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231277-92-2 Usage

Uses

An antineoplastic agent used in breast cancer research

Mechanisms of Action

Lapatinib is a tyrosine kinase inhibitor which can effectively inhibit the tyrosine kinase activity of human epidermal growth factor receptors 1 and 2 (ErbB1, ErbB2). It can uniquely act in a variety of ways, ensuring that breast cancer cells cannot receive growth signals. It inhibits intracellular EGFR (ErbB-1) and HER2 (ErbB-2) ATP sites, preventing tumor cell phosphorylation and activation, blocking down-regulation signals through the homogeneity and heterogeneity of EGFR (ErbB-1) and HER2 (ErbB-1) dimerization.

Indications and Usage

Lapatinib is a drug targeting breast cancer developed by British GlaxoSmithKline Co.
Human ErbB receptors belong to the type I tyrosine kinase (TK) receptor family, including ErbB1 (EGFR), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4). The ErbB-1 (EGFR) and ErbB-2 (HER-2) receptors are often overexpressed or otherwise altered in cancer patients. Human epidermal growth factor receptor 2 (ErbB-2, HER-2) is known to be a human oncogene closely related with breast cancer. Its high expression in breast cancer often predicts lymph node metastasis and poor tumor differentiation, with poor prognosis. HER-2 is one of the target molecules for breast cancer-specific therapy. Lapatinib can act simultaneously on both Her-1 Her-2. The biological effects of this method inhibiting the proliferation and growth of tumor cells are much larger than only acting on one target. The combination of Lapatinib with Capecitabine is used to treat patients with advanced or metastatic breast cancer with overexpression of human epidermal receptor2, already treated with anthracyclines, paclitaxel, and trastuzumab. Clinical trials have shown that Lapatinib also effectively treats HER2-type cancer patients with Herceptin resistance.

Uses

antineoplastic, tyrosine kinase inhibitor

Uses

Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.

Uses

Lapatinib Ditosylate (GW572016, GW2016, Tykerb, Tyverb) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.
InChI:InChI=1/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35)

231277-92-2SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 18, 2017

Revision Date: Aug 18, 2017

1.Identification

1.1 GHS Product identifier

Product name lapatinib

1.2 Other means of identification

Product number -
Other names Tykerb

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:231277-92-2 SDS

231277-92-2Synthetic route

2-(methylsulfonyl)ethylamine hydrochloride
104458-24-4

2-(methylsulfonyl)ethylamine hydrochloride

5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
231278-84-5

5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20℃; for 0.333333h;
Stage #2: 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With acetic acid In tetrahydrofuran at 40℃; for 2h;
Stage #3: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 25 - 40℃; for 3h; Concentration;
100%
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With N-ethyl-N,N-diisopropylamine In isopropyl alcohol at 50 - 60℃; for 4h;
Stage #2: With sodium cyanoborohydride In isopropyl alcohol at 20℃; for 2h;
92.6%
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With sodium sulfate; triethylamine In methanol at 0℃; for 0.333333h;
Stage #2: 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With formic acid; sodium cyanoborohydride In tetrahydrofuran; methanol; N,N-dimethyl-formamide for 2h; pH=5 - 6;
82%
C27H19ClFN3O3

C27H19ClFN3O3

2-(methylsulfonyl)ethylamine hydrochloride
104458-24-4

2-(methylsulfonyl)ethylamine hydrochloride

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
With triethylamine In dichloromethane at 25 - 30℃; Inert atmosphere;97%
lapatinib ditosylate
388082-78-8

lapatinib ditosylate

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: lapatinib ditosylate In ethyl acetate at 20℃; for 1h;
Stage #2: With sodium carbonate In water; ethyl acetate for 1h;
96.2%
With sodium carbonate In water; acetonitrile at 5 - 40℃; for 3.58333h;91%
With sodium carbonate In water; ethyl acetate at 22 - 70℃; for 3.25h;56%
formaldehyd
50-00-0

formaldehyd

6-(furan-2-yl)-4-[3-chloro-4-(3-fluorobenzyloxy)phenyl]aminoquinazoline

6-(furan-2-yl)-4-[3-chloro-4-(3-fluorobenzyloxy)phenyl]aminoquinazoline

2-(methylsulfonyl)ethylamine hydrochloride
104458-24-4

2-(methylsulfonyl)ethylamine hydrochloride

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
In tetrahydrofuran at 35 - 40℃; for 4h;90.3%
C11H18BNO5S

