cas 288383-20-0, Cediranib | Articles data

Articles about 288383-20-0Total 9 be found

Article title
Article abstract
Author
Journal number and time
Download

Understanding the Alkylation of a Phenol by 1-(3-Chloropropyl)pyrrolidine: Evidence for the Intermediacy of an Azetidinium Ion
The final synthetic step in the synthesis of cediranib, AZD2171, 1, is the alkylation of a phenol with an alkyl halide to generate an ether. Our need to understand and control the formation of synthetic impurities generated in this step of the synthesis led us to investigate the kinetics and mechanism of the alkylation of indolphenol, 2, 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxyquinazolin-7-ol, by chloropyrrolidine, 3, 1-(3-chloropropyl)pyrrolidine. Studies in 1-methyl-2-pyrrolidinone (NMP) established that the active alkylating agent is the azetidinium ion, 4, 4-azoniaspiro[3.4]octane, formed via a slow intramolecular cyclization reaction of chloropyrrolidine, 3. The azetidinium ion was isolated as its tetraphenylborate salt from water by heating 3 in the presence of aqueous potassium tetraphenyl borate, and its competence as an intermediate was demonstrated by its fast reaction with 2 to yield cediranib, 1.
Ashworth, Ian W.,Chan, Lai C.,Cox, Brian G.,McFarlane, Ian M.,Phillips, Andrew R.
p. 4754 - 4762
(2018/11/25)

Preparation method for anti-cancer drug of Cediranib
The invention discloses a preparation method for an anti-cancer drug of Cediranib. According to the preparation method, the chemical name of the anti-cancer drug of the Cediranib is 4-(4-fluoro-2-methylindole-5-yloxy)-6-methoxy-7-[3-(pyrrolidine-1-yl)propoxy] quinazoline, the chemical formula of the anti-cancer drug of the Cediranib is C25H27FN4O3, and the structural formula of the anti-cancer drug of the Cediranib is as shown in the specification. The preparation method has the advantages that the 4-(4-fluoro-2-methylindole-5-yloxy)-6-methoxy-7-[3-(pyrrolidine-1-yl)propoxy] quinazoline is generated through etherification reaction and reduction reaction, the Cediranib is finally generated through oxidation cyclization reaction, and therefore the phenomenon that chlorinating agents such asphosphorus trichloride, phosphorus pentachloride, thionyl chloride, phosgene and phosphorus oxychloride which are harmful to the environment are used due to the fact that the Cediranib is synthesizedthrough existing chlorination reaction can be avoided, the environment can be protected, the technological process is simple, the method is rapid and convenient, raw materials are easy to obtain, economical and environmentally friendly, the product yield and the product purity are high, the quality is controllable, and the method is suitable for industrial production.
-
(2018/08/04)

Preparation methods for drug cediranib treating non-small cell lung cancer and kidney cancer and intermediate thereof
The invention discloses preparation methods for a drug cediranib treating non-small cell lung cancer and kidney cancer and an intermediate thereof. The chemical name of the drug cediranib treating non-small cell lung cancer and kidney cancer is 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline, and the structural formula thereof is as shown in the description.The preparation methods are simple, the cediranib intermediate and 5-hydroxy-4-fluoro-2-methylindole are synthesized to obtain cediranib through a condensation reaction, so that the atom is more economical, the reaction is more selective, and the operation is more controllable, the preparation method for the cediranib is more controllable, the product quality is improved, and the economic technology of active ingredients is advanced.
-
(2018/06/15)

Preparation method of vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor Cediranib
The invention discloses a preparation method of a vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor Cediranib. The chemical name of the VEGF receptor tyrosine kinase inhibitor Cediranib is 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline, the chemical formula is C25H27FN4O3, and the structural formula is shown in the description. A preparation technology which adopts readily-available raw materials and is economical and environmentally friendly is adopted, a process method suitable for industrial production is found, the preparation process is novel, and the reaction process is simplified, so that the reaction yield is increased; the preparation method has important significance to the improvement on the economical and socialbenefits of the Cediranib.
-
(2018/06/15)

