High quality. Factory supply. In stock. Best price. 1.Quick response within 24 hours. 2.Best quality in your requirement. 3.We pay more attention on delivery time, and usually ship on time. 4.Free samples will be provided. 5.Ensure specifications an
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inquiryOur Services 1. New Molecules R&D 2. Own test center HPLC NMR GC LC-MS 3. API and Intermediates from China reputed manufacturers 4. Documents support COA MOA MSDS DMF open part Our advantages 1. Government awarded company. Top 100 enterprises in
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inquiryHangzhou Hysen pharma CO.,LTD. is a professional Pharmaceutical company. We are specialized in manufacturing and R&D of API & Intermediates, Contract Manufacturing, Contract Research, and International Trading business as well. *We ow
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inquiryDayangchem's R&D center can offer custom synthesis according to the contract research and development services for the fine chemicals, pharmaceutical, biotechnique and some of the other chemicals. DayangChem can provide different quantities
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inquiryJinlan Pharm-Drugs Technology Co.,Limited (with its export company Hangzhou Royall Import & Export Co.,Ltd.)is located in Hangzhou, Zhejiang Province. Neighboring Ningbo port, Shanghai port, Hangzhou Xiaoshan Int’l Airport and Shanghai Pu
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inquiry1. Guaranteed purity; 2. Large quantity in stock; 3. Largest manufacturer; 4. Best service after shipment with email; 5. High quality & competitive price; ...... Appearance:Yellow powder Package:1kg/foil bag; 1kg/tin ; 25kg/drum ; 25k
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inquiryName Lapatinib Synonyms N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine Molecular Formul
Cas:388082-78-8
Min.Order:100 Gram
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Type:Other
inquiryThe above product is Ality Chemical's strong item with best price, good quality and fast supply. Ality Chemical has been focusing on the research and production of this field for over 14 years. At the same time, we are always committed to providi
1. Factory price and high quality must be guaranteed, base on 8 years of production and R&D experience2. Free samples will be provided,ensure specifications and quality are right for customer3. Customers will receive the most professional technical s
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inquiryShanghai Seasonsgreen Chemical is a high-tech research and development, production, sale and custom synthesis set in one high-tech chemical products enterprises. Our sales and marketing division is located in Shanghai, serving international pharmaceu
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inquiryOur advantage: 1: High quality and Competitive price 2: Quality control, GC&HPLC&NMR or as your requested 3: Packing as your requested, and double check before shipment 4: Prompt shipment with professional documents 5: Excellent after-
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inquiryOur main production base is located in Xuzhou industry park. We are certified both to the ISO 9001 and ISO 14001 Standards, have a safety management system in place.Our R&D team masters core technology for process-design of target building block
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Type:Manufacturers
inquiryName:Lapatinib Ditosylate CAS NO:388082-78-8 Grade:Medical scientific research and export Molecular formula:C41H40ClFN4O11S3 Molecular weight:915.4229 Product Quality 12 years of chemical raw materials Mature operation of the industry Syst
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inquiryTIANFUCHEM--388082-78-8-- Lapatinib ditosylate in stock Our company was built in 2009 with an ISO certificate.In the past 10 years, we have grown up as a famous fine chemicals supplier in China And we had established stable business rel
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inquiryLIDE PHARMACEUTICALS LIMITED is a professional chemicals and APIs leading manufacturer in China. Our core business line covers APIs, Intermediates, Herb extract, etc. We are specialized in chemical synthesis, process development of pharmaceu
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inquiryOur advantages: 1, High quality with competitive price: 1) Standard:BP/USP/EP/Enterprise standard 2) All Purity≥99% 3) We are manufacturer and can provide high quality products with factory price. 2, Fast and safe delivery 1) Parcel can be
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inquiryWITH US,YOUR MONEY IN SAFE,YOUR BUSINESS IN SAFE 1)Quick Response Within 12 hours; 2)Quality Guarantee: All products are strictly tested by our QC, confirmed by QA and approved by third party lab in China, USA, Canada, Germany, UK, Italy, France et
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Type:Trading Company
inquirycas 388082-78-8 99% Lapatinib ditosylate powder Product Name: Lapatinib ditosylate CAS: 388082-78-8 MF: C41H40ClFN4O11S3 MW: 925.46 EINECS: 642-915-3 Appearance:white Storage:roo
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Negotiable
Type:Trading Company
inquiryName: Lapatinib ditosylate monohydrate Synonyms: Lapatinib ditosylate hydrate; N-(3-Chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine bis(4-methylbenzenesulfonate) monohydrate CAS:
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inquiryWe are leading fine chemicals supplier in China and we had established stable business relationships with Samsung,LG,Merck,Thermo Fisher Scientific and so on.Our main business covers the fields below: 1.Noble Metal Catalysts (Pt.Pd...)
