1275595-86-2Relevant academic research and scientific papers
Preparation method of 6-substituted furanyl-4-substituted aminoquinazoline derivative and key intermediate thereof
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, (2020/02/14)
The invention relates to a preparation method of a 6-substituted furanyl-4-substituted aminoquinazoline derivative and a key intermediate thereof. 2-halo-5-cyanobenzoate and 3-chloro-4-(3-fluorobenzyloxy)aniline are used as raw materials, and 6-cyano-4-[3-chloro-4-(3-fluorobenzyloxy)phenyl]aminoquinazoline is obtain through an amidation reaction, a formamidine salt substitution reaction and a condensation reaction; then 6-(furan-2-yl)-4-[3-chloro-4-(3-fluorobenzyloxy)phenyl]aminoquinazoline or 6-(5-formylfuran-2-yl)-4-[3-chloro-4-(3-fluorobenzyloxy)phenyl]aminoquinazoline are obtained througha Grignard reaction and an acidification reaction; and then lapatinib or selatinib are prepared through a Mannich reaction or imidization and a reductive amination reaction. The preparation method hasthe advantages that the raw materials are cheap and are easily available, selectivity of the reaction is high, purity of the product is high, and industrial production is facilitated.
A pharmaceutically acceptable salt and its preparation and use
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Paragraph 0093-0095, (2018/06/19)
The invention relates to a pharmaceutical salt, and a preparation method and application thereof, in particular to an acid addition salt of N-(4-(3-fluorobenzyl)-3-chlorphenyl)-6-(5-((2-(methylsulfinyl)ethylamino)methyl)-2-furyl)-quinazoline-4-amine shown
N-[ 3-chloro-4 - (3-fluorobenzyloxy) phenyl] - 6 - [5 - [[ 2 - (methyl sulfinyl) ethyl] amino] methyl] - 2-furyl] - 4-quinazolinamine polymorphic and its preparation method
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Paragraph 0090; 0103-0105, (2017/02/24)
The invention relates to an N-[3-chloro-4-(3-fluorobenzyloxy) phenyl]-6-[5-[[2-(methylenesulfonyl) ethyl] amino] methyl]-2-furanyl]-4-quinazolinamine polymorph and a preparation method thereof, in particular to an N-[3-chloro-4-(3-fluorobenzyloxy) phenyl]
4 - (substituted anilino) quinazoline derivatives polymorphs of xylene sulfonate and its preparation and use
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Paragraph 0121; 0122; 0123; 0124; 0125, (2016/10/10)
The invention relates to the polymorphs of N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfinyl)ethylamino)methyl)-2-furanyl)-quinazoline-4-aminexylene sulfonate (compound I) used as tyrosine kinase inhibitors. In particular, the invention re
Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer
Zhang, Long,Fan, Chuanwen,Guo, Zongru,Li, Ying,Zhao, Shuyong,Yang, Shaobo,Yang, Yingying,Zhu, Jianrong,Lin, Dong
, p. 833 - 841 (2013/10/22)
To develop potent dual EGFR/HER-2 inhibitors with improved druggability, a series of new lapatinib analogs were designed and synthesized. Compared with lapatinib, L-2, L-4 and M-6 were more active against BT-474 or NCI-N87 cells. In vivo efficacy studies indicated that L-2 significantly suppressed tumor growth in NCI-N87 (94.8% inhibition) or SK-OV-3 xenograft (85.7% inhibition) without causing significant loss of body weight. And the inhibition rates of lapatinib in the two xenograft models were 89.7% and 78.8%, respectively. Moreover, further studies revealed that the potent in vivo activities of L-2 may be mainly attributed to its superior aqueous solubility and oral bioavailability. In addition, a high-yielding one-pot procedure was developed for the synthesis of lapatinib and its analogs.
4-(SUBSTITUTED ANILINO)QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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Page/Page column 17, (2012/08/14)
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositons and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
4-(Substituted Anilino)-Quinazoline Derivatives Useful as Tyrosine Kinase Inhibitors
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Page/Page column 12, (2012/08/28)
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
