- Ethyl N-cyanoethylimidoate preparation method
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The invention belongs to the field of organic matter synthesis, and particularly relates to an ethyl N-cyanoethylimidoate preparation method, wherein the ethyl N-cyanoethylimidoate is prepared by using acetonitrile as a solvent, using a 50% cyanamide aqueous solution to replace cyanamide, and using ethyl acetimidate hydrochloride as an intermediate. According to the present invention, the new synthesis method is used so as to achieve advantages of cost reducing, environment protection, simple operation, convenient post-treatment, high yield and simple synthesis, and is suitable for industrialproduction.
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Paragraph 0010-0011
(2019/05/16)
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- Preparation method of acetamiprid
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The invention relates to a preparation method of acetamiprid. The preparation method comprises the following steps of enabling 2-chloro-5-chloromethylpyridine and a methylamine water solution to be reacted so as to synthesize N- (6-chloro-3-pyridylmethyl) methylamine; enabling acetonitrile, ethanol and cyanamide to be reacted so as to synthesize ethyl N-cyanoethanimideate; and further synthesizing the acetamiprid from the N-(6-chloro-3-pyridylmethyl) methylamine and the ethyl N-cyanoethanimideate. The preparation method of the acetamiprid, disclosed by the invention, has the following advantages that through control of reaction conditions, the conversion rate of used raw materials is increased, and the preparation method is suitable for industrial production. In addition, the acetamiprid product prepared by the preparation method is high in purity, low in impurity content, and high in mole yield, and a favorable economic benefit is obtained.
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Paragraph 0014
(2017/02/23)
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- A simple and efficient approach to the synthesis of 1-phosphonated 5-amino-1-H-[1,2,4]-triazole from N-functionalized imidates
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In this study, we describe a new and easy synthetic approach to variously substituted triazoles based on the reaction of imidates with phosphorylated hydrazine in good yields. A general mechanism of the reactions was also proposed. Characterization of the products was carried out by several analytical and spectroscopic tools including infrared and nuclear magnetic resonance spectroscopies (1H,13C NMR,31P NMR).
- Jabli, Dhiab,Dridi, Khaireddine,Efrit, Mohamed Lotfi
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p. 759 - 764
(2016/05/09)
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- NOVEL ANTIVIRAL COMPOUNDS
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The present invention relates to compounds of formula (A) as defined herein having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
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Page/Page column 42
(2013/02/27)
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- PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF
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The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, CSK, C-Src, EphB1, EphB2, EphB4, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, SAPK2α, Src, SIK, Syk, Tie2 and TrkB kinases.
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Page/Page column 33-34
(2009/01/23)
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- Easy access to triazoles, triazolopyrimidines, benzimidazoles and imidazoles from imidates
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We have described a new and easy synthesis of triazoles, triazolopyrimidines, benzimidazoles and imidazoles variously substituted based on the reaction of imidates with diamine derivatives. The products were obtained in moderate to good yields. A general mechanism for the reactions is proposed.
- Zarguil,Boukhris,El Efrit,Souizi,Essassi
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body text
p. 5883 - 5886
(2009/04/05)
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- MITOTIC KINESIN INHIBITORS AND METHODS OF USE THEREOF
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This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment of various disorders.
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Page/Page column 33
(2008/06/13)
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- Triazole derivative and pharmaceutical use thereof
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An agent for the prophylaxis and treatment of immune-related diseases, in particular, immunosuppressant, an agent for the prophylaxis and treatment of allergic diseases, an agent for the prophylaxis and treatment of eosinophil-related diseases and an eosinophilia inhibitor, comprising, as an active ingredient, a series of triazole derivatives of the following formula (I) STR1 or the following formula (III) STR2 wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. A novel monocyclic or bicyclic triazole derivative. The agent for the prophylaxis and treatment of immune-related diseases, in particular, immunosuppressant, the agent for the prophylaxis and treatment of allergic diseases, the agent for the prophylaxis and treatment of eosinophil-related diseases, the eosinophilia inhibitor and the novel triazole derivative of the present invention all, have superior eosinophilia-inhibitory action and lymphocyte activation-inhibitory action. They are low toxic and persistent in action. They are particularly effective in the treatment of accumulation and activation of eosinophil and lymphocytes, inflammatory respiratory tract diseases, eosinophil-related diseases such as eosinophilia, and immune-related diseases.
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- Synthesis and pharmacological activity of triazole derivatives inhibiting eosinophilia
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In order to develop novel antiasthmatic agents based on a new mechanism of action, a series of 3-substituted 5-amino-1- [(methylamino)(thiocarbonyl)]-1H-1,2,4-triazole derivatives were synthesized and evaluated in a model in which eosinophilia was induced in the airway through intravenous (iv) injection of Sephadex particles on days 0, 2, and 5. After screening of several hundred derivatives, we finally identified the highly potent eosinophilia inhibitor 5-amino-3-(4-chlorophenyl)-1- [(methylamino)(thiocarbonyl)]-1H-triazole (23c, GCC-AP0341), which had ID50 values of 0.3 and 0.07 mg/kg when administered orally (os) and intraperitoneally (ip), respectively. This compound showed complete inhibition of the hypersensitivity induced by ascaris inhalation at an ip dose of 1 mg/kg as well as low toxicity, with an LD50 value of >2.0 g/kg in mice. Extensive study of its mechanism of action revealed that 23c inhibited eosinophil survival induced by interleukin-5 (IL-5), but had little or no effect on leukotriene D4 (LTD4) or platelet-activating factor (PAF)- induced responses. Taken together, these results suggest 23c as a novel candidate for the treatment of chronic asthma. Further studies are now underway.
- Naito, Youichiro,Akahoshi, Fumihiko,Takeda, Shinji,Okada, Takehiro,Kajii, Masahiko,Nishimura, Hiroko,Sugiura, Masanori,Fukaya, Chikara,Kagitani, Yoshio
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p. 3019 - 3029
(2007/10/03)
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