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Dayang Chem (Hangzhou) Co.,Ltd.

DayangChem exported this product to many countries and regions at best price. If you are looking for the material’s manufacturer or supplier in China, DayangChem is your best choice. Pls contact with us freely for getting detailed product s

Afatinib Manufacturer/High quality/Best price/In stock

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $7.0

Type:Lab/Research institutions

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Zibo Hangyu Biotechnology Development Co., Ltd

Zibo Hangyu Biotechnology Development Co., Ltd is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemi

Afatinib manufacturer

Cas:850140-72-6

Min.Order:10 Gram

FOB Price: $100.0

Type:Lab/Research institutions

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Hubei Vanz Pharm Co.,Ltd

Hubei Vanz Pharm Co. Ltd. is located in Wuhan, Hubei province. We are one of the most professional company in pharm/chmecial industry for more than 10 years. We export to many countries and area with very competitive price, high quality, good serv

Afatinib 850140-72-6 Factory supply

Cas:850140-72-6

Min.Order:1 Gram

Negotiable

Type:Manufacturers

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Hangzhou Dingyan Chem Co., Ltd

Items Standard Result Assay 98%min ----------------------------------------------------------------------------------------------

High purity Various Specifications Tovok,BIBW 2992 CAS:850140-72-6

Cas:850140-72-6

Min.Order:1 Gram

FOB Price: $100.0 / 500.0

Type:Manufacturers

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Kono Chem Co.,Ltd

Afatinib Afatinib Brief Description CAS No.:850140-72-6 MF:C24H25ClFN5O3 MW:485.9384032 Competitive price with high quality Conforms to BP/USP/EP/FCC Afatinib COA ITEM STANDARD

CAS:850140-72-6 afatinib

Cas:850140-72-6

Min.Order:1 Kilogram

Negotiable

Type:Other

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Hangzhou Think Chemical Co. Ltd

Afatinib CAS No.:850140-72-6 Name: Afatinib Synonyms: BIBW 2992; Tovok; (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide

High purity Afatinib CAS No.:850140-72-6

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $2.0

Type:Other

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Henan Allgreen Chemical Co.,Ltd

high quality Appearance:White or off-white Solid Storage:Sealed, dry, microtherm , avoid light and smell. Package:According to the demand of customer Application:Organic synthesis Transportation:by air or by sea Port:shanghai

Afatinib

Cas:850140-72-6

Min.Order:1 Kilogram

Negotiable

Type:Manufacturers

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Ality Chemical Corporation

The 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

Factory Supply Afatinib

Cas:850140-72-6

Min.Order:1

Negotiable

Type:Other

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Xi'an Xszo Chem Co., Ltd.

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

Factory Price API 99% Afatinib 850140-72-6 GMP Manufacturer

Cas:850140-72-6

Min.Order:1 Gram

FOB Price: $0.1

Type:Manufacturers

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Shanghai Seasonsgreen Chemical Co.,Ltd

Shanghai 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

lower price High quality Afatinib

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Manufacturers

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Chemwill Asia Co., Ltd.

Our 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

Afatinib

Cas:850140-72-6

Min.Order:5 Kiloliter

FOB Price: $1.2 / 5.0

Type:Manufacturers

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Hubei DiBo chemical co., LTD

Name:BIBW2992 The alias:Tovok,BIBW 2992 CAS NO: 850140-72-6 Molecular formula:C24H25ClFN5O3 Molecular weight:485.9384 Product Quality 12 years of chemical raw materials Mature operation of the industry System stability Data storage Secur

BIBW2992/CAS:850140-72-6/Raw material supply

Cas:850140-72-6

Min.Order:25 Kilogram

FOB Price: $1.0 / 2.0

Type:Other

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Hebei Nengqian Chemical Import and Export Co., LTD

Our advantages: 1. All inquiries will be replied within 12 hours. 2. Dedication to quality, supply & service. 3. Strictly on selecting raw materials. 4. Reasonable & competitive price, fast lead time. 5. Sample is available for your eva

Afatinib

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $9.0 / 99.0

Type:Trading Company

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Henan Tianfu Chemical Co., Ltd.