C11H18BNO5S

N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine
231278-20-9

N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium dihydrogenphosphate In N,N-dimethyl-formamide at 80℃; for 5h; Temperature; Solvent; Reagent/catalyst; Inert atmosphere;89.8%
2-Methanesulfonyl-ethylamine
49773-20-8

2-Methanesulfonyl-ethylamine

5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
231278-84-5

5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: 2-Methanesulfonyl-ethylamine; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde In methanol; dichloromethane at 20℃;
Stage #2: With hydrogen In methanol; dichloromethane Inert atmosphere;
85%
Stage #1: 2-Methanesulfonyl-ethylamine; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With sodium tris(acetoxy)borohydride; N-ethyl-N,N-diisopropylamine
Stage #2: With toluene-4-sulfonic acid
80%
Stage #1: 2-Methanesulfonyl-ethylamine; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With triethylamine In tetrahydrofuran; methanol for 3h;
Stage #2: With methanol; sodium tetrahydroborate In tetrahydrofuran at 20℃; Cooling with ice;
70%
C18H22N4O3S

C18H22N4O3S

3-chloro-4-(3-fluorobenzyloxy)aniline
202197-26-0

3-chloro-4-(3-fluorobenzyloxy)aniline

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
With acetic acid for 1h; Reflux; Industrial scale;84.2%
N(1)-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-N,N-dimethylformamidine
1227853-05-5

N(1)-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-N,N-dimethylformamidine

2-amino-5-[5-[[[2-(methanesulfonyl)ethyl]amino]methyl]furan-2-yl]benzonitrile

2-amino-5-[5-[[[2-(methanesulfonyl)ethyl]amino]methyl]furan-2-yl]benzonitrile

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
With acetic acid for 1h; Reflux; Industrial scale;82.4%
NEU-0000388

NEU-0000388

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
With 20% palladium hydroxide-activated charcoal; hydrogen In methanol at 20℃; under 2585.81 - 2844.39 Torr;81.67%
N-((5-bromofuran-2-yl)methyl)-2-(methylsulfonyl)ethanamine
845658-68-6

N-((5-bromofuran-2-yl)methyl)-2-(methylsulfonyl)ethanamine

N-[3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-bromo-quinazolin-4-amine
944549-41-1

N-[3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-bromo-quinazolin-4-amine

bis(pinacol)diborane
73183-34-3

bis(pinacol)diborane

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: N-((5-bromofuran-2-yl)methyl)-2-(methylsulfonyl)ethanamine; bis(pinacol)diborane With bis-triphenylphosphine-palladium(II) chloride; potassium acetate In dimethyl sulfoxide at 75℃; for 5h; Inert atmosphere;
Stage #2: N-[3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-bromo-quinazolin-4-amine In dimethyl sulfoxide at 75℃; for 16h; Catalytic behavior; Temperature; Solvent; Reagent/catalyst;
47%
3-chloro-4-(3-fluorobenzyloxy)nitrobenzene
443882-99-3

3-chloro-4-(3-fluorobenzyloxy)nitrobenzene

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: H2 / Pt/C / ethanol; tetrahydrofuran
2: propan-2-ol / 70 °C
3: Pd(OAc)2; PPh3; Et3N / dimethylformamide
4: Na(OAc)3BH; HOAc / CH2Cl2
View Scheme
Multi-step reaction with 5 steps
1.1: platinum on carbon; hydrogen / ethanol / 0.83 h / 1292.9 Torr / High pressure
2.1: isopropyl alcohol / 3.5 h / 70 °C
3.1: bis-triphenylphosphine-palladium(II) chloride; N-ethyl-N,N-diisopropylamine / 1,4-dioxane / Inert atmosphere; Reflux
4.1: hydrogenchloride / 1,4-dioxane; tetrahydrofuran / 20 °C
5.1: triethylamine / tetrahydrofuran; methanol / 3 h
5.2: 20 °C / Cooling with ice
View Scheme
Multi-step reaction with 3 steps
1.1: iron; hydrogenchloride / ethanol; water / 3 h / 70 °C
2.1: acetic acid / 1.5 h / 90 °C
3.1: potassium acetate; bis-triphenylphosphine-palladium(II) chloride / dimethyl sulfoxide / 5 h / 75 °C / Inert atmosphere
3.2: 16 h / 75 °C
View Scheme
Multi-step reaction with 4 steps
1: zinc; ammonium chloride / ethanol; water / 12 h / 60 °C
2: isopropyl alcohol / Reflux
3: potassium carbonate; palladium diacetate / ethanol; tetrahydrofuran / 2 h / Reflux
4: 20% palladium hydroxide-activated charcoal; hydrogen / methanol / 20 °C / 2585.81 - 2844.39 Torr
View Scheme
4-chloro-6-iodoquinazoline
98556-31-1

