylaminoacetaldehyde diethyl acetal

850140-72-6

afatinib

Conditions
ConditionsYield
Stage #1: dimethylaminoacetaldehyde diethyl acetal With hydrogenchloride In water at 20 - 30℃; Inert atmosphere;
Stage #2: (S)-diethyl 2-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-ylamino)-2-oxoethylphosphonate With lithium chloride; potassium hydroxide In tetrahydrofuran at -15 - 20℃; for 2.5h; Product distribution / selectivity; Inert atmosphere;
97.7%
Stage #1: dimethylaminoacetaldehyde diethyl acetal With hydrogenchloride In water at 30 - 35℃; for 8.33333h;
Stage #2: (S)-diethyl 2-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-ylamino)-2-oxoethylphosphonate With potassium hydroxide; lithium chloride In tetrahydrofuran; water at -7 - 30℃; for 2.16667h;
78%
Stage #1: dimethylaminoacetaldehyde diethyl acetal With hydrogenchloride In water at 30 - 35℃; for 8.33333h; Inert atmosphere; Large scale;
Stage #2: With potassium hydroxide In water at -5℃; Large scale;
Stage #3: (S)-diethyl 2-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-ylamino)-2-oxoethylphosphonate With lithium chloride In tetrahydrofuran at -7℃; for 1.16667h; Large scale;

C18H14BrClFN3O2

(E)-4-(dimethylamino)but-3-enamide

850140-72-6

afatinib

Conditions
ConditionsYield
With potassium phosphate; dicyclohexyl-(2′,4′,6′-triisopropyl-3,6-dimethoxy-[1,1′-biphenyl]-2-yl)phosphine; palladium diacetate In water; tert-butyl alcohol at 110℃; for 16h; Inert atmosphere; Sealed tube;4%

6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

(2E)-4-(dimethylamino)but-2-enoic acid hydrochloride

850140-72-6

afatinib

Conditions
ConditionsYield
Stage #1: (2E)-4-(dimethylamino)but-2-enoic acid hydrochloride With thionyl chloride In N,N-dimethyl acetamide at -20 - -15℃;
Stage #2: 6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline In N,N-dimethyl acetamide at -25 - -20℃;
48 g

4-[(3-chloro-4-fluorophenyl)amino]-6-amino-7-((S)-tetrahydrofuran-3-yloxy)quinazoline dihydrochloride

1056149-69-9

(2E)-(N,N-dimethylamino)-2-butenoyl chloride

850140-72-6

afatinib

Conditions
ConditionsYield
Stage #1: 4-[(3-chloro-4-fluorophenyl)amino]-6-amino-7-((S)-tetrahydrofuran-3-yloxy)quinazoline dihydrochloride With hydrogenchloride In ethyl acetate at 25 - 65℃; for 0.25h;
Stage #2: (2E)-(N,N-dimethylamino)-2-butenoyl chloride In 1-methyl-pyrrolidin-2-one at 55 - 60℃; for 3h; Temperature; Solvent;
35 g

4-[(3-chloro-4-fluorophenyl)amino]-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 5%-palladium/activated carbon; hydrogen / tetrahydrofuran / 8 h / 80 °C / 3000.3 Torr
2: piperidine / tetrahydrofuran / 9 h / 5 - 40 °C
View Scheme
Multi-step reaction with 3 steps
1.1: iron; acetic acid / ethyl acetate / 1 h / 70 °C
2.1: tetrahydrofuran / 40 °C
2.2: 2 h / 30 - 40 °C
3.1: lithium chloride; potassium hydroxide / water; ethanol / 2 h / -10 °C
View Scheme
Multi-step reaction with 2 steps
1.1: acetic acid; iron / tetrahydrofuran; water / 3 h / 25 - 30 °C
1.2: 1.5 h / 0 - 5 °C
2.1: hydrogenchloride / ethyl acetate / 0.25 h / 25 - 65 °C
2.2: 3 h / 55 - 60 °C
View Scheme

