99586-65-9Relevant articles and documents
Preparation method of 2-cyano-4-fluoropyridine
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Paragraph 0015; 0018; 0021; 0024, (2021/01/30)
The invention discloses a preparation method of 2-cyano-4-fluoropyridine, which comprises the steps of by using 4-chloropyridine-2-methyl formate as a raw material, carrying out ester ammonolysis reaction, amide dehydration reaction and halogen exchange reaction to prepare the 2-cyano-4-fluoropyridine. The method is simple in synthesis process, mild in reaction condition, high in yield and good inproduct purity; the used raw materials are easy to obtain and low in cost, and the preparation method is suitable for industrial production.
Synthesis method of imidazopyridine or pyrimidine derivative
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Paragraph 0022-0025, (2021/05/29)
The invention belongs to the technical field of synthesis, and particularly relates to a synthesis method of an imidazopyridine or pyrimidine derivative. The imidazopyridine or pyrimidine compound is obtained by taking pyridine or pyrimidinecarboxylic acid as a synthon through amidation, Hofmann degradation and cyclization reaction, and the obtained imidazopyridine or pyrimidine derivative can be further converted to generate a functional product. The method has the advantages of easily available raw materials, simple operation, high reaction efficiency, convenient post-treatment, and diversity of functional groups.
Synthesis method of Tucatinib and intermediate product thereof
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Paragraph 0078; 0079; 0080; 0081, (2020/11/09)
The invention discloses a synthesis method of Tucatinib, and the method comprises the following step: carrying out substitution reaction on halate of a compound shown in a formula VI or free alkali thereof serving as a raw material and a compound shown in a formula VII under an alkaline condition to obtain a compound shown in a formula VIII. The raw materials used in the whole synthesis route areeasy to obtain, expensive catalysts are not needed, and the method is suitable for large-scale production and beneficial to industrial production of the Tucatinib.
Preparation method of 2-amino-4-fluoropyridine
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Paragraph 0008; 0020-0021; 0024-0025; 0028-0029, (2018/09/12)
The invention discloses a preparation method of 2-amino-4-fluoropyridine, comprising the synthetic steps of 1, subjecting 2-pyridinecarboxylic acid as a raw material to reaction in the presence of thionyl chloride and a salt to obtain 4-chloropyridine-2-acyl chloride, and subjecting 4-chloropyridine-2-acyl chloride the presence of ammonia to obtain 4-chloropyridine-2-amide; 2, subjecting 4-chloropyridine-2-amide to Hofmann rearrangement reaction to obtain 2-amino-4-chloropyridine; 3, subjecting 2-amino-4-chloropyridine to halogen exchange to obtain 2-amino-4-fluoropyridine. The problems of theexisting preparation method, such as long synthetic path, operational complexity, high pollution of three wastes, poor atomic economy, low yield and high manufacture cost, are solved.
Transition-metal-free synthesis of primary to tertiary carboxamides: A quick access to prodrug-pyrazinecarboxamide
Mete, Trimbak B.,Singh, Ankit,Bhat, Ramakrishna G.
supporting information, p. 4709 - 4712 (2017/11/21)
One-pot expedient and direct carbamoylation of heterocyclics is described. The transformation is realized via direct dehydrogenative aminocarbonylation of heterocyclic compounds under transition-metal-free conditions. This method is regioselective and the protocol is proved to be scalable on a gram scale. Further, the therapeutically useful antitubercular agent pyrazinecarboxamide is successfully synthesized by employing this protocol.
ARYL UREAS WITH ANGIOGENISIS INHIBITING ACTIVITY
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Paragraph 0194; 0195, (2016/02/12)
This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.
As opioid receptor antagonists or inverse agonists of the novel compounds
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Paragraph 0346-0348; 0350; 0352, (2016/10/08)
Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
SUBSTITUTED PYRAZOLONE COMPOUNDS AND METHODS OF USE
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Paragraph 0414, (2015/02/19)
The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Aryl ureas as kinase inhibitors
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Page/Page column 21; 22, (2015/11/30)
This invention relates to new aryl ureas and methods for their synthesis. The inventive compounds are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VE
Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach
Wang, Jun,Zhan, Peng,Li, Zhenyu,Liu, Huiqing,De Clercq, Erik,Pannecouque, Christophe,Liu, Xinyong
, p. 531 - 538 (2014/05/06)
As a continuation of our efforts to discover and develop back-up analogs of DAPYs, novel substituted nitropyridine derivatives were designed via a structure-based core refining approach, synthesized and evaluated for their in vitro HIV-1 activity in MT-4 cells. Preliminary biological evaluation indicated that most of the compounds exhibited marked inhibitory activity against wild-type HIV-1 IIIB. Most notably, the compound 7b was identified as the most promising candidate in inhibiting HIV-1 replication with an EC 50 value of 0.056 μM and a selective index (SI) of 1251, which were much better than those of NVP (EC50 = 0.23 μM) and DLV (EC50 = 0.51 μM). Some other compounds, 7k, 7c, 7j and 7e, were also endowed with a favorable anti-HIV-1 potency (EC50 = 0.034, 0.11, 0.11 and 0.16 μM, respectively). Some antivirally active compounds also showed moderate inhibitory activity against RT. Preliminary structure-activity relationships (SARs) and molecular modeling of these new analogs provide valuable avenues for future molecular optimization.