4-chloro-6-iodoquinazoline

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: propan-2-ol / 70 °C
2: Pd(OAc)2; PPh3; Et3N / dimethylformamide
3: Na(OAc)3BH; HOAc / CH2Cl2
View Scheme
Multi-step reaction with 3 steps
1: isopropyl alcohol / Reflux
2: potassium carbonate; palladium diacetate / ethanol; tetrahydrofuran / 2 h / Reflux
3: 20% palladium hydroxide-activated charcoal; hydrogen / methanol / 20 °C / 2585.81 - 2844.39 Torr
View Scheme
Multi-step reaction with 4 steps
1.1: toluene / 1 h / 90 °C
1.2: 5 h / 20 - 72 °C
2.1: N-ethyl-N,N-diisopropylamine / palladium 10% on activated carbon / ethanol / 3 h / 70 °C
3.1: tetrahydrofuran; ethanol; water / 4 h / 25 - 65 °C
4.1: acetic acid; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / 1 h / 30 - 35 °C
4.2: 2.25 h / 22 °C
View Scheme
2-chloro-4-nitrophenol
619-08-9

2-chloro-4-nitrophenol

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: K2CO3 / acetonitrile
2: H2 / Pt/C / ethanol; tetrahydrofuran
3: propan-2-ol / 70 °C
4: Pd(OAc)2; PPh3; Et3N / dimethylformamide
5: Na(OAc)3BH; HOAc / CH2Cl2
View Scheme
Multi-step reaction with 6 steps
1.1: potassium carbonate / acetonitrile / 2 h / 20 - 60 °C / Inert atmosphere
2.1: platinum on carbon; hydrogen / ethanol / 0.83 h / 1292.9 Torr / High pressure
3.1: isopropyl alcohol / 3.5 h / 70 °C
4.1: bis-triphenylphosphine-palladium(II) chloride; N-ethyl-N,N-diisopropylamine / 1,4-dioxane / Inert atmosphere; Reflux
5.1: hydrogenchloride / 1,4-dioxane; tetrahydrofuran / 20 °C
6.1: triethylamine / tetrahydrofuran; methanol / 3 h
6.2: 20 °C / Cooling with ice
View Scheme
Multi-step reaction with 4 steps
1.1: potassium carbonate / acetonitrile / 0.5 h / 20 °C
1.2: Reflux
2.1: iron; hydrogenchloride / ethanol; water / 3 h / 70 °C
3.1: acetic acid / 1.5 h / 90 °C
4.1: potassium acetate; bis-triphenylphosphine-palladium(II) chloride / dimethyl sulfoxide / 5 h / 75 °C / Inert atmosphere
4.2: 16 h / 75 °C
View Scheme
Multi-step reaction with 5 steps
1: potassium carbonate / acetonitrile / 2 h / 60 °C / Inert atmosphere
2: zinc; ammonium chloride / ethanol; water / 12 h / 60 °C
3: isopropyl alcohol / Reflux
4: potassium carbonate; palladium diacetate / ethanol; tetrahydrofuran / 2 h / Reflux
5: 20% palladium hydroxide-activated charcoal; hydrogen / methanol / 20 °C / 2585.81 - 2844.39 Torr
View Scheme
1-(Bromomethyl)-3-fluorobenzene
456-41-7