6-Amino-4-[(3-chloro-4-fluorophenyl)amino]-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: 1,1'-carbonyldiimidazole / dichloromethane / 30 - 55 °C
1.2: 3 h / 20 - 40 °C
2.1: lithium chloride; potassium hydroxide / ethanol; water / 2 h / -5 - 10 °C / Inert atmosphere
2.2: 7 h / 0 - 18 °C
View Scheme
Multi-step reaction with 2 steps
1.1: tetrahydrofuran / 40 °C
1.2: 2 h / 30 - 40 °C
2.1: lithium chloride; potassium hydroxide / water; ethanol / 2 h / -10 °C
View Scheme
Multi-step reaction with 4 steps
1.1: phosphorus trichloride / dichloromethane / 1.5 h / 0 - 20 °C
1.2: 1.5 h / 20 °C
2.1: n-butyllithium / tetrahydrofuran / 1 h / 0 - 20 °C
3.1: sodium tetrahydroborate / ethanol / 1 h / Reflux
4.1: sodium hydride / N,N-dimethyl-formamide / 1 h / 20 °C
View Scheme
162012-67-1

N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: potassium tert-butylate / N,N-dimethyl-d6-formamide / 1 h / 0 °C
1.2: 20 °C
2.1: iron; acetic acid / ethyl acetate / 1 h / 70 °C
3.1: tetrahydrofuran / 40 °C
3.2: 2 h / 30 - 40 °C
4.1: lithium chloride; potassium hydroxide / water; ethanol / 2 h / -10 °C
View Scheme
Multi-step reaction with 4 steps
1.1: iron(III) chloride / tert-butyl alcohol; acetone / 4 h / Inert atmosphere
2.1: 1,1'-carbonyldiimidazole / tetrahydrofuran / 1 h / 40 °C
2.2: 1 h
3.1: potassium hydroxide / tetrahydrofuran; water / 0 - 20 °C
4.1: potassium tert-butylate / tert-butyl alcohol / 1 h / 50 °C
View Scheme
Multi-step reaction with 3 steps
1.1: 1-methyl-pyrrolidin-2-one / 0.17 h / 25 - 30 °C / Inert atmosphere
1.2: 1.5 h / 15 - 20 °C
2.1: acetic acid; iron / tetrahydrofuran; water / 3 h / 25 - 30 °C
2.2: 1.5 h / 0 - 5 °C
3.1: hydrogenchloride / ethyl acetate / 0.25 h / 25 - 65 °C
3.2: 3 h / 55 - 60 °C
View Scheme
162012-69-3

7-fluoro-6-nitro-3H-quinazolin-4-one

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: sodium t-butanolate / acetonitrile / 2 h / 25 °C / Inert atmosphere
1.2: 18 h / 30 - 100 °C
2.1: phosphorus trichloride / acetonitrile / 10 h / 100 °C
3.1: tributyl-amine / propan-1-ol / 24 h / 60 °C
4.1: 5%-palladium/activated carbon; hydrogen / tetrahydrofuran / 8 h / 80 °C / 3000.3 Torr
5.1: piperidine / tetrahydrofuran / 9 h / 5 - 40 °C
View Scheme
Multi-step reaction with 4 steps
1.1: trichlorophosphate; triethylamine / acetonitrile / 5 h / 0 - 85 °C
1.2: 3 h / 25 - 30 °C
2.1: 1-methyl-pyrrolidin-2-one / 0.17 h / 25 - 30 °C / Inert atmosphere
2.2: 1.5 h / 15 - 20 °C
3.1: acetic acid; iron / tetrahydrofuran; water / 3 h / 25 - 30 °C
3.2: 1.5 h / 0 - 5 °C
4.1: hydrogenchloride / ethyl acetate / 0.25 h / 25 - 65 °C
4.2: 3 h / 55 - 60 °C
View Scheme
Multi-step reaction with 5 steps
1.1: trichlorophosphate; triethylamine / acetonitrile
2.1: potassium hydroxide / 1,4-dioxane
3.1: 1-methyl-pyrrolidin-2-one / 0.17 h / 25 - 30 °C / Inert atmosphere
3.2: 1.5 h / 15 - 20 °C
4.1: acetic acid; iron / tetrahydrofuran; water / 3 h / 25 - 30 °C
4.2: 1.5 h / 0 - 5 °C
5.1: hydrogenchloride / ethyl acetate / 0.25 h / 25 - 65 °C
5.2: 3 h / 55 - 60 °C
View Scheme
1421354-12-2