SOLID STATE FORMS OF CEDIRANIB MALEATE
The present disclosure relates to solid state forms of Cediranib maleate, processes for preparation thereof and pharmaceutical compositions thereof.
-
Paragraph 0076; 0077;0078

(2017/03/14)

west Neeb salt and its crystalline form, and its preparation method and pharmaceutical composition (by machine translation)
The invention relates to west Neeb salt and its crystalline form, compared with the prior art, and its west Neeb salt of the invention the crystalline form has more excellent in water solubility. The present invention also relates to the west states the Neeb salt and its crystal preparation method, the medicament composition and its use in treating and/or preventing the pathological angiogenic diseases use of the medicament. (by machine translation)
-
(2017/03/21)

CHEMICAL PROCESS
The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline.
-
Page/Page column 54

(2008/12/05)

QUINAZOLINE DERIVATIVES AS ANGIOGENESIS INHIBITORS
The invention relates to the use of compounds of the formula I: wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S; Z is -O-, -NH-, -S-, -CH2- or a direct bond; n is 0-5; m is 0-3; R represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, -NRR (wherein R and R, which may be the same or different, each represents hydrogen or C1-3alkyl), or RX- (wherein X and R are as defined herein; R represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N-C1-4alkylcarbamoyl, N,N-di(C1-4alkyl)carbamoyl, aminosulphonyl, N-C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N-(C1-4alkylsulphonyl)amino, N-(C1-4alkylsulphonyl)-N-(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group RX (wherein X and R are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
-
Page/Page column 138

(2008/06/13)

Therapeutic combinations of antihypertensive and antiangiogenics agents
The invention concerns the use of a combination of an anti-angiogenic agent and an anti-hypertensive agent for use in the manufacture of a medicament for the treatment of a disease state associated with angiogenesis in a warm-blooded mammal, such as a human being. The invention also relates to pharmaceutical compositions comprising an anti-angiogenic agent and an anti-hypertensive agent, to kits thereof and to a method of treatment of a disease state associated with angiogenesis which comprises the administration of an effective amount of a combination of an anti-angiogenic agent and an anti-hypertensive agent to a warm-blooded animal, such as a human being.
-
(2008/06/13)

Chemical Properties

Boiling Point: 626.557 °C at 760 mmHg
Flash Point:332.73 °C
Density: 1.286 g/cm³
Solubility:Acetone (Slightly), DMSO (Slightly), Methanol (Slightly)
Storage Temp.:Sealed in dry,Store in freezer, under -20°C
Vapor Pressure: 0mmHg at 25°C
Refractive Index: 1.642
PKA: 16.14±0.30(Predicted)
PSA: 72.50000
LogP: 5.16210

Global suppliers and manufacturers of 288383-20-0total 120 suppliers on LookChem

Company Name
Business Type
Min Order
FOB Price
Main Products
Contact

Hubei DiBo chemical co., LTD
Business Type:Other
Min Order:100 Kilogram
FOB Price:USD $ 1.0-1.0 / Kilogram
Main Products:34
Country:

Dayang Chem (Hangzhou) Co.,Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:USD $ 3.0-3.0 / Kilogram
Main Products:993
Country:

Xi'an Xszo Chem Co., Ltd.
Business Type:Manufacturers
Min Order:1 Gram
FOB Price:USD $ 0.1-0.1 / Gram
Main Products:108
Country:

Chemwill Asia Co., Ltd.
Business Type:Manufacturers
Min Order:5 Kiloliter
FOB Price:USD $ 1.2-5.0 / Kiloliter
Main Products:56
Country:

Hebei yanxi chemical co.,LTD.
Business Type:Trading Company
Min Order:1 Gram
FOB Price:USD $ 500.0-500.0 / Gram
Main Products:79
Country:

Henan Tianfu Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:USD $ 230.0-230.0 / Kilogram
Main Products:67
Country:

