1025720-99-3Relevant academic research and scientific papers
The hydration of nitriles catalyzed by simple transition metal salt of the fourth period with the aid of acetaldoxime
Ma, Xiaoyun,He, Ying,Wang, Pengcheng,Lu, Ming
, p. 377 - 382 (2012)
We describe here a method for selective hydration of nitriles into the corresponding amides by employing commercially available acetaldoxime and simple transition metal catalysts such as nickel salts, zinc salts, cobalt salts and manganese salts in water. Nickel salts show the highest catalytic activity, owing to their relatively small diameter of the metal cation. Nitriles having electron-withdrawing groups could be converted into the corresponding amides in excellent yields using nickel catalyst at room temperature. Heterocyclic nitriles with heteroatom lone pair positioned ortho to the nitrile group show high reactivity; even these special nitriles could be hydrated by transition metal catalyst and water at refluxing temperature in the absence of acetaldoxime. Copyright
An improved method for the conversion of nitriles to amides using N,N-disubstituted hydroxylamine
Ma, Xiao-Yun,Lu, Ming
, p. 480 - 483 (2011)
An improved method for the selective hydration of nitriles to amides employing N,N-disubstituted hydroxylamine is described leading to a reduction in reaction time and improved yield. Amides having electron-donating groups, which were not reported using the original method, were obtained in excellent yields. The amount of N,N-disubstituted hydroxylamine was reduced from three equivalents to one equivalent and the use of water as the reaction medium is environmentally friendly.
PHOSPHONATE CONJUGATES AND USES THEREOF
-
, (2020/07/31)
Phosphonate conjugates, preferably, bisphosphonate conjugates; methods of inhibiting Ron receptor tyrosine kinase and methods of treatment of bone destruction due to cancer or other conditions utilizing the provided phosphonate conjugates.
Antitumor compound used as AXL inhibitor and application of antitumor compound
-
, (2019/10/23)
The invention discloses a compound shown in a general formula (I) or pharmaceutically acceptable salt of the compound and preparation methods of the compound and the salt, and further discloses pharmaceutical composition containing the compound and an application of the compound and the pharmaceutical composition in preparation of an AXL inhibitory drug. The AXL inhibitory drug is used for treating tumor, nephropathy, immune system disease or circulatory system disease.
INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
-
, (2019/09/30)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
Double-[...] compound and its method and use thereof
-
Paragraph 0590; 0591, (2018/10/11)
The invention provides a type of substituted bicyclic pyrazolone compounds which can be used for inhibiting the activities of receptor tyrosine kinases especially the activities of Axl, Mer, c-Met and Ron kinases. The invention also provides medicine compositions comprising the type of compounds, and applications of the compound and the medicine compositions in drug preparation. The medicines can be used for preventing and treating proliferative diseases or reducing the severity of the diseases.
PHARMACEUTICAL COMPOSITION AND APPLICATION REPLACING QUINOLONE DERIVATIVE, PHARMACEUTICAL ACCEPTABLE SALT, OR STEREOISOMER
-
Paragraph 0218; 0219, (2018/07/06)
Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.
2-QUINOLONE DERIVED INHIBITORS OF BCL6
-
Paragraph 00362, (2018/12/13)
The present invention relates to compounds of formula I that function as inhibitors of BCL6(B- cell lymphoma 6) activity: Formula I wherein X1, X2, X3, R1, R2, R3, R4 and R5 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer,as well as other diseases or conditions in which BCL6 activity is implicated.
Polysubstituted quinolone compounds, and preparation method and use thereof
-
Paragraph 0134; 0135; 0136, (2017/09/19)
The invention provides polysubstituted quinolone compounds, and a preparation method and a use thereof, and concretely provides a polysubstituted quinolone compound represented by formula I, and optical isomers, pharmaceutically acceptable salts or solvates thereof. All groups in the formula I are defined in the description. The quinolone compound has excellent c-Met inhibition activity, and can be used for treating c-Met activity or expression level corrected diseases.
Synthesis and evaluation of a series of pyridine and pyrimidine derivatives as type II c-Met inhibitors
Zhao, Yanmei,Zhang, Jiankang,Zhuang, Rangxiao,He, Ruoyu,Xi, Jianjun,Pan, Xuwang,Shao, Yidan,Pan, Jinming,Sun, Jingjing,Cai, Zhaobin,Liu, Shourong,Huang, Weiwei,Lv, Xiaoqing
, p. 3195 - 3205 (2017/05/25)
In this study, a series of novel pyridine and pyrimidine-containing derivatives were designed, synthesized and biologically evaluated for their c-Met inhibitory activities. In the biological evaluation, half of the target compounds exhibited moderate to p
