cas 937263-43-9, Irbinitinib | Articles data

Articles about 937263-43-9Total 9 be found

Preparation method of tucatinib
The invention relates to a preparation method of tucatinib. The method comprises the following steps: by taking 4-hydroxy-6-chloroquinazoline as a raw material, firstly carrying out copper-catalyzed C-N cross-coupling reaction on the 4-hydroxy-6-chloroquinazoline and 2-amino-4, 4-dimethyl-4, 5-dihydrooxazole, then activating the 4-hydroxy of quinazolinone by adopting a BOP, and enabling product and 4-([1, 2, 4] triazolo [1, 5-a] pyridine-7-yloxy)-3-methylaniline to be subjected to a nucleophilic substitution reaction to obtain tucatinib. With the method, using of high-corrosivity and high-toxicity reagents is avoided, and the method has low requirements on equipment, the operation difficulty and environmental protection requirements are reduced, and the method has the advantages of high product yield and high product purity; the process is simple and environment-friendly and suitable for large-scale production.
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Paragraph 0016; 0028; 0030; 0031; 0033; 0034 0036; 0037

(2021/01/25)

Preclinical activity of HER2-selective tyrosine kinase inhibitor tucatinib as a single agent or in combination with trastuzumab or docetaxel in solid tumor models
HER2 is a transmembrane tyrosine kinase receptor that mediates cell growth, differentiation, and survival. HER2 is overexpressed in approximately 20% of breast cancers and in subsets of gastric, colorectal, and esophageal cancers. Both antibody and smallm
De Vries, Peter,Forero-Torres, Andres,Kulukian, Anita,Lee, Patrice,Peterson, Scott,Rosler, Robert,Taylor, Janelle,Watson, Daniel
p. 976 - 987
(2020/08/06)

New Synthetic Route to Tucatinib
A new and improved synthetic route to tucatinib is described that involves three key intermediates. The first of these, 4-([1,2,4]triazolo[1,5- a ]pyridin-7-yloxy)-3-methylaniline, was prepared on a 100 g scale in 33percent yield over five steps and 99percent purity. Next, N 4 -(4-([1,2,4]triazolo[1,5- a ]pyridin-7-yloxy)-3-methylphenyl)quinazoline-4,6-diamine was isolated in 67percent yield over three steps and >99percent purity. Then, 4,4-dimethyl-2-(methylthio)-4,5-dihydrooxazole trifluoromethanesulfonate was prepared under mild conditions in 67percent yield over two steps. Finally, tucatinib was obtained in 17percent yield over nine steps and in >99percent purity (HPLC). Purification methods used to isolate the product and the intermediates involved in the route are also reported.
Bu, Lehao,Chen, Wenxin,Liu, Yaowei,Mao, Yongjun,Yin, Lingfeng,Zhang, Long
p. 2660 - 2664
(2019/06/19)

Irbinitinib intermediates for preparation of (by machine translation)
The invention belongs to the organic synthesis and bulk drug preparation technology field, in particular to the treatment of breast cancer drug Irbinitinib preparation method and intermediate, comprising the steps of: 2 - methyl - 4 - nitro-phenol (formul
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(2019/07/10)

Solid dispersions of a ERB2 (HER2) inhibitor
A solid dispersion of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and processes for preparing the solid dispersion are provided herein. Also, a pharmaceutical composition comprising a solid dispersion of N4-(4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and uses thereof are provided herein.
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Page/Page column 21; 22

(2016/10/27)

TREATMENT OF BRAIN CANCER
Compounds for the treatment of brain cancer are provided herein. Pharmaceutical compositions comprised of those compounds for the treatment of brain cancer are also provided herein.
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Paragraph 00153

(2013/10/08)

SOLID DISPERSION
A solid dispersion of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and processes for preparing the solid dispersion are provided herein. Also, a pharmaceutical composition comprising a solid dispersion of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and uses thereof are provided herein.
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Paragraph 000141

(2013/04/25)

Processes and intermediates for the preparation of N4-phenyl-quinazoline-4-amine derivatives
This invention provides compounds of Formula (I), wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.
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Page/Page column 56

(2009/09/05)