Our company was built in 2009 with an ISO certificate.In the past 5 years, we have grown up as a famous fine chemicals supplier in China and we had established stable business relationships with Samsung,LG,Merck,Thermo Fisher Scientific and so on.O

Afatinib 850140-72-6

Cas:850140-72-6

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

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Zhuozhou Wenxi import and Export Co., Ltd

WITH 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

New production CAS 850140-72-6 with best quality

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $139.0 / 210.0

Type:Trading Company

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Hebei Sankai Chemical Technology Co., Ltd

1. Product advantages ♦ High purity, all above 98.5%, no impurities after dissolution ♦ We will test each batch to ensure quality ♦ OEM and private brand services designed for free ♦ Various cap colors available ♦ W

Afatinib CAS850140-72-6

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $289.0 / 499.0

Type:Trading Company

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Henan Sinotech Import&Export Corporation

Chemical Name: Afatinib Cas No.: 850140-72-6 Molecular Structure: Appearance:White powder Storage:Store in cool and dry place, away from sun light. Package:25kg/drum Application: APIs Transportation:By sea

Afatinib? CAS:850140-72-6

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Other

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Hubei Langyou International Trading Co., Ltd

Advantages: Hubei XinRunde Chemical Co., Ltd is a renowned pharmaceutical manufacturer. We can offer high quality products at competitive price in quick delivery with 100% custom pass guaranteed. Never stop striving to offer our best service is

Afatinib CAS NO 850140-72-6

Cas:850140-72-6

Min.Order:1 Kilogram

Negotiable

Type:Other

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HANWAYS CHEMPHARM CO.,LIMITED

Hanways chempharm is a specialized company concentrating on the R&D, production, marketing and technical service of APIs and pharmaceutical intermediates. The marketing department is located in Wuhan. We have two GMP facilities in Hubei Pr

Hot Selling 99% High Purity Top Quality Afatinib CAS 850140-72-6 with Reasonable Price

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $200.0 / 400.0

Type:Trading Company

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Shanghai Upbio Tech Co.,Ltd

1.No Less 8 years exporting experience. Clients can 100% received goods 2.Lower Price with higher quality 3,Free sample 4,We are sincerely responsible for the "product quality" and "After Service" Upbio is Specialized

Afatinib 850140-72-6

Cas:850140-72-6

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

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Xi'an Faithful Biotech Co., Ltd.

We are the manufacturers and suppliers of API in China, and warehouse in Germany and USA of California, which can quickly and safely deliver to your address 1.High quality and competitive price. 2.Free sample for your evaluation. 3.Promptly delivery

ISO Factory Supply 98% High Purity Bulk Afatinib/ Afatinib(BIBW2992MA2) / GILOTRIF(AFATINIB)

Cas:850140-72-6

Min.Order:10 Gram

FOB Price: $3.5

Type:Trading Company

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Qingdao Beluga Import and Export Co., LTD

Beluga chemical professional supply Afatinib/BIBW-2992/CAS:850140-72-6 Why choose Beluga chemical 1. Beluga Chemical has a professional RESEARCH and development team and strong technical force to ensure technical support and research capabilities

Afatinib/BIBW-2992/CAS:850140-72-6

Cas:850140-72-6

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

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Shandong Hanjiang Chemical Co., Ltd.

Hello, 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

Afatinib CAS NO.850140-72-6

Cas:850140-72-6

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

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LIDE PHARMACEUTICALS LIMITED

Advantage : LIDE PHARMACEUTICALS LTD. is a mid-small manufacturing-type enterprise, engaged in pharmaceutical intermediates of R&D, custom-made and production, and also involving trading chemicals for export. We have established the R&amp

Afatinib/ LIDE PHARMA- Factory supply / Best price

Cas:850140-72-6

Min.Order:0

Negotiable

Type:Lab/Research institutions

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Hubei Jiutian Bio-medical Technology Co., Ltd

1,we produce and sell good chemicals around the world. 2,our success rate is about 95%. this means, if customer order is accepted, the probability that the customer will obtain the ordered substances, is 95%. 3,our staff consists of highly qualifie

cas 850140-72-6 Afatinib

Cas:850140-72-6

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

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Hangzhou JINLAN Pharm-Drugs Technology Co., Ltd

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

Afatinib manufacture

Cas:850140-72-6

Min.Order:1 Gram

Negotiable

Type:Trading Company

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Triumph International Development Limilted

Appearance:white powder 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

Sell/Synthesis Afatinib dimaleate|850140-73-7 |BIBW2992 99.9% white powder

Cas:850140-72-6

Min.Order:0 Metric Ton

Negotiable

Type:Lab/Research institutions

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Afine Chemicals Limited

Our 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 enter

high purity Afatinib Base cas no.439081-18-2

Cas:850140-72-6

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

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Enke Pharma-tech Co.,Ltd. (Cangzhou, China )

Cangzhou Enke Pharma Tech Co.,ltd. is located in Cangzhou City, Hebei province ,where is a famous petroleum chemical industry city in China. Enke Pharma a high-tech enterprise ,and we are dedicated to developing and manufacturing new api, intermediat

Afatinib

Cas:850140-72-6

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Lab/Research institutions

inquiry

Hangzhou Keyingchem Co.,Ltd

Hangzhou KeyingChem Co., Ltd. exported this product to many countries and regions at best price. If you are looking for the material’s manufacturer or supplier in China, KeyingChem is your best choice. Pls contact with us freely for getting det