(E)-4-dimethylamino-but-2-enoic acid tert-butyl ester

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: hydrogenchloride / ethyl acetate / 10 - 25 °C / Inert atmosphere
2: thionyl chloride / 1-methyl-pyrrolidin-2-one / 0.42 - 0.5 h / -5 - 0 °C
3: water; 1-methyl-pyrrolidin-2-one / 0.5 - 0.75 h / -5 - 0 °C
View Scheme
Multi-step reaction with 3 steps
1: hydrogenchloride / water; ethyl acetate / 10 - 25 °C / Inert atmosphere
2: thionyl chloride / 1-methyl-pyrrolidin-2-one / -5 - 0 °C
3: 1-methyl-pyrrolidin-2-one / -5 - 0 °C
View Scheme
367-21-5

3-chloro-4-fluorophenylamine

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: 3.5 h / 80 °C
2.1: triphenylphosphine; iodine; triethanolamine / dichloromethane / 1 h / 20 °C
3.1: palladium diacetate; oxygen; caesium carbonate / toluene / 4.5 h / Reflux
4.1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 0.5 h / 10 - 20 °C
5.1: iron; hydrogenchloride; sodium hydroxide / water / 10.5 h / 40 - 80 °C / pH 8 - 9
6.1: trimethylaluminum / dichloromethane; hexane / 2 h / 20 °C
6.2: 5 h / 60 °C
View Scheme
Multi-step reaction with 4 steps
1.1: trichlorophosphate; triethylamine / acetonitrile / 5 h / 0 - 85 °C
1.2: 3 h / 25 - 30 °C
2.1: 1-methyl-pyrrolidin-2-one / 0.17 h / 25 - 30 °C / Inert atmosphere
2.2: 1.5 h / 15 - 20 °C
3.1: acetic acid; iron / tetrahydrofuran; water / 3 h / 25 - 30 °C
3.2: 1.5 h / 0 - 5 °C
4.1: hydrogenchloride / ethyl acetate / 0.25 h / 25 - 65 °C
4.2: 3 h / 55 - 60 °C
View Scheme
16499-57-3

7-fluoro-3H-quinazolin-4-one

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: sodium hydride / mineral oil / 0.33 h / 0 - 20 °C
1.2: 16 h / 130 °C
2.1: bromine / chloroform / 64 h / 0 - 20 °C / Inert atmosphere
3.1: thionyl chloride / N,N-dimethyl-formamide / 16 h / 90 °C
4.1: isopropyl alcohol / 3 h / 100 °C
5.1: dicyclohexyl-(2′,4′,6′-triisopropyl-3,6-dimethoxy-[1,1′-biphenyl]-2-yl)phosphine; potassium phosphate; palladium diacetate / water; tert-butyl alcohol / 16 h / 110 °C / Inert atmosphere; Sealed tube
View Scheme
Multi-step reaction with 5 steps
1.1: bromine / water / 5 h / 85 °C
2.1: sodium hydride / mineral oil / 0.33 h / 0 - 20 °C
2.2: 2 h / 130 °C
3.1: thionyl chloride / N,N-dimethyl-formamide / 16 h / 90 °C
4.1: isopropyl alcohol / 3 h / 100 °C
5.1: dicyclohexyl-(2′,4′,6′-triisopropyl-3,6-dimethoxy-[1,1′-biphenyl]-2-yl)phosphine; potassium phosphate; palladium diacetate / water; tert-butyl alcohol / 16 h / 110 °C / Inert atmosphere; Sealed tube
View Scheme
1621182-18-0

6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]-3,4-dihydroquinazoline-4-one

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: phosphorus trichloride / acetonitrile / 10 h / 100 °C
2: tributyl-amine / propan-1-ol / 24 h / 60 °C
3: 5%-palladium/activated carbon; hydrogen / tetrahydrofuran / 8 h / 80 °C / 3000.3 Torr
4: piperidine / tetrahydrofuran / 9 h / 5 - 40 °C
View Scheme

4-chloro-6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]quinazoline

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: tributyl-amine / propan-1-ol / 24 h / 60 °C
2: 5%-palladium/activated carbon; hydrogen / tetrahydrofuran / 8 h / 80 °C / 3000.3 Torr
3: piperidine / tetrahydrofuran / 9 h / 5 - 40 °C
View Scheme

