丙二醛 以97%的收率获得1,3,5-三嗪-2,4,6-三胺,N,N'''-1,2-乙二基二[n-[3-[[4,6-二[丁基(2,2,6,6-四甲基-4-哌啶基)氨基]-1,3,5-三嗪-2-基]氨基]丙基]-N,N''-二丁基-N,N''-二(2,2,6,6-四甲基-4-哌啶基)- 参考文献:Manufacture Of Derivatives Of Malondialdehyde 标题:Manufacture Of Derivatives Of Malondialdehyde 摘要:通式为##equ1##的化合物可以在合成反应中替代丙二醛,该化合物可以通过一步反应从二甲基甲酰胺,光气和烷基乙烯醚中得到.
专利信息
专利号:US-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
专利号:US-9994567-B2 优先权日:2015-05-22 标 题:Synthesis of heterocyclic compounds 发明人:IBRAHIM PRABHA N; LIN JACK; SPEVAK WAYNE; ZHANG JIAZHONG 权利人:PLEXXIKON INC 摘要:Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): n nor a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P 1 and P 2 are as defined in this disclosure.
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-8334381-B2 优先权日:2006-11-16 标题 :Process for the preparation of intermediates useful in the synthesis of imatinib 发明人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO 权利人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO; ITALIANA SINT SPA 摘要:It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.
专利号:US-4266058-A 优先权日:1979-07-04 标 题:Synthesis of 2-isopropylamino-pyrimidine 发明人:DEMOSTHENE CLAUDE G; ASPISI CHRISTIAN R 权利人:SOC D ETUDES PROD CHIMIQUE 摘要:The present invention provides a process for the synthesis of 2-isopropylamino-pyrimidine by aminolysis of 2-methylsulphonyl-pyrimidine using isopropylamine. The aminolysis is effected, according to the present invention, by refluxing isopropylamine and 2-methylsulphonyl-pyrimidine in the absence of a solvent. Using this technique, the 2-isopropylamino-pyrimidine has been obtained in a substantially quantitative yield.
专利号:US-8492390-B2 优先权日:2002-05-08 标题 :Synthesis of locked nucleic acid derivatives 发明人:DETLEF SORENSEN MADS; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER 权利人:DETLEF SORENSEN MADS; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER; SANTARIS PHARMA AS 摘要:The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α- L -oxy-LNA, amino-LNA, α- L -amino-LNA, thio-LNA, α- L -thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
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合成参考文献
参考文献:10.1107/s1600536811011123 摘要:Elboulali A, Akriche ST, Al-Deyab SS, Rzaigui M. 2-Amino-pyrimidinium hydrogen sulfate. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o1013. 参考文献:10.1107/s1600536811010658 摘要:Marouani H, Al-Deyab SS, Rzaigui M. 2-Amino-pyrimidinium dihydrogen phosphate monohydrate. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o970–1. 参考文献:10.1107/s1600536811019635 摘要:Hossain GMG. Bis[4-amino-N-(pyrimidin-2-yl)benzenesulfonamidato]-κ2N,N′;κN-aquabis(dimethylformamide-κO)cadmium(II) monohydrate. Acta Crystallogr E Struct Rep Online. 2011 May 28;67(6):m805–6. doi: 10.1107/s1600536811019635. 参考文献:10.1107/s1600536811018198 摘要:Tabatabaee M, Noozari N. 2-Amino-pyrimidin-1-ium 4-methyl-benzene-sulfonate. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1457.