66296-67-1Relevant articles and documents
ALK KINASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF
-
Paragraph 0358; 0361; 0362, (2017/04/18)
An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors
Zhang, Peilong,Dong, Jiaqiang,Zhong, Boyu,Zhang, Deyi,Jin, Can,Meng, Xuejing,Sun, Desheng,Xu, Xiangyuan,Zhou, Yong,Liang, Zhi,Ji, Minghua,Li, Hailong,Xu, Tao,Song, Guowei,Zhang, Ling,Chen, Gang,Yuan, Hongbin,Shih, Joe,Zhang, Ruihao,Hou, Guojun,Jin, Ying,Yang, Qiong
, p. 3738 - 3743 (2015/08/06)
Abstract A new series of 2,4-diamino pyrimidine derivatives with a sulfone-substituted pyrazole right side-chain were discovered as potent anaplastic lymphoma kinase inhibitors. Structure-activity relationship of the left side-chain on phenyl substitutions were explored which delivered many potent ALK inhibitors. Among them, 29a showed favorable pharmacokinetic profiles in rats and dogs together with significant antitumor efficacy in EML4-ALK fusion xenograft model. Graphical abstract
A simple and environmentally benign nitration of pyrazoles by impregnated bismuth nitrate
Ravi,Gore, Girish M.,Tewari, Surya P.,Sikder, Arun K.
, p. 1322 - 1327 (2014/01/06)
We report herein a facile, rapid, and environmentally friendly synthesis of nitropyrazoles in good yields using silica-bismuth nitrate and silica-sulfuric acid-bismuth nitrate at room temperature for the first time. The relatively non-toxic nature, ease o
Faujasite catalyzed nitrodeiodination of iodopyrazoles
Ravi,Tewari, Surya P.
, p. 35 - 39 (2013/09/12)
Nitrodeiodination of iodopyrazoles using nitric acid/Faujasite has been investigated. The present procedure is simple, rapid and convenient and requires no sulfuric acid or oleum and may be applied for the synthesis of several nitropyrazoles in good yield
Facile and environmentally friendly synthesis of nitropyrazoles using montmorillonite K-10 impregnated with bismuth nitrate
Ravi,Tewari, Surya P.
experimental part, p. 37 - 41 (2012/04/10)
Nitropyrazoles in higher yields were synthesized using montmorillonite K-10 impregnated with bismuth nitrate and the present procedure may be applied for the nitration of a wide variety of azoles in the drug and pharmaceutical industries.
Silica-sulfuric acid catalyzed nitrodeiodination of iodopyrazoles
Ravi,Gore, Girish M.,Sikder, Arun K.,Tewari, Surya P.
experimental part, p. 3463 - 3471 (2012/09/22)
We report here the synthesis of nitropyrazoles in good to excellent yields from iodopyrazoles over silica-sulfuric acid catalyst for the first time. The present procedure require less acid, offers a simplified workup procedure, and may be applied for the
Nitrodeiodination of 4-iodo-1-methylpyrazoles
Tret'yakov,Vasilevsky
, p. 2581 - 2584 (2007/10/03)
4-Iodo-1-methylpyrazoles react with a nitrating mixture at 55°C to give the corresponding 4-nitro-1-methylpyrazoles. The qualitative dependence of the nitrodeiodination rate on the structure of the heterocycles and the reaction conditions was considered.