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inquiry1. Guaranteed purity; 2. Large quantity in stock; 3. Largest manufacturer; 4. Best service after shipment with email; 5. High quality & competitive price; Appearance:White Crystalline Powder Storage:Store in sealed conta
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Min.Order:10 Gram
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Type:Other
inquiry1,In No Less ten years exporting experience. 2.Lower Price with higher quality 3,Free sample 4,We are sincerely responsible for the "product quality" and "After Service" Onchem specialized in APIs, chemical intermedi
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Type:Trading Company
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Type:Trading Company
inquiryLapatinib ditosylate CAS:388082-78-8 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of chemical intermediates, specializing in high quality organic int
Cas:388082-78-8
Min.Order:1 Gram
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Type:Lab/Research institutions
inquiryHello, dear friend! I'm Hansen and Allen from China. Welcome to my lookchem mall! The following is a brief introduction of our company's products and services. If you are interested in our products, please contact us by emai
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inquiry1)quick response within 12 hours; 2)quality guarantee: all products are strictly tested by our qc, confirmed by qa and approved by third party lab in china, usa, canada, germany, uk, italy, france etc. 3) oem/odm available; 4) reasonable &
Cas:388082-78-8
Min.Order:10 Gram
Negotiable
Type:Trading Company
inquiryLapatinib Ditosylate CAS: 388082-78-8 Specification WATER CONTENT NMT 0.5% w/w 9 SPECIFIC OPTICAL ROTATION Between +108 and +115 measured at 365 nm. 10 R
Cas:388082-78-8
Min.Order:1 Kilogram
Negotiable
Type:Other
inquiryAppearance:Yellow solid Storage:Store in a cool,dry place and keep away from direct strong light Package:As customer request Application:Used for Synthesis API and Research Transportation:By Sea/Air/Courier Port:Qingdao/Shanghai
Cas:388082-78-8
Min.Order:0 Metric Ton
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inquiry2-(methylsulfonyl)ethylamine hydrochloride
toluene-4-sulfonic acid
5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
lapatinib ditosylate
Conditions | Yield |
---|---|
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With tetrabutylammomium bromide; triethylamine In tetrahydrofuran at 30℃; for 3h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 20℃; for 4h; Stage #3: toluene-4-sulfonic acid In tetrahydrofuran at 50℃; for 1h; | 94.9% |
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran at 20℃; for 3h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran at 20℃; for 12h; Stage #3: toluene-4-sulfonic acid In tetrahydrofuran at 20℃; for 12h; | 82.8% |
Stage #1: 2-(methylsulfonyl)ethylamine hydrochloride; 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde With acetic acid; N-ethyl-N,N-diisopropylamine In tetrahydrofuran; N,N-dimethyl-formamide at 35℃; for 1h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran; N,N-dimethyl-formamide at 20 - 25℃; for 2h; Stage #3: toluene-4-sulfonic acid | 72% |
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 tetrahydrofuran; acetic acid at 30 - 35℃; for 1h; Stage #2: With sodium tris(acetoxy)borohydride In tetrahydrofuran; acetic acid at 22℃; for 2 - 4h; Stage #3: toluene-4-sulfonic acid With sodium hydroxide In tetrahydrofuran; acetic acid |
2-Methanesulfonyl-ethylamine
toluene-4-sulfonic acid
5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde
lapatinib ditosylate
Conditions | Yield |
---|---|
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; Stage #3: toluene-4-sulfonic acid In methanol; dichloromethane | 93% |
Conditions | Yield |
---|---|
In tetrahydrofuran at 20 - 57.5℃; | 92.5% |
In methanol at 45 - 65℃; Reflux; | 88% |
In methanol at 25 - 65℃; for 3h; | 88% |
Conditions | Yield |
---|---|