1-(Bromomethyl)-3-fluorobenzene

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: K2CO3 / acetonitrile
2: H2 / Pt/C / ethanol; tetrahydrofuran
3: propan-2-ol / 70 °C
4: Pd(OAc)2; PPh3; Et3N / dimethylformamide
5: Na(OAc)3BH; HOAc / CH2Cl2
View Scheme
Multi-step reaction with 6 steps
1.1: potassium carbonate / acetonitrile / 2 h / 20 - 60 °C / Inert atmosphere
2.1: platinum on carbon; hydrogen / ethanol / 0.83 h / 1292.9 Torr / High pressure
3.1: isopropyl alcohol / 3.5 h / 70 °C
4.1: bis-triphenylphosphine-palladium(II) chloride; N-ethyl-N,N-diisopropylamine / 1,4-dioxane / Inert atmosphere; Reflux
5.1: hydrogenchloride / 1,4-dioxane; tetrahydrofuran / 20 °C
6.1: triethylamine / tetrahydrofuran; methanol / 3 h
6.2: 20 °C / Cooling with ice
View Scheme
Multi-step reaction with 4 steps
1.1: potassium carbonate / acetonitrile / 0.5 h / 20 °C
1.2: Reflux
2.1: iron; hydrogenchloride / ethanol; water / 3 h / 70 °C
3.1: acetic acid / 1.5 h / 90 °C
4.1: potassium acetate; bis-triphenylphosphine-palladium(II) chloride / dimethyl sulfoxide / 5 h / 75 °C / Inert atmosphere
4.2: 16 h / 75 °C
View Scheme
Multi-step reaction with 5 steps
1: potassium carbonate / acetonitrile / 2 h / 60 °C / Inert atmosphere
2: zinc; ammonium chloride / ethanol; water / 12 h / 60 °C
3: isopropyl alcohol / Reflux
4: potassium carbonate; palladium diacetate / ethanol; tetrahydrofuran / 2 h / Reflux
5: 20% palladium hydroxide-activated charcoal; hydrogen / methanol / 20 °C / 2585.81 - 2844.39 Torr
View Scheme
N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine
231278-20-9

N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: Pd(OAc)2; PPh3; Et3N / dimethylformamide
2: Na(OAc)3BH; HOAc / CH2Cl2
View Scheme
Multi-step reaction with 3 steps
1: triethylamine; 1,2-dimethoxyethane / palladium 10% on activated carbon / methanol / Inert atmosphere
2: triethylamine / methanol / 12 h / Reflux
3: methanol / tetrahydrofuran / 0 - 15 °C
View Scheme
Multi-step reaction with 3 steps
1: triethylamine / palladium 10% on activated carbon / 1,2-dimethoxyethane; methanol / 15 h / 45 - 50 °C / Inert atmosphere
2: triethylamine / methanol / 12 h / Reflux
3: sodium tetrahydroborate / tetrahydrofuran; methanol / 4 h / 10 - 15 °C
View Scheme
3-chloro-4-(3-fluorobenzyloxy)aniline
202197-26-0

3-chloro-4-(3-fluorobenzyloxy)aniline

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: propan-2-ol / 70 °C
2: Pd(OAc)2; PPh3; Et3N / dimethylformamide
3: Na(OAc)3BH; HOAc / CH2Cl2
View Scheme
Multi-step reaction with 5 steps
1: acetic acid / toluene / 2 h / Reflux
2: acetic acid / xylene / 10 h / Reflux
3: triethylamine / palladium 10% on activated carbon / 1,2-dimethoxyethane; methanol / 15 h / 45 - 50 °C / Inert atmosphere
4: triethylamine / methanol / 12 h / Reflux
5: sodium tetrahydroborate / tetrahydrofuran; methanol / 4 h / 10 - 15 °C
View Scheme
Multi-step reaction with 4 steps
1.1: isopropyl alcohol / 3.5 h / 70 °C
2.1: bis-triphenylphosphine-palladium(II) chloride; N-ethyl-N,N-diisopropylamine / 1,4-dioxane / Inert atmosphere; Reflux
3.1: hydrogenchloride / 1,4-dioxane; tetrahydrofuran / 20 °C
4.1: triethylamine / tetrahydrofuran; methanol / 3 h
4.2: 20 °C / Cooling with ice
View Scheme
5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde 4-methylbenzenesulfonate

5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde 4-methylbenzenesulfonate