2-chloro-1-fluoro-4-isocyanobenzene

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: palladium diacetate; oxygen; caesium carbonate / toluene / 4.5 h / Reflux
2.1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 0.5 h / 10 - 20 °C
3.1: iron; hydrogenchloride; sodium hydroxide / water / 10.5 h / 40 - 80 °C / pH 8 - 9
4.1: trimethylaluminum / dichloromethane; hexane / 2 h / 20 °C
4.2: 5 h / 60 °C
View Scheme

7-hydroxy-N-(3-chloro-4-fluorophenyl)-6-nitroquinazolin-4-amine

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 0.5 h / 10 - 20 °C
2.1: iron; hydrogenchloride; sodium hydroxide / water / 10.5 h / 40 - 80 °C / pH 8 - 9
3.1: trimethylaluminum / dichloromethane; hexane / 2 h / 20 °C
3.2: 5 h / 60 °C
View Scheme
27684-84-0

5-bromo-2-nitrophenol

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: tris-(dibenzylideneacetone)dipalladium(0); caesium carbonate; t-BuBrettPhos / methanol / 2 h / 85 °C
2.1: palladium diacetate; oxygen; caesium carbonate / toluene / 4.5 h / Reflux
3.1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 0.5 h / 10 - 20 °C
4.1: iron; hydrogenchloride; sodium hydroxide / water / 10.5 h / 40 - 80 °C / pH 8 - 9
5.1: trimethylaluminum / dichloromethane; hexane / 2 h / 20 °C
5.2: 5 h / 60 °C
View Scheme

C7H7N3O3

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: palladium diacetate; oxygen; caesium carbonate / toluene / 4.5 h / Reflux
2.1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 0.5 h / 10 - 20 °C
3.1: iron; hydrogenchloride; sodium hydroxide / water / 10.5 h / 40 - 80 °C / pH 8 - 9
4.1: trimethylaluminum / dichloromethane; hexane / 2 h / 20 °C
4.2: 5 h / 60 °C
View Scheme
770-22-9

N-(3-chloro-4-fluoro-phenyl)-formamide

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: triphenylphosphine; iodine; triethanolamine / dichloromethane / 1 h / 20 °C
2.1: palladium diacetate; oxygen; caesium carbonate / toluene / 4.5 h / Reflux
3.1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 0.5 h / 10 - 20 °C
4.1: iron; hydrogenchloride; sodium hydroxide / water / 10.5 h / 40 - 80 °C / pH 8 - 9
5.1: trimethylaluminum / dichloromethane; hexane / 2 h / 20 °C
5.2: 5 h / 60 °C
View Scheme

N-(3-chloro-4-fluorophenyl)-7-fluoro-6-amino-4-quinazolinamine

850140-72-6

afatinib

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: 1,1'-carbonyldiimidazole / tetrahydrofuran / 1 h / 40 °C
1.2: 1 h
2.1: potassium hydroxide / tetrahydrofuran; water / 0 - 20 °C
3.1: potassium tert-butylate / tert-butyl alcohol / 1 h / 50 °C
View Scheme
850140-72-6

afatinib

56-84-8

L-Aspartic acid

afatinib di-L-aspartate

Conditions
ConditionsYield
In tetrahydrofuran; water at 20 - 110℃;97%
850140-72-6

afatinib

110-16-7

maleic acid

2-butenamide, N-(4-((3-chloro-4-fluorophenyl)amino)-7-([(3S)-tetrahydro-3-furanyl]oxy)-6-quinazolinyl)-4-(dimethylamino)-, (2E)-, (2Z)-2-butenedioate

Conditions
ConditionsYield
In tetrahydrofuran at 20℃; Solvent; Temperature; Concentration;96.5%
In ethanol at 70℃;91.5%
In ethanol at 0 - 50℃; for 5.5h; Temperature; Large scale;91%
850140-72-6

afatinib

110-16-7

maleic acid

(2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4(dimethylamino)-2-butenamide dimaleate