Stage #1: N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazoline-4-amine hydrochloride With sodium hydroxide In water; ethyl acetate pH=~ 10; Inert atmosphere; Stage #2: toluene-4-sulfonic acid In N,N-dimethyl-formamide at 40℃; for 1h; | 90.1% |
lapatinib monohydrochloride
toluene-4-sulfonic acid
lapatinib ditosylate
Conditions | Yield |
---|---|
Stage #1: lapatinib monohydrochloride With sodium hydroxide In water; ethyl acetate pH=10; Inert atmosphere; Stage #2: toluene-4-sulfonic acid In N,N-dimethyl-formamide at 40℃; for 1h; | 90.1% |
2-Methanesulfonyl-ethylamine
toluene-4-sulfonic acid
lapatinib ditosylate
Conditions | Yield |
---|---|
Stage #1: 2-Methanesulfonyl-ethylamine; 5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde tosylate With N-ethyl-N,N-diisopropylamine In tetrahydrofuran; isopropyl alcohol for 1h; Industrial scale; Stage #2: With sodium tris(acetoxy)borohydride; isopropyl alcohol In tetrahydrofuran at 20℃; for 1.66667h; Industrial scale; Stage #3: toluene-4-sulfonic acid Industrial scale; Further stages; | 88% |
N’-(2-cyano-4-iodophenyl)-N,N-dimethyl formamidine
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 5 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 5: methanol / 3 h / Reflux View Scheme |
5-formylfurane-2-boronic acid
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 4 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 4: methanol / 3 h / 25 - 65 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: triethylamine; palladium / tetrahydrofuran; ethanol / 7 h / 65 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / tetrahydrofuran / 0.33 h / 20 °C 2.2: 2 h / 40 °C 2.3: 3 h / 25 - 40 °C 3.1: tetrahydrofuran / 6 h / 65 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: palladium 10% on activated carbon / isopropyl methanesulfonate / 0.08 h 1.2: 3 h / 70 °C 3.1: tetrahydrofuran / 4 h / 20 - 55 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: palladium 10% on activated carbon / isopropyl methanesulfonate / 0.08 h 1.2: 3 h / 70 °C 2.1: isopropyl methanesulfonate; water / 4.08 - 4.17 h / 25 - 65 °C 3.1: acetic acid; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / 1 h / 30 - 35 °C 3.2: 2.25 h / 22 - 23 °C 3.3: 0.5 h 4.1: tetrahydrofuran / 4 h / 20 - 55 °C View Scheme |
3-chloro-4-(3-fluorobenzyloxy)aniline
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 6 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 6: methanol / 3 h / 25 - 65 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: 1-methyl-pyrrolidin-2-one / 0.5 h / 20 - 25 °C 1.2: 0.33 - 0.5 h 2.1: palladium 10% on activated carbon / ethanol; water / 0.08 h 2.2: 3 h / 70 °C 3.1: tetrahydrofuran; ethanol; isopropyl methanesulfonate; water / 2.08 h / 20 - 65 °C 4.1: acetic acid; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / 1 h / 30 - 35 °C 4.2: 2 - 4 h / 22 - 23 °C 4.3: 0.5 h 5.1: tetrahydrofuran; water / 3 - 4 h / 20 - 63 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: tributyl-amine / toluene / 70 - 80 °C 1.2: 2 h / Heating / reflux 2.1: palladium 10% on activated carbon / ethanol; water / 0.08 h 2.2: 3 h / 70 °C 3.1: tetrahydrofuran; ethanol; isopropyl methanesulfonate; water / 2.08 h / 20 - 65 °C 4.1: acetic acid; N-ethyl-N,N-diisopropylamine / tetrahydrofuran / 1 h / 30 - 35 °C 4.2: 2 - 4 h / 22 - 23 °C 4.3: 0.5 h 5.1: tetrahydrofuran; water / 3 - 4 h / 20 - 63 °C View Scheme |
N(1)-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-N,N-dimethylformamidine
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 5 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 5: methanol / 3 h / 25 - 65 °C View Scheme |
2-(diethoxymethyl)furan
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 3 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 3.1: Isopropyl acetate / 1 h / 65 - 70 °C View Scheme |
6-iodo-4-hydroxyquinazoline