2-(methylsulfonyl)ethylamine hydrochloride
104458-24-4

2-(methylsulfonyl)ethylamine hydrochloride

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: 5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde 4-methylbenzenesulfonate; 2-(methylsulfonyl)ethylamine hydrochloride With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 30 - 35℃; for 1h;
Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 22 - 23℃; for 2.25h;
Stage #3: With sodium hydroxide In tetrahydrofuran; water for 0.5h;
Stage #1: 5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde 4-methylbenzenesulfonate; 2-(methylsulfonyl)ethylamine hydrochloride With sodium acetate; acetic acid In ethyl acetate at 25 - 30℃; for 1h;
Stage #2: With sodium tris(acetoxy)borohydride In ethyl acetate at 25 - 30℃; for 1.5h;
Stage #3: With water; sodium carbonate In ethyl acetate Product distribution / selectivity;
Stage #1: 5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde 4-methylbenzenesulfonate; 2-(methylsulfonyl)ethylamine hydrochloride With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 30 - 35℃; for 1h;
Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 22℃; for 2.25h;
N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((2-(methylsulfonyl)ethylimino)methyl)furan-2-yl)quinazolin-4-amine
1227853-06-6

N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((2-(methylsulfonyl)ethylimino)methyl)furan-2-yl)quinazolin-4-amine

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((2-(methylsulfonyl)ethylimino)methyl)furan-2-yl)quinazolin-4-amine With methanol; sodium tetrahydroborate In tetrahydrofuran at 0 - 15℃;
Stage #2: With water In tetrahydrofuran
With methanol In tetrahydrofuran at 0 - 15℃;
With sodium tetrahydroborate In tetrahydrofuran; methanol at 10 - 15℃; for 4h;
anthranilic acid nitrile
1885-29-6

anthranilic acid nitrile

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1: Iodine monochloride; acetic acid / 3 h / 25 - 35 °C
2: 2 h / 70 - 75 °C
3: acetic acid / 2 h / 115 - 120 °C
4: triethylamine; 1,2-dimethoxyethane / palladium 10% on activated carbon / methanol / Inert atmosphere
5: triethylamine / methanol / 12 h / Reflux
6: methanol / tetrahydrofuran / 0 - 15 °C
View Scheme
Multi-step reaction with 5 steps
1: acetic acid / 3 h / 25 - 35 °C
2: acetic acid / xylene / 10 h / Reflux
3: triethylamine / palladium 10% on activated carbon / 1,2-dimethoxyethane; methanol / 15 h / 45 - 50 °C / Inert atmosphere
4: triethylamine / methanol / 12 h / Reflux
5: sodium tetrahydroborate / tetrahydrofuran; methanol / 4 h / 10 - 15 °C
View Scheme
Multi-step reaction with 4 steps
1.1: acetic acid; Iodine monochloride / 3 h / 20 °C
2.1: triethylamine; palladium 10% on activated carbon / methanol; 1,2-dimethoxyethane / 3 h / 20 - 45 °C
2.2: 60 °C
3.1: triethylamine; acetic acid / tetrahydrofuran / 1 h / 20 - 35 °C
3.2: 2.5 h / 22 - 25 °C
4.1: acetic acid / 1 h / Reflux; Industrial scale
View Scheme
5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
231278-84-5

5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: triethylamine / methanol / 12 h / Reflux
2: methanol / tetrahydrofuran / 0 - 15 °C
View Scheme
Multi-step reaction with 2 steps
1: triethylamine / methanol / 12 h / Reflux
2: sodium tetrahydroborate / tetrahydrofuran; methanol / 4 h / 10 - 15 °C
View Scheme
Multi-step reaction with 2 steps
1.1: tetrahydrofuran; ethanol; water / 4 h / 25 - 65 °C
2.1: acetic acid; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / 1 h / 30 - 35 °C
2.2: 2.25 h / 22 °C
View Scheme
5-iodoanthranilonitrile
132131-24-9

5-iodoanthranilonitrile

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: 2 h / 70 - 75 °C
2: acetic acid / 2 h / 115 - 120 °C
3: triethylamine; 1,2-dimethoxyethane / palladium 10% on activated carbon / methanol / Inert atmosphere
4: triethylamine / methanol / 12 h / Reflux
5: methanol / tetrahydrofuran / 0 - 15 °C
View Scheme
Multi-step reaction with 4 steps
1: acetic acid / xylene / 10 h / Reflux
2: triethylamine / palladium 10% on activated carbon / 1,2-dimethoxyethane; methanol / 15 h / 45 - 50 °C / Inert atmosphere
3: triethylamine / methanol / 12 h / Reflux
4: sodium tetrahydroborate / tetrahydrofuran; methanol / 4 h / 10 - 15 °C
View Scheme
Multi-step reaction with 3 steps
1.1: triethylamine; palladium 10% on activated carbon / methanol; 1,2-dimethoxyethane / 3 h / 20 - 45 °C
1.2: 60 °C
2.1: triethylamine; acetic acid / tetrahydrofuran / 1 h / 20 - 35 °C
2.2: 2.5 h / 22 - 25 °C
3.1: acetic acid / 1 h / Reflux; Industrial scale
View Scheme
N’-(2-cyano-4-iodophenyl)-N,N-dimethyl formamidine
903597-10-4