Afatinib

Cas:850140-72-6

Min.Order:0 Metric Ton

Negotiable

Type:Lab/Research institutions

inquiry

Synthetic route

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

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

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

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

afatinib
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;
dimethylaminoacetaldehyde-hydrogen sulphite adduct
1413945-87-5

dimethylaminoacetaldehyde-hydrogen sulphite adduct

afatinib
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

C36H36ClFN5O5P

afatinib
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

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

(2E)-(N,N-dimethylamino)-2-butenoyl chloride
1056149-69-9

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

afatinib
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

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

(E)-4-(dimethylamino)-2-butenoic acid methyl ester
212776-19-7

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

afatinib
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

2-dimethylamino-1-hydroxyethanesulfonic acid sodium salt

C26H31ClFN4O6P

C26H31ClFN4O6P

afatinib
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

C20H18ClF2N5O

(S)-3-hydroxytetyrahydrofurane
86087-23-2

(S)-3-hydroxytetyrahydrofurane

afatinib
850140-72-6

afatinib

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

dimethylaminoacetaldehyde diethyl acetal

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

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

afatinib
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

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

trans-4-dimethylamino crotonic acid chloride hydrochloride salt
1055943-40-2

trans-4-dimethylamino crotonic acid chloride hydrochloride salt

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

2-dimethylamino-1-hydroxyethanesulfonic acid sodium salt

afatinib
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

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

C18H14ClFIN3O2

C18H14ClFIN3O2

afatinib
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%
(S)-diethyl 2-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-ylamino)-2-oxoethylphosphonate
618061-76-0

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

dimethylaminoacetaldehyde diethyl acetal
3616-56-6

dimethylaminoacetaldehyde diethyl acetal

afatinib
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

C18H14BrClFN3O2

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

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

afatinib
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

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

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

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

afatinib
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

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

(2E)-(N,N-dimethylamino)-2-butenoyl chloride
1056149-69-9

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

afatinib
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

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

afatinib
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

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

afatinib
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
N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine
162012-67-1

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

afatinib
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
7-fluoro-6-nitro-3H-quinazolin-4-one
162012-69-3

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

afatinib
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
(E)-4-dimethylamino-but-2-enoic acid tert-butyl ester
1421354-12-2

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

afatinib
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
3-chloro-4-fluorophenylamine
367-21-5

3-chloro-4-fluorophenylamine

afatinib
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
7-fluoro-3H-quinazolin-4-one
16499-57-3

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

afatinib
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
6-nitro-7-[(S)-(tetrahydrofuran-3-yl)oxy]-3,4-dihydroquinazoline-4-one
1621182-18-0

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

afatinib
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

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

afatinib
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

2-chloro-1-fluoro-4-isocyanobenzene

afatinib
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

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

afatinib
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
5-bromo-2-nitrophenol
27684-84-0

5-bromo-2-nitrophenol

afatinib
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

C7H7N3O3

afatinib
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
N-(3-chloro-4-fluoro-phenyl)-formamide
770-22-9

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

afatinib
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

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

afatinib
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
afatinib
850140-72-6

afatinib

L-Aspartic acid
56-84-8

L-Aspartic acid

afatinib di-L-aspartate

afatinib di-L-aspartate

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

afatinib

maleic acid
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

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%
afatinib
850140-72-6

afatinib

maleic acid
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

(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
afatinib
850140-72-6

afatinib

afatinib disulphate

afatinib disulphate

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

afatinib

C22H20ClFN4O4

C22H20ClFN4O4

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

afatinib

afatinib diphosphate

afatinib diphosphate

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

afatinib

methanesulfonic acid
75-75-2

methanesulfonic acid

afatinib dimesylate

afatinib dimesylate

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

afatinib

(S)-Malic acid
97-67-6

(S)-Malic acid

afatinib di-L-malate

afatinib di-L-malate

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

afatinib

dimethyl amine
124-40-3

dimethyl amine

C26H32ClFN6O3

C26H32ClFN6O3

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

afatinib

afatinib dihydrochloride

afatinib dihydrochloride

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

afatinib

oxalic acid
144-62-7

oxalic acid

afatinib dioxalate

afatinib dioxalate

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

afatinib

succinic acid
110-15-6

succinic acid

afatinib disuccinate

afatinib disuccinate

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

afatinib

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

(2E)-but-2-enedioic acid

afatinib fumarate
1398312-22-5

afatinib fumarate

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

afatinib

benzenesulfonic acid
98-11-3

benzenesulfonic acid

afatinib dibenzenesulphonate

afatinib dibenzenesulphonate

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

afatinib

citric acid
77-92-9

citric acid

afatinib citrate
1398313-22-8

afatinib citrate

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

afatinib

C22H20ClFN4O4

C22H20ClFN4O4

Conditions
ConditionsYield
With sodium hydroxide In methanol; water at 50℃; for 24h; Reagent/catalyst; Temperature; Solvent;43%
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