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1.1: trifluoroacetic acid / toluene / 110 - 115 °C / Molecular sieve; Inert atmosphere 2.1: potassium carbonate / triphenyl-arsane; tris-(dibenzylideneacetone)dipalladium(0) / N,N-dimethyl-formamide / 2 h / 60 - 65 °C / Inert atmosphere 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 3.2: 2 h / 20 - 25 °C 4.1: toluene-4-sulfonic acid / methanol / 1 h / 25 °C 5.1: trichlorophosphate / toluene / 0.17 h / 20 °C / Inert atmosphere 5.2: 3 h / 30 - 75 °C 6.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 7.1: sodium hydroxide / ethyl acetate; water / pH ~ 10 / Inert atmosphere 7.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 8 steps 1.1: trifluoroacetic acid / toluene / 110 - 115 °C / Molecular sieve; Inert atmosphere 2.1: potassium carbonate / triphenyl-arsane; tris-(dibenzylideneacetone)dipalladium(0) / N,N-dimethyl-formamide / 2 h / 60 - 65 °C / Inert atmosphere 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 4.1: sodium tris(acetoxy)borohydride / dichloromethane / 2 h / 20 - 25 °C 5.1: toluene-4-sulfonic acid; methanol / 1 h / 25 °C 6.1: triethylamine; trichlorophosphate / toluene / 3 h / 75 °C / Inert atmosphere 7.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 8.1: sodium hydroxide / ethyl acetate; water / pH 10 / Inert atmosphere 8.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 9 steps 1.1: trifluoroacetic acid / toluene / 110 °C / Inert atmosphere 2.1: bis(dibenzylideneacetone)-palladium(0); potassium carbonate; triphenyl-arsane / N,N-dimethyl-formamide / 2 h / 60 - 65 °C / Inert atmosphere 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 3.2: 2 h / 20 - 25 °C / Inert atmosphere 4.1: triethylamine / N,N-dimethyl-formamide / 1 h / 20 - 55 °C / Inert atmosphere 5.1: sulfuric acid / acetonitrile / 5.25 h / 40 °C / Inert atmosphere 6.1: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 7.1: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 8.1: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 9.1: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 9 steps 1.1: trifluoroacetic acid / toluene / 110 °C / Inert atmosphere 2.1: bis(dibenzylideneacetone)-palladium(0); potassium carbonate; triphenyl-arsane / N,N-dimethyl-formamide / 2 h / 60 - 65 °C / Inert atmosphere 3.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 3.2: 2 h / 20 - 25 °C / Inert atmosphere 4.1: sulfuric acid; methanol / 2.5 h / 40 - 45 °C / Inert atmosphere 4.2: pH 6-7 5.1: triethylamine / N,N-dimethyl-formamide / 20 - 25 °C / Inert atmosphere 6.1: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 7.1: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 8.1: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 9.1: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme |
2-(methylsulphonyl)-N-({5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-yl}methyl)ethanamine
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: toluene-4-sulfonic acid / methanol / 1 h / 25 °C 2.1: trichlorophosphate / toluene / 0.17 h / 20 °C / Inert atmosphere 2.2: 3 h / 30 - 75 °C 3.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 4.1: sodium hydroxide / ethyl acetate; water / pH ~ 10 / Inert atmosphere 4.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: toluene-4-sulfonic acid; methanol / 1 h / 25 °C 2.1: triethylamine; trichlorophosphate / toluene / 3 h / 75 °C / Inert atmosphere 3.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 4.1: sodium hydroxide / ethyl acetate; water / pH 10 / Inert atmosphere 4.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: sulfuric acid; methanol / 2.5 h / 40 - 45 °C / Inert atmosphere 1.2: pH 6-7 2.1: triethylamine / N,N-dimethyl-formamide / 20 - 25 °C / Inert atmosphere 3.1: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 4.1: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 5.1: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 6.1: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 6 steps 1: triethylamine / N,N-dimethyl-formamide / 1 h / 20 - 55 °C / Inert atmosphere 2: sulfuric acid / acetonitrile / 5.25 h / 40 °C / Inert atmosphere 3: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 4: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 5: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 6: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme |
5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-carbaldehyde