N’-(2-cyano-4-iodophenyl)-N,N-dimethyl formamidine

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: acetic acid / 2 h / 115 - 120 °C
2: triethylamine; 1,2-dimethoxyethane / palladium 10% on activated carbon / methanol / Inert atmosphere
3: triethylamine / methanol / 12 h / Reflux
4: methanol / tetrahydrofuran / 0 - 15 °C
View Scheme
Multi-step reaction with 3 steps
1.1: acetic acid / 0.25 h / 125 - 130 °C
2.1: palladium 10% on activated carbon; triethylamine / methanol; 1,2-dimethoxyethane / 0.5 h / 50 °C
3.1: triethylamine; sodium sulfate / methanol / 0.33 h / 0 °C
3.2: 2 h / pH 5 - 6
View Scheme
5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde hydrochloride
388082-76-6

5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde hydrochloride

2-(methylsulfonyl)ethylamine hydrochloride
104458-24-4

2-(methylsulfonyl)ethylamine hydrochloride

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20℃; for 0.5h;
Stage #2: 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde hydrochloride With water In tetrahydrofuran at 20℃; for 4h;
Stage #3: With sodium tris(acetoxy)borohydride In tetrahydrofuran
N-((5-(4-chloro-quinazoline-6-yl)furan-2-yl)methyl)-2-methylsulfonyl ethylamine
1334953-75-1

N-((5-(4-chloro-quinazoline-6-yl)furan-2-yl)methyl)-2-methylsulfonyl ethylamine

3-chloro-4-(3-fluorobenzyloxy)aniline
202197-26-0

3-chloro-4-(3-fluorobenzyloxy)aniline

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: N-((5-(4-chloro-quinazoline-6-yl)furan-2-yl)methyl)-2-methylsulfonyl ethylamine; 3-chloro-4-(3-fluorobenzyloxy)aniline In toluene; butanone at 20 - 90℃;
Stage #2: With sodium hydroxide In tetrahydrofuran; water; toluene; butanone at 20℃;
5-formylfurane-2-boronic acid
27329-70-0

5-formylfurane-2-boronic acid

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: triethylamine / palladium 10% on activated carbon / 1,2-dimethoxyethane; methanol / 15 h / 45 - 50 °C / Inert atmosphere
2: triethylamine / methanol / 12 h / Reflux
3: sodium tetrahydroborate / tetrahydrofuran; methanol / 4 h / 10 - 15 °C
View Scheme
Multi-step reaction with 3 steps
1.1: tetrahydrofuran / 2 h / 20 °C
2.1: palladium 10% on activated carbon / methanol / 8 h / Reflux
3.1: N-ethyl-N,N-diisopropylamine; acetic acid / tetrahydrofuran / 1 h / 40 °C
3.2: 3 h / 20 °C
View Scheme
Multi-step reaction with 3 steps
1.1: tetrahydrofuran / 2 h / 20 °C
2.1: palladium 10% on activated carbon; N-ethyl-N,N-diisopropylamine / methanol / 8 h / Reflux
3.1: N-ethyl-N,N-diisopropylamine; acetic acid / tetrahydrofuran / 1 h / 40 °C
3.2: 3 h / 20 °C
View Scheme
N(1)-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-N,N-dimethylformamidine
1227853-05-5

N(1)-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-N,N-dimethylformamidine

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: acetic acid / xylene / 10 h / Reflux
2: triethylamine / palladium 10% on activated carbon / 1,2-dimethoxyethane; methanol / 15 h / 45 - 50 °C / Inert atmosphere
3: triethylamine / methanol / 12 h / Reflux
4: sodium tetrahydroborate / tetrahydrofuran; methanol / 4 h / 10 - 15 °C
View Scheme
2-Methanesulfonyl-ethylamine
49773-20-8