Hebei Nengqian Chemical Import and Export Co., LTD
Business Type:Trading Company
Min Order:1 Gram
FOB Price:USD $ 1.0-2.0 / Gram
Main Products:161
Country:

Zhuozhou Wenxi import and Export Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 139.0-210.0 / Kilogram
Main Products:1
Country:

Shanghai Upbio Tech Co.,Ltd
Business Type:Lab/Research institutions
Min Order:1 Gram
FOB Price:USD $ 11.0-11.0 / Gram
Main Products:30
Country:

Qingdao Beluga Import and Export Co., LTD
Business Type:Lab/Research institutions
Min Order:1 Gram
FOB Price:No Data
Main Products:116
Country:

Shandong Hanjiang Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:No Data
Main Products:77
Country:

Henan Wentao Chemical Product Co., Ltd.
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:43
Country:

Triumph International Development Limilted
Business Type:Lab/Research institutions
Min Order:1 Gram
FOB Price:USD $ 1.0-1.0 / Gram
Main Products:24
Country:

Taizhou Crene Biotechnology co.ltd
Business Type:Lab/Research institutions
Min Order:100 Milligram
FOB Price:No Data
Main Products:16
Country:

Hangzhou Keyingchem Co.,Ltd
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:102
Country:

Afine Chemicals Limited
Business Type:Lab/Research institutions
Min Order:1 Gram
FOB Price:No Data
Main Products:95
Country:

Hangzhou J&H Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:No Data
FOB Price:No Data
Main Products:46
Country:

Zibo Hangyu Biotechnology Development Co., Ltd
Business Type:Lab/Research institutions
Min Order:10 Gram
FOB Price:USD $ 100.0-100.0 / Gram
Main Products:3478
Country:

SHANGHAI SYSTEAM BIOCHEM CO., LTD
Business Type:Lab/Research institutions
Min Order:100 Gram
FOB Price:USD $ 100.0-2000.0 / Gram
Main Products:24
Country:

HANGZHOU YUNUO CHEMICAL CO.,LTD
Business Type:Trading Company
Min Order:1 Gram
FOB Price:No Data
Main Products:83
Country:

Post a RFQ

Cas No.:

Product Name:

Quantity:

Email:

Company name:

Valid Period:

Detailed Requirements:

Enter 15 to 2000 letters.Word count: 0 letters

Attach files(File Format: Jpeg, Jpg, Gif, Png, PDF, PPT, Zip, Rar,Word or Excel Maximum File Size: 3MB)

What can I do for you?
Get Best Price

Get Best Price for 288383-20-0

Article Database

288383-20-0

Articles about 288383-20-0Total 9 be found

More Articles about upstream products of 288383-20-0

More Articles about downstream products of 288383-20-0

Chemical Properties

Boiling Point: 626.557 °C at 760 mmHg

Flash Point:332.73 °C

Density: 1.286 g/cm³

Solubility:Acetone (Slightly), DMSO (Slightly), Methanol (Slightly)

Storage Temp.:Sealed in dry,Store in freezer, under -20°C

Vapor Pressure: 0mmHg at 25°C

Refractive Index: 1.642

PKA: 16.14±0.30(Predicted)

PSA: 72.50000

LogP: 5.16210

Global suppliers and manufacturers of 288383-20-0total 120 suppliers on LookChem

Article Database

288383-20-0

Articles about 288383-20-0Total 9 be found

More Articles about upstream products of 288383-20-0

More Articles about downstream products of 288383-20-0

Chemical Properties

Boiling Point: 626.557 °C at 760 mmHg

Flash Point:332.73 °C

Density: 1.286 g/cm3

Solubility:Acetone (Slightly), DMSO (Slightly), Methanol (Slightly)

Storage Temp.:Sealed in dry,Store in freezer, under -20°C

Vapor Pressure: 0mmHg at 25°C

Refractive Index: 1.642

PKA: 16.14±0.30(Predicted)

PSA: 72.50000

LogP: 5.16210

Global suppliers and manufacturers of 288383-20-0total 120 suppliers on LookChem

Density: 1.286 g/cm³