Conditions
ConditionsYield
In ethanol at 70℃;94.1%
In ethanol at 0 - 70℃; for 5h; Solvent; Temperature; Large scale;91.5%
In ethyl acetate at 20 - 30℃; Solvent; Temperature;4 g
850140-72-6

afatinib

afatinib disulphate

Conditions
ConditionsYield
With sulfuric acid In ethyl acetate at 20℃; Product distribution / selectivity;94%
850140-72-6

afatinib

C22H20ClFN4O4

Conditions
ConditionsYield
With water; potassium hydroxide In ethanol at 50℃; for 24h; Solvent; Temperature; Reagent/catalyst;93.3%
850140-72-6

afatinib

afatinib diphosphate

Conditions
ConditionsYield
With phosphoric acid In ethyl acetate at 20℃; for 0.866667h; Product distribution / selectivity;93%
850140-72-6

afatinib

75-75-2

methanesulfonic acid

afatinib dimesylate

Conditions
ConditionsYield
In ethyl acetate at 20℃; for 0.7h; Product distribution / selectivity;92%
850140-72-6

afatinib

97-67-6

(S)-Malic acid

afatinib di-L-malate

Conditions
ConditionsYield
In ethyl acetate at 20℃; for 1.03333h;80.7%
850140-72-6

afatinib

124-40-3

dimethyl amine

C26H32ClFN6O3

Conditions
ConditionsYield
In water; N,N-dimethyl-formamide at 80℃; for 2h; Temperature; Solvent;80.6%
850140-72-6

afatinib

afatinib dihydrochloride

Conditions
ConditionsYield
With hydrogenchloride In isopropyl alcohol at 20℃; for 1.31667h;80%
850140-72-6

afatinib

144-62-7

oxalic acid

afatinib dioxalate

Conditions
ConditionsYield
In ethanol at 40℃; for 0.833333h; Reflux;78%
850140-72-6

afatinib

110-15-6

succinic acid

afatinib disuccinate

Conditions
ConditionsYield
In ethyl acetate at 20℃; for 6.5h;75.7%
850140-72-6

afatinib

110-17-8

(2E)-but-2-enedioic acid

1398312-22-5

afatinib fumarate

Conditions
ConditionsYield
In ethanol at 20 - 70℃; Product distribution / selectivity;67.7%
850140-72-6

afatinib

98-11-3

benzenesulfonic acid

afatinib dibenzenesulphonate

Conditions
ConditionsYield
In ethanol at 20 - 70℃;63.6%
850140-72-6

afatinib

77-92-9

citric acid

1398313-22-8

afatinib citrate

Conditions
ConditionsYield
In ethanol at 20℃; for 0.283333h;57%
850140-72-6

afatinib

C22H20ClFN4O4

Conditions
ConditionsYield
With sodium hydroxide In methanol; water at 50℃; for 24h; Reagent/catalyst; Temperature; Solvent;43%
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    Our advantages 1, Rich Experience in produce----We have 26 years experiences in chemical products and 6years experiences in Pharmaceutical Intermediate products and APIS. 2, Competitive price ---We have the competitive price owing to low

    Welcome to Hebei Bosang International Trade Co.,Ltd. Hebei Bosang International Trade Co.,Ltd. specializes in exporting high quality Pharmaceutical intermediates,Pharmaceutical

  •  Hebei Bosang International Trade Co.,Ltd.

     China (Mainland)  |  Contact Details

    Business Type:Trading Company

    Tel:18522547319

    Address:Wanda Plaza Commercial Complex, 123 Huaian East Road, Yuhua District, Shijiazhuang City, Hebei Province, China

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  • Afatinib manufacture

  • Casno:

    850140-72-6

    Afatinib manufacture

    Min.Order: 1 Gram

    FOB Price:  USD $ 0.0-0.0/Gram

    afatinib 1.Other name:Doxorubicin CAS:850140-72-6 Specification:EP/USP Stock:Fresh Package:25kg drum Application:850140-72-6

    Hangzhou Jinlan Pharm-Drugs Technology Co.,Ltd is located in Hangzhou, Zhejiang Province. Neighboring Ningbo port, Shanghai port, Hangzhou Xiaoshan Int’l Airport and Shanghai Pudon

  •  Hangzhou JINLAN Pharm-Drugs Technology Co., Ltd

     China (Mainland)  |  Contact Details

    Business Type:Other

    Tel:+86-571-85829053

    Address:Rm A606, Fuyi Center, jianqiao street, Jianggan Area

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  • Tovok,BIBW 2992

  • Casno:

