CAS: 598-52-7; N-Methylthiourea

该化合物是一种有机硫化合物,其分子式CH4N2S通常用于有机合成和工业应用,是生产药品,农用化学品和橡胶化学品的多种中间体.该化合物的硫尿亚衍生物结构在核生殖替代和复杂反应中具有回活动性,使其对协调化学和催化具有价值.甲基硫尿亚在标准条件下具有稳定性,并且可溶解于极地溶剂,便于其在实验室和制造过程中使用.它作为硫磺捐献者和金属复合体中的离子,其作用进一步增强了其在专门化学合成物中的效用. 适当处理建议是由于潜在的毒性.

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145013-05-4 621-83-0 268551-65-1

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合成工艺路线路线简述

    S-Methyl N-Methyl Dithiocarbamate置于ammonium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应 2.0H,反应生成 N-甲硫脲
    参考文献:新型hsp70抑制剂n,N'-二取代硫脲衍生物的设计,合成和生物学评估
    标题:新型hsp70抑制剂n,N'-二取代硫脲衍生物的设计,合成和生物学评估
    摘要:作为新型的热激蛋白70(hsp70)抑制剂,基于atpase域(核苷酸结合域,Nbd)的x射线结构设计并合成了n,N'-二取代的硫脲衍生物.atpase活性抑制试验表明,这些化合物有效抑制hsp70 Atpase活性.结果表明,化合物370/371/374/379/380 // 392/394/397/404/405和407可以抑制hsp70 Atpase的转换,且抑制率较高:50.42,38.46,50.45,44.12,47.13,200μm中分别为50.50,40.95,65.36,46.23,35.78和58.37.在bt474乳腺癌细胞系中观测到与化合物379和化合物405的拉帕替尼具有显着的协同作用.r 1.0拉帕替尼耐药细胞系.hsp70抑制剂可能被开发为抗药性癌症治疗中的协同药物.
    DOI:10.1016/j.Ejmech.2016.04.042

    海关参考信息

    专利信息


    专利号:US-11759760-B2
    优先权日:2016-01-12
    标题:Apparatus and process for the automated chemical synthesis of compounds
    发明人:BODE JEFFREY WILLIAM; WANNER BENEDIKT MATTHIAS; CHEN KUANG-YEN; PATTABIRAMAN VIJAYA; NICHOLS PAULA LOUISE
    权利人:ETH ZUERICH
    摘要:Provided is an apparatus for the automated synthesis of at least one chemical compound including: at least one cartridge including at least one first compartment for providing at least one first reagent for the chemical synthesis of the at least one compound; at least one second compartment for providing at least one second reagent for the chemical synthesis of the at least one compound, and at least one third compartment for purifying the at least one synthesized compound; at least one reaction container for providing the compounds to be fed into at least one of the compartments of the cartridge and/or collecting the reaction product from at least one of the compartments of the cartridge; at least one solvent container at least two flow path selecting valves and at least one pump.

    专利号:US-8314090-B2
    优先权日:2008-11-06
    标 题:Methods of synthesis of benzazepine derivatives
    发明人:HOWBERT J JEFFRY; KUSUKUNTLA VENKAT REDDY; TRETYAKOV ALEXANDER; NIELSEN NATHAN; KRASIK PAVEL; JIANG JI-LONG; YANG HONG WOON
    权利人:HOWBERT J JEFFRY; KUSUKUNTLA VENKAT REDDY; TRETYAKOV ALEXANDER; NIELSEN NATHAN; KRASIK PAVEL; JIANG JI-LONG; YANG HONG WOON; VENTIRX PHARMACEUTICALS INC; ARRAY BIOPHARMA INC
    摘要:The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.

