2'-甲基乙酰乙酰苯胺 反应生成 邻甲苯异氰酸酯 参考文献:Novel Method For The Preparation Of Organic Isocyanates1 标题:Novel Method For The Preparation Of Organic Isocyanates1 摘要: DOI:10.1021/jo01069A048
专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-6924385-B2 优先权日:2002-11-18 标 题:Method for synthesis of aliphatic isocyanates from aromatic isocyanates 发明人:LETTMANN CHRISTIAN; KOHLSTRUK STEPHAN; STOCHNIOL GUIDO; SPYROU EMMANOUIL 权利人:DEGUSSA 摘要:The invention relates to a method for synthesis of aliphatic isocyanates from aromatic isocyanates in substantially 3 stages. In particular, the invention relates to a method for synthesis of bis{4-isocyanatocyclohexyl}methane (H 12 MDI) from bis{4-isocyanatophenyl}methane (MDI). More especially, the invention relates to a method for synthesis of H 12 MDI with a trans-trans isomer content of <30%, preferably of <20%, particularly preferably of 5 to 15%.
专利号:US-4267070-A 优先权日:1979-10-30 标题:Catalyst for the synthesis of aromatic monoisocyanates 发明人:NEFEDOV BORIS K; MANOV-JUVENSKY VLADIMIR I; DERGUNOV JURY I; RYSIKHIN ANATOLY I; CHIMISHKIAN ALEXANDR L 权利人:NEFEDOV BORIS K; MANOV JUVENSKY VLADIMIR I; DERGUNOV JURY I; RYSIKHIN ANATOLY I; CHIMISHKIAN ALEXANDR L 摘要:A catalyst for the synthesis of aromatic monoisocyanates comprising 1.64 to 16.6% by weight of palladium chloride, 0.16 to 47.6% by weight of an oxide of a metal of Group VB of the periodic system, 1.5 to 81.8% by weight of an oxide of a metal of Group VI B of the periodic system, 1.64 to 89.8% by weight of pyridine or an alkylsubstituted pyridine. n The use of the catalyst according to the invention in the synthesis of aromatic monoisocyanates makes it possible to obtain a high degree of conversion of the starting compound of up to 100%, a high yield of the desired product of up to 97%, and increased productivity of the catalyst of up to 40 g of the desired product per g of PdCl 2 per hour.
专利号:US-9994508-B2 优先权日:2012-12-11 标 题:Versatile and functionalised intermediates for the synthesis of vitamin D and novel vitamin D derivatives 发明人:LOPEZ PEREZ BORJA; SIGUEIRO PONTE RITA; MAESTRO SAAVEDRA MIGUEL A; MOURINO MOSQUERA ANTONIO 权利人:ENDOTHERM GMBH 摘要:Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.
专利号:US-2007282078-A1 优先权日:2006-06-01 标题:Synthesis of aryl N-acylurea from aryl isocyanates or aryl carbodiimides for use as intermediate in novel sequential self-repetitive reaction (SSRR) to form amides, amide-imides and their polymers 发明人:DAI SHENGHONG A; LIN JIANG-JEN; WEI KUAN-LIANG; WU CHIH-HENG; HUANG WEI-HSIANG 权利人:DAI SHENGHONG A; LIN JIANG-JEN; WEI KUAN-LIANG; WU CHIH-HENG; HUANG WEI-HSIANG 摘要:Disclosed is a process for synthesizing an aryl N-acylurea in both high selectivity and high yield, comprising reacting an aryl carbodiimide with a carboxylic acid under mild conditions. Thermolysis of N-acylureas at above about 120° C. gives amides and isocyanates, and the latter will undergo the repetitive reaction sequences in the presence of a carbodiimide catalyst. Based on this unique model, a sequential self-repetitive reaction (SSRR) is also developed in a versatile manner for converting aryl carbodiimides into amides, polyamides, polyamide-imides and polyamide