氰基甲酸乙酯置于氢氧化钾,氮体系中,用 硝基甲烷,二甲基亚砜 作为反应溶剂,以68%的收率获得产物硝基乙酸乙酯 参考文献:Preparation Of Nitroesters Via The Reaction Of Nitroparaffins With 标题:Preparation Of Nitroesters Via The Reaction Of Nitroparaffins With 摘要:一种制备烷基硝基乙酸酯的方法,包括在共同溶剂和碱性条件下反应硝基烷和氰基甲酸酯.所得产物通过简单的一步反应,使用廉价易得的反应物制备.
专利号:US-5144034-A 优先权日:1990-04-06 标题 :Process for the synthesis of cyclopentene derivatives of purines 发明人:JOHNSON M ROSS; PEEL MICHAEL R; STERNBACH DANIEL D 权利人:GLAXO INC 摘要:This invention relates to a new process for preparing certain optically active cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1'R-cis isomer of carbovir, (1'R-cis)-2-amino-1,9-dihydro-9[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-purin-6-one, an antiviral agent.
专利号:US-4866175-A 优先权日:1966-11-08 标 题 :Novel process for the synthesis of quinoxaline and benzimidazole-N-oxides 发明人:ISSIDORIDES COSTAS H; HADDADIN MAKHLUF J 权利人:RESEARCH CORP 摘要:The synthesis of quinoxaline and benzimidazole-N-oxides and of ester amd amide derivatives of 3-hydroxy-2-quinoxalinecarboxylic acid by a movel process consisting of the reaction between a benzofuroxan and an activated methylene-containing compound under basic conditions.
专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:WO-9815532-A1 优先权日:1996-10-09 标 题:Solid phase synthesis of heterocyclic compounds 发明人:MARZINZIK ANDREAS; FELDER EDUARD 权利人:CIBA GEIGY AG; MARZINZIK ANDREAS; FELDER EDUARD 摘要:Here we report a study on a reaction sequence on solid phase, suitable for the generation of molecular diversity on small heterocycles. For each reaction, suitable conditions on solid phase were worked out and a variety of reactive agents (building blocks) was utilized in an effort to grasp the system's breadth of applicability. The inventive reaction sequence can be applied, for example, to exploit by the combinatorial approaches of the split and mix concept. The reaction sequence comprises the following steps: a) a solid carrier having reactive surface groups is loaded directly or via a spacer group with a compound bearing an aldehyde or a methylketon function, b) said function is modified using the Witting reaction or the aldol condensation, c) the heterocyclic ring is closed using a compound comprising two nucleophiles, wherein at least one of the said nucleophiles is NH2.
专利号:US-4460786-A 优先权日:1980-07-10 标题 :Process for the selective addition of a compound having an activated carbon atom onto a substituted conjugated diene 发明人:MOREL DIDIER 权利人:RHONE POULENC IND 摘要:The selective addition of a compound having an activated carbon atom onto the carbon atom in the 4-position of a buta-1,3-diene carrying a hydrocarbon substituent on the carbon atom in the 2-position is achieved by reacting the compound having the activated carbon atom with the buta-1,3-diene carrying the hydrocarbon substituent in water or in an aqueous-alcoholic mixture in the presence of a catalyst which consists of at least one water-soluble phosphine and at least one rhodium compound, the catalyst being in solution in the water or aqueous alcoholic mixture. The products obtained are useful as precursors of intermediates for the synthesis of vitamins and perfumes.
专利号:US-4532322-A 优先权日:1983-05-23 标题:Preparation of thiazine derivatives 发明人:JACKSON ARTHUR; HEYES GRAHAM 权利人:FINE ORGANICS LTD 摘要:A method for the preparation of a thiazine derivative of the formula ##STR1## where each R is independently selected from hydrogen or a lower alkyl having 1 to 4 carbon atoms, the method comprising reacting together a sulphur donor which is selected from sulfur, ammonium or alkali metal sulfides, ammonium or alkali metal hydrosulfides, or hydrogen sulfide, 1,1-bis(methylthio)-2-nitroethene and a compound of the formula n n H.sub.2 NCR.sub.2 CR.sub.2 CR.sub.2 OSO.sub.3 H n n where each R is as defined above. n A preferred method is for the preparation of tetra-2-(nitromethylene)-2H-1,3-thiazine which possesses broad spectrum insecticidal activity, and is also useful as an intermediate in the synthesis of other insecticides.
参考标题:Synthesis Of (+/-)-Phthalascidin 650 Analogue: New Synthetic Route To (+/-)-Phthalascidin 622 作者:Christian R. Razafindrabe,Sylvain Aubry,Benjamin Bourdon,Marta Andriantsiferana,Stéphane Pellet-Rostaing,Marc Lemaire |发布日期:2010.11 摘要:Synthesis Of Functionalized Phenolic α-Amino-Alcohol (+/-)-13 As Synthetic Precursor Of The Catechol Tetrahydroisoquinoline Structure Of Phthalascidin 650 Is Disclosed. Starting From 3-Methylcatechol 5, Eight Steps Of Synthesis Give Rise To The Synthesis Of Phenolic α-Amino-Alcohol (+/-)-13 In 27% Overall Yield. This Synthetic Strategy Involves The Elaboration Of Fully Functionalized Aromatic Aldehyde 8 And Its
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 270. 摘要:Härtinger, S., Science of Synthesis Knowledge Updates, (2010) 1, 133. 摘要:Crawley, M. L., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 414. 摘要:MacMillan, D. W. C.; Watson, A. J. B., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 345. 摘要:Mase, N., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 176.