    850140-72-6

    Tovok,BIBW 2992

    Min.Order: 100 Metric Ton

    FOB Price:  USD $ 0.0-0.0/Metric Ton

    Lorcaserin(856681-05-5)is an orally administered agent and a selective 5-HT2C receptor agonist for the treatment of obesity. It had been approved for marketing in US by FDA on 27 June in 2012. In clinical studies, lorcaserin h

    Triumph International Development Limilted is engaged in the API, pharmaceutical intermediates research and developmen.Adhering to the "customer first" business philosophy,we suppl

  •  Triumph International Development Limilted

    China (Mainland)  |  Contact Details

    Business Type:Lab/Research institutions

    Tel:+86-536-7971999

    Address:Yinhai Road,Shouguang

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  • Factory Supply Afatinib/GILOTRIF CAS 850140-72-6

  • Casno:

    850140-72-6

    Factory Supply Afatinib/GILOTRIF CAS 850140-72-6

    Min.Order: 1 Kilogram

    FOB Price:  USD $ 0.0-0.0/Kilogram

    Advantage 1. High quality with competitive price: We are manufacturer and we have 2 factories in China,we can provide excellent quality products with factory price. 2. Fast and safe delivery: 1) Parcels can be sent out within 3 days after payment

    Xi'an ZB Biotech Co., Ltd is specialized in researching, producing and selling herbal extract and API powder, which are mainly used in nutraceutical, cosmetic, beverage and food ad

  •  Xi'an ZB Biotech Co., Ltd.

    China (Mainland)  |  Contact Details

    Business Type:Trading Company

    Tel:+86-18591943808

    Address:Bldg. 3, East Of South Tangyan Road, High-Tech Zone, Xi'an, Shaanxi, China (Mainland)

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  • High Purity Good Quality Powder Afatinib

  • Casno:

    850140-72-6

    High Purity Good Quality Powder Afatinib

    Min.Order: 1 Gram

    FOB Price:  USD $ 10.0-20.0/Gram

    Strong backup of facotry: high R&D ability, favorable quality and competitive price 2. Stock avaliability 3. Flexible business way, like payment term and product delivery 4. Fast response 24*7 5. A good troubleshooter/very positive atti

    Beijing Yibai Biotechnology Co., Ltd, backed up with factory toppest support with high R&D ability, we have confidence to make you more competitive on market. Yibai is devoting fo

  •  Beijing Yibai Biotechnology Co., Ltd

    China (Mainland)  |  Contact Details

    Business Type:Trading Company

    Tel:86-010-60404860

    Address:Xuhui Plaza, Shunyi district, Beijing

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  • Hot sale high quality afatinib

  • Casno:

    850140-72-6

    Hot sale high quality afatinib

    Min.Order: 1 Kilogram

    FOB Price:  USD $ 199.0-200.0/Kilogram

    Our Advantages: 1.We have abundant professional production experience. 2.We have our own chemical factory. 3.Sample is free of charge. 4. Reasonable Price, Excellent Quality & Attentive Service 5. Prompt reply: we can reply you

    ShanLong Biotechnology Co., Ltd. is a high-tech enterprise specializing in high-tech and high value-added cosmetic raw materials, pharmaceutical intermediates, chemical customizati

  •  Shanlong Biotechnology (hebei) Co., Ltd.

     China (Mainland)  |  Contact Details

    Business Type:Trading Company

    Tel:0086-15530135359

    Address:QiaoXiQu

       Inquiry Now

  • Afatinib

  • Casno:

    850140-72-6

    Afatinib

    Min.Order: 100 Gram

    FOB Price:  USD $ 1.0-1.0/Gram

    We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research. We are committed to provide excellence in researching, manufacturing and drug discovery process. Our research

    ACHIEVER SYSTEAM BIOCHEM CO., LTD. is one of the professional suppliers in Chinese pharmaceutical market and is specialized in custom synthesis, chemical/pharmaceutical/ pesticides

  •  ACHIEVER SYSTEAM BIOCHEM CO., LTD.

     China (Mainland)  |  Contact Details

    Business Type:Lab/Research institutions

    Tel:86-021-58380978

    Address:Building 87,Lane 669, Dong Jing Road Shanghai,P.R.China

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