2-Methanesulfonyl-ethylamine

5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde tosylate

5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde tosylate

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Stage #1: 2-Methanesulfonyl-ethylamine; 5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde tosylate With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 30 - 35℃; for 2h;
Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 20 - 25℃; for 3h;
Stage #3: With water; sodium hydroxide In tetrahydrofuran
2-(diethoxymethyl)furan
13529-27-6

2-(diethoxymethyl)furan

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: n-butyllithium / 1,2-dimethoxyethane / 2.75 h / -40 - -35 °C / Inert atmosphere
1.2: 2.5 h / -40 - -35 °C
2.1: N-ethyl-N,N-diisopropylamine; acetic acid / tetrahydrofuran / 2 h / 30 - 35 °C
2.2: 3 h / 20 - 25 °C
View Scheme
Multi-step reaction with 3 steps
1.1: n-butyllithium / hexane; 1,2-dimethoxyethane / 5 h / -50 °C / Inert atmosphere
1.2: 6.5 h / -40 - 20 °C / Inert atmosphere
2.1: palladium 10% on activated carbon; N-ethyl-N,N-diisopropylamine / methanol / 8 h / Reflux
3.1: N-ethyl-N,N-diisopropylamine; acetic acid / tetrahydrofuran / 1 h / 40 °C
3.2: 3 h / 20 °C
View Scheme
5-formylfurane-2-boronic acid
27329-70-0

5-formylfurane-2-boronic acid

N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine
231278-20-9

N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine

lapatanib
231277-92-2

lapatanib

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: palladium 10% on activated carbon; triethylamine / 1,2-dimethoxyethane; methanol / 14 h / 50 °C
2.1: N-ethyl-N,N-diisopropylamine; acetic acid / tetrahydrofuran / 1 h / 40 °C
2.2: 3 h / 20 °C
View Scheme
lapatanib
231277-92-2

lapatanib

lapatinib hydrogen bromide salt
1092929-27-5

lapatinib hydrogen bromide salt

Conditions
ConditionsYield
With hydrogen bromide In tetrahydrofuran; water at 21 - 60℃; for 23.5833h;99.9%
With hydrogen bromide In methanol; water Reflux;83.4%
lapatanib
231277-92-2

lapatanib

lapatinib dihydrochloride

lapatinib dihydrochloride

Conditions
ConditionsYield
With hydrogenchloride In methanol; water Reflux;96.5%
With hydrogenchloride In methanol; water at 20℃;93%
With hydrogenchloride In methanol at 25℃; for 20h;
lapatanib
231277-92-2

lapatanib

lapatinib monohydrochloride
1383531-68-7

lapatinib monohydrochloride

Conditions
ConditionsYield
With hydrogenchloride In tetrahydrofuran; water at 20℃;96%
With hydrogenchloride In methanol; water Reflux;95.2%
lapatanib
231277-92-2

lapatanib

lapatinib nitric acid salt

lapatinib nitric acid salt

Conditions
ConditionsYield
With nitric acid In water; acetonitrile Reflux;95.8%
lapatanib
231277-92-2

lapatanib

toluene-4-sulfonic acid
104-15-4

toluene-4-sulfonic acid

({5-[4-({3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}amino)quinazolin-6-yl]furan-2-yl}methyl) [2-(methylsulfonyl)ethyl]azanium 4-methylbenzenesulfonate

({5-[4-({3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}amino)quinazolin-6-yl]furan-2-yl}methyl) [2-(methylsulfonyl)ethyl]azanium 4-methylbenzenesulfonate

Conditions
ConditionsYield
In methanol at 20℃;95%
In methanol at 25℃; for 20h;
lapatanib
231277-92-2

lapatanib

benzenesulfonic acid
98-11-3

benzenesulfonic acid

N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine ditosylate

N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine ditosylate

Conditions
ConditionsYield
In acetonitrile at 20℃; Heating;94.5%
lapatanib
231277-92-2

lapatanib

(2E)-but-2-enedioic acid
110-17-8

(2E)-but-2-enedioic acid

lapatinib difumarate

lapatinib difumarate

Conditions
ConditionsYield
In acetonitrile Heating;94.3%
lapatanib
231277-92-2

lapatanib

methanesulfonic acid
75-75-2

methanesulfonic acid

lapatinib dimesylate

lapatinib dimesylate

Conditions
ConditionsYield
In propan-1-ol at 20℃; Product distribution / selectivity; Heating;93.2%
lapatanib
231277-92-2

