合成目标产物 Ethoxymethylenemalononitrile 主要起始原料 Acetic Anhydride And Malononitrile
(文献来源)合成步骤主要原料 Acetic Anhydride 和 Malononitrile
丙二腈置于原甲酸三乙酯体系中,化学反应生成乙氧基亚甲基丙二腈 参考文献:Reactions Of Orthoesters With Active Methylene Compounds 标题:Reactions Of Orthoesters With Active Methylene Compounds 摘要: Doi:10.1021/ja01139A046
专利号:US-7034154-B2 优先权日:1999-08-10 标 题:Synthesis of substituted pyrazolopyrimidines 发明人:GROSS RAYMOND S; WILCOXEN KEITH M; OGLESBY RICHARD CHRISTOPHER 权利人:NEUROCRINE BIOSCIENCES INC 摘要:Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.
专利号:US-2022340517-A1 优先权日:2019-12-18 标题 :Continuous synthesis method for ethoxymethylenemalononitrile 发明人:HONG HAO; LU JIANGPING; BAO DENGHUI; LIU CHAOJIE; JIA XIAOTONG 权利人:ASYMCHEM LAB TIANJIN CO LTD 摘要:Provided is a continuous synthesis method for ethoxymethylenemalononitrile. The method includes the following steps: malononitrile, triethyl orthoformate and acetic anhydride are continuously fed into a continuous reaction device to perform a condensation reaction, to obtain the ethoxymethylenemalononitrile, and in the process of the condensation reaction, the generated ethoxymethylenemalononitrile is continuously discharged; herein, the molar ratio of the malononitrile, the triethyl orthoformate and the acetic anhydride is 1:(0.9-6.0):(2.0-6.0). By adopting the continuous reaction device in the present disclosure, since the amount of materials involved in the reaction per unit time is greatly reduced, a high temperature dangerous area is reduced, and a safety risk is greatly reduced. In addition, through the continuous reactor, the raw materials may be transiently heated to the reaction temperature, so that the decomposition of the raw materials caused by the long-time heating process is avoided, and the yield is significantly improved. Moreover, in the reaction process of the present disclosure, there is no need for a second-class toxic solvent such as a toluene.
专利号:US-2005020616-A1 优先权日:2003-07-21 标 题 :Aryl fused azapolycyclic compounds 发明人:COE JOTHAM W; O'DONNELL CHRISTOPHER J 权利人:PFIZER 摘要:This invention is directed to compounds of the formula (I): n n nand their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 and Z are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
专利号:US-7205300-B2 优先权日:1997-12-31 标 题:Aryl fused azapolycyclic compounds 发明人:COE JOTHAM WADSWORTH; BROOKS PAIGE ROANNE PALMER 权利人:PFIZER 摘要:This invention is directed to compounds of the formula (I): n nand their pharmaceutically acceptable salts, wherein R 1 , R 2 , and R 3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
专利号:EP-1208102-A1 优先权日:1999-08-10 标 题 :Synthesis of substituted pyrazolopyrimidines
专利号:EP-1344768-A2 优先权日:1999-08-10 标题:Synthesis of substituted pyrazolopyrimidines
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 180. 摘要:Aggarwal, P.; Bebbington, M. W. P., Science of Synthesis Knowledge Updates, (2012) 2, 378. 参考文献:10.1016/j.bmc.2005.10.053 摘要:Holla BS, Mahalinga M, Karthikeyan MS, Akberali PM, Shetty NS. Synthesis of some novel pyrazolo[3,4-d]pyrimidine derivatives as potential antimicrobial agents. Bioorg Med Chem. 2006 Mar 15;14(6):2040–7. doi: 10.1016/j.bmc.2005.10.053.