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 1.2: 2 h / 20 - 25 °C 2.1: toluene-4-sulfonic acid / methanol / 1 h / 25 °C 3.1: trichlorophosphate / toluene / 0.17 h / 20 °C / Inert atmosphere 3.2: 3 h / 30 - 75 °C 4.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 5.1: sodium hydroxide / ethyl acetate; water / pH ~ 10 / Inert atmosphere 5.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 6 steps 1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 2.1: sodium tris(acetoxy)borohydride / dichloromethane / 2 h / 20 - 25 °C 3.1: toluene-4-sulfonic acid; methanol / 1 h / 25 °C 4.1: triethylamine; trichlorophosphate / toluene / 3 h / 75 °C / Inert atmosphere 5.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 6.1: sodium hydroxide / ethyl acetate; water / pH 10 / Inert atmosphere 6.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 7 steps 1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 1.2: 2 h / 20 - 25 °C / Inert atmosphere 2.1: triethylamine / N,N-dimethyl-formamide / 1 h / 20 - 55 °C / Inert atmosphere 3.1: sulfuric acid / acetonitrile / 5.25 h / 40 °C / Inert atmosphere 4.1: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 5.1: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 6.1: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 7.1: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 7 steps 1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 1.2: 2 h / 20 - 25 °C / Inert atmosphere 2.1: sulfuric acid; methanol / 2.5 h / 40 - 45 °C / Inert atmosphere 2.2: pH 6-7 3.1: triethylamine / N,N-dimethyl-formamide / 20 - 25 °C / Inert atmosphere 4.1: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 5.1: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 6.1: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 7.1: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme |
6-[5-({[2-(methylsulphonyl)ethyl]amino}methyl)furan-2-yl]quinazolin-4-ol
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: trichlorophosphate / toluene / 0.17 h / 20 °C / Inert atmosphere 1.2: 3 h / 30 - 75 °C 2.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 3.1: sodium hydroxide / ethyl acetate; water / pH ~ 10 / Inert atmosphere 3.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: triethylamine; trichlorophosphate / toluene / 3 h / 75 °C / Inert atmosphere 2.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 3.1: sodium hydroxide / ethyl acetate; water / pH 10 / Inert atmosphere 3.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: dmap / tetrahydrofuran / 2.5 h / 25 - 30 °C / Inert atmosphere 2.1: thionyl chloride; N,N-dimethyl-formamide / chloroform / 5.75 h / Reflux; Inert atmosphere 3.1: tetrahydrofuran / 25 - 65 °C / Inert atmosphere 4.1: water; sodium hydroxide / methanol / 2 h / 25 - 30 °C / Reflux 4.2: 3.5 h / 45 - 50 °C / Reflux View Scheme | |
Multi-step reaction with 5 steps 1: triethylamine / N,N-dimethyl-formamide / 20 - 25 °C / Inert atmosphere 2: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 3: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 4: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 5: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme |
6-iodo-4-(tetrahydro-2H-pyran-2-yloxy)quinazoline
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: potassium carbonate / triphenyl-arsane; tris-(dibenzylideneacetone)dipalladium(0) / N,N-dimethyl-formamide / 2 h / 60 - 65 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 2.2: 2 h / 20 - 25 °C 3.1: toluene-4-sulfonic acid / methanol / 1 h / 25 °C 4.1: trichlorophosphate / toluene / 0.17 h / 20 °C / Inert atmosphere 4.2: 3 h / 30 - 75 °C 5.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 6.1: sodium hydroxide / ethyl acetate; water / pH ~ 10 / Inert atmosphere 6.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 7 steps 1.1: potassium carbonate / triphenyl-arsane; tris-(dibenzylideneacetone)dipalladium(0) / N,N-dimethyl-formamide / 2 h / 60 - 65 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 3.1: sodium tris(acetoxy)borohydride / dichloromethane / 2 h / 20 - 25 °C 4.1: toluene-4-sulfonic acid; methanol / 1 h / 25 °C 5.1: triethylamine; trichlorophosphate / toluene / 3 h / 75 °C / Inert atmosphere 6.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 7.1: sodium hydroxide / ethyl acetate; water / pH 10 / Inert atmosphere 7.2: 1 h / 40 °C View Scheme | |