    专利号:US-2023312596-A1
    优先权日:2020-07-20
    标题:Method for large-scale synthesis of tetrodotoxin
    发明人:WANG GUANGYIN; LI XIAOMING; WANG CHENGXI; HUANG PING; BAI HUA; LAI LIANG; GUO PENG; JIANG BIAO; ZHU WENFENG
    权利人:SHANGHAI SHENGPING MEDICAL EQUIPMENT CO LTD; SHANGHAI VASTPRO TECH DEVELOPMENT CO LTD; ZHEJIANG BOXIAO BIOPARMACEUTICAL CO LTD
    摘要:The present invention provides a method for biological and chemical synthesis of tetrodotoxin, specifically comprising the following steps: using cheap and easily available benzyl acetate as a raw material, and performing biological fermentation to obtain an optically pure intermediate ((5S, 6R)-5, 6-dihydroxycyclohexa-1, 3-dienyl) methyl acetate (formula I); and performing a series of chemical conversions on the intermediate to finally obtain tetrodotoxin at a purity of 95% or more without purifying the product. The present invention has the potential of large-scale production, and is an excellent alternative to the existing extraction method from a pufferfish.

    专利号:US-6525061-B1
    优先权日:1999-11-16
    标题 :Methods for the solid phase synthesis of 2-amino-4(H)-quinazolinone derivatives
    发明人:GOPALSAMY ARIAMALA; YANG HUI Y
    权利人:WYETH CORP
    摘要:The present invention relates to solid phase synthesis of substituted 2-amino-4(H)-quinazolinone compounds of formula (I):having pharmacological activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.

    专利号:US-4627968-A
    优先权日:1984-09-10
    标 题 :Synthesis of crystalline aluminosilicate with alkylurea or alkylthiourea
    发明人:KAI TADASHI
    权利人:ASAHI CHEMICAL IND
    摘要:In the synthesis of a crystalline aluminosilicate by heating an aqueous mixture containing a silica source, an alumina source and an alkali metal source, at least one compound selected from lower alkylureas and lower alkylthioureas is permitted to co-exist with the mixture.

    专利号:WO-2011156355-A1
    优先权日:2010-06-09
    标题 :Production method of phenyl guanidine salts and their intermediates
    发明人:JOHNSON MICHAEL ROSS; KANG MYUNG-CHOL; BRAY BRIAN L; SCHNEIDER STEPHEN
    权利人:KAINOS MEDICINE INC; JOHNSON MICHAEL ROSS; KANG MYUNG-CHOL; BRAY BRIAN L; SCHNEIDER STEPHEN
    摘要:This invention relates to methods for producing phenyl guanidine salts having pharmacological activity, as well as to the identification and synthesis of compounds useful as intermediates for producing phenyl guanidine salts having pharmacological activity.
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    主要参考文献

    [参考文献]: A R Jones, Et Al. The Fate Of N-Methyl-N'-(Hydroxymethyl)Thiourea In The Rat. Xenobiotica. 1983 Feb;13(2):73-9.
    [参考文献]: Christine M Gross, Et Al. Endothelial Nitric Oxide Synthase Deficient Mice Are Protected From Lipopolysaccharide Induced Acute Lung Injury. Plos One. 2015 Mar 18;10(3):E0119918.
    [参考文献]: J Maldonado, Et Al. [参考文献]: Therapie. 1980 May-Jun;35(3):409-12.
    [参考文献]: M Yabuki, Et Al. Metabolism Of 4-[参考文献]: Reza Heidari, Et Al. Ameliorative Effects Of Taurine Against Methimazole-Induced Cytotoxicity In Isolated Rat Hepatocytes. Sci Pharm. 2012 Oct-Dec;80(4):987-99.

    合成参考文献


    摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 280.
    摘要:Chebanov, V. A.; Gorobets, N. Yu.; Sedash, Yu. V., Science of Synthesis: Multicomponent Reactions, (2013) 1, 31.
    摘要:Wan, J.-P., Science of Synthesis: Multicomponent Reactions, (2013) 2, 385.
    摘要:Wan, J.-P., Science of Synthesis: Multicomponent Reactions, (2013) 2, 383.
    摘要:Teratology, The International Journal of Abnormal Development., 23(335), 1981 []
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