lapatanib

benzoic acid
65-85-0

benzoic acid

lapatinib dibenzoate

lapatinib dibenzoate

Conditions
ConditionsYield
In tetrahydrofuran; water at 60℃; for 0.5h;93%
lapatanib
231277-92-2

lapatanib

toluene-4-sulfonic acid
104-15-4

toluene-4-sulfonic acid

lapatinib ditosylate
388082-78-8

lapatinib ditosylate

Conditions
ConditionsYield
In tetrahydrofuran at 20 - 57.5℃;92.5%
In methanol at 45 - 65℃; Reflux;88%
In methanol at 25 - 65℃; for 3h;88%
lapatanib
231277-92-2

lapatanib

(1S)-10-camphorsulfonic acid
3144-16-9

(1S)-10-camphorsulfonic acid

lapatinib (1S)(+)-camphorsulfonic acid salt

lapatinib (1S)(+)-camphorsulfonic acid salt

Conditions
ConditionsYield
In acetone at 20℃; for 24h;89.8%
lapatanib
231277-92-2

lapatanib

ethanesulfonic acid
594-45-6

ethanesulfonic acid

lapatinib diesylate

lapatinib diesylate

Conditions
ConditionsYield
In methanol at 21 - 60℃; for 26.5h;89.3%
lapatanib
231277-92-2

lapatanib

maleic acid
110-16-7

maleic acid

lapatinib dimaleate

lapatinib dimaleate

Conditions
ConditionsYield
In ethanol; water Product distribution / selectivity; Heating;89%
lapatanib
231277-92-2

lapatanib

naphthalene-1,5-disulfonate
81-04-9

naphthalene-1,5-disulfonate

lapatinib naphthalene-1,5-disulfonic acid salt

lapatinib naphthalene-1,5-disulfonic acid salt

Conditions
ConditionsYield
In methanol Reflux;86.5%
lapatanib
231277-92-2

lapatanib

citric acid
77-92-9

citric acid

lapatinib citric acid salt
1092929-12-8

lapatinib citric acid salt

Conditions
ConditionsYield
In methanol for 1h; Concentration; Solvent; Temperature; Reflux;86.2%
In tetrahydrofuran at 21 - 60℃; for 4h; Product distribution / selectivity;62.6%
lapatanib
231277-92-2

lapatanib

methanesulfonic acid
75-75-2

methanesulfonic acid

lapatinib monomesylate
1092928-98-7

lapatinib monomesylate

Conditions
ConditionsYield
In water; acetone at 50 - 55℃; Product distribution / selectivity;85.8%
lapatanib
231277-92-2

lapatanib

naphthalene-2-sulfonate
120-18-3

naphthalene-2-sulfonate

lapatinib naphthalene-2-sulfonic acid salt

lapatinib naphthalene-2-sulfonic acid salt

Conditions
ConditionsYield
In acetonitrile Concentration; Solvent; Reflux;85.4%
lapatanib
231277-92-2

lapatanib

(S)-Malic acid
97-67-6

(S)-Malic acid

lapatinib mono-L-malate
1092929-16-2

lapatinib mono-L-malate

Conditions
ConditionsYield
In isopropyl methanesulfonate; water Product distribution / selectivity; Heating;85.1%
lapatanib
231277-92-2

lapatanib

aspirin
50-78-2

aspirin

alapatinib

alapatinib

Conditions
ConditionsYield
With dmap; diisopropyl-carbodiimide In diethyl ether at -20℃; Reagent/catalyst; Solvent; Temperature; Schlenk technique; Inert atmosphere;85%
lapatanib
231277-92-2

lapatanib

ethanesulfonic acid
594-45-6

ethanesulfonic acid

lapatinib monoesylate
1092929-02-6

lapatinib monoesylate

Conditions
ConditionsYield
In water; acetone at 21℃; for 18.5h; Reflux;84.7%
lapatanib
231277-92-2

lapatanib

(S)-Malic acid
97-67-6

(S)-Malic acid

lapatinib di-L-malate

lapatinib di-L-malate

Conditions
ConditionsYield
In ethyl acetate at 20℃; Heating;84.6%
lapatanib
231277-92-2

lapatanib

malonic acid
141-82-2

malonic acid

lapatinib dimalonate

lapatinib dimalonate

Conditions
ConditionsYield
In ethanol Reflux;83.4%

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