Multi-step reaction with 8 steps 1.1: bis(dibenzylideneacetone)-palladium(0); potassium carbonate; triphenyl-arsane / N,N-dimethyl-formamide / 2 h / 60 - 65 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 2.2: 2 h / 20 - 25 °C / Inert atmosphere 3.1: sulfuric acid; methanol / 2.5 h / 40 - 45 °C / Inert atmosphere 3.2: pH 6-7 4.1: triethylamine / N,N-dimethyl-formamide / 20 - 25 °C / Inert atmosphere 5.1: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 6.1: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 7.1: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 8.1: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme | |
Multi-step reaction with 8 steps 1.1: bis(dibenzylideneacetone)-palladium(0); potassium carbonate; triphenyl-arsane / N,N-dimethyl-formamide / 2 h / 60 - 65 °C / Inert atmosphere 2.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0.5 h / 20 - 35 °C / Inert atmosphere 2.2: 2 h / 20 - 25 °C / Inert atmosphere 3.1: triethylamine / N,N-dimethyl-formamide / 1 h / 20 - 55 °C / Inert atmosphere 4.1: sulfuric acid / acetonitrile / 5.25 h / 40 °C / Inert atmosphere 5.1: trichlorophosphate; triethylamine / 1,4-dioxane / 20 - 100 °C / Inert atmosphere 6.1: 1,4-dioxane / 1 h / 55 - 60 °C / Inert atmosphere 7.1: potassium carbonate / 1,4-dioxane; water / 2 h / 55 - 85 °C / Inert atmosphere 8.1: N,N-dimethyl-formamide / 1 h / 35 - 40 °C / Inert atmosphere View Scheme |
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: sodium tris(acetoxy)borohydride / dichloromethane / 2 h / 20 - 25 °C 2.1: toluene-4-sulfonic acid; methanol / 1 h / 25 °C 3.1: triethylamine; trichlorophosphate / toluene / 3 h / 75 °C / Inert atmosphere 4.1: isopropyl alcohol / 4 h / 70 °C / Inert atmosphere 5.1: sodium hydroxide / ethyl acetate; water / pH 10 / Inert atmosphere 5.2: 1 h / 40 °C View Scheme |
4-chloro-6-iodoquinazoline
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: acetonitrile / 1 h / Reflux 2.1: triethylamine; palladium 10% on activated carbon / water; 1,2-dimethoxyethane; methanol / 45 - 50 °C 3.1: water / 20 - 30 °C 4.1: N-ethyl-N,N-diisopropylamine / methanol / 20 h / 20 - 25 °C 5.1: sodium hydroxide / methanol / 20 h / 20 - 25 °C 6.1: sodium tris(acetoxy)borohydride / tetrahydrofuran / 1 h / 20 - 25 °C 6.3: 3 h View Scheme | |
Multi-step reaction with 5 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 5.1: tetrahydrofuran; water / 3.5 h / 20 - 60 °C View Scheme | |
Multi-step reaction with 5 steps 1.1: toluene / 1 h / 90 °C 1.2: 3 h / 20 - 72 °C 2.1: N-ethyl-N,N-diisopropylamine / palladium 10% on activated carbon / ethanol / 3 h / 70 °C 3.1: 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 5.1: tetrahydrofuran; water / 2.5 h / 60 °C View Scheme |
2-chloro 4-aminophenol
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: acetonitrile / 1 h / Reflux 2.1: triethylamine; palladium 10% on activated carbon / water; 1,2-dimethoxyethane; methanol / 45 - 50 °C 3.1: water / 20 - 30 °C 4.1: N-ethyl-N,N-diisopropylamine / methanol / 20 h / 20 - 25 °C 5.1: sodium hydroxide / methanol / 20 h / 20 - 25 °C 6.1: sodium tris(acetoxy)borohydride / tetrahydrofuran / 1 h / 20 - 25 °C 6.3: 3 h View Scheme |
2-chloro-4-(6-iodoquinazolin-4-ylamino)phenol
lapatinib ditosylate
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1.1: triethylamine; palladium 10% on activated carbon / water; 1,2-dimethoxyethane; methanol / 45 - 50 °C 2.1: water / 20 - 30 °C 3.1: N-ethyl-N,N-diisopropylamine / methanol / 20 h / 20 - 25 °C 4.1: sodium hydroxide / methanol / 20 h / 20 - 25 °C 5.1: sodium tris(acetoxy)borohydride / tetrahydrofuran / 1 h / 20 - 25 °C 5.3: 3 h View Scheme |
lapatinib ditosylate
Conditions | Yield |
---|---|
With water | 100% |
With water In tetrahydrofuran at 55 - 60℃; for 0.5h; | |
With water In tetrahydrofuran at 5 - 64℃; for 2.5 - 4h; Heating / reflux; |
lapatinib ditosylate
lapatanib
Conditions | Yield |
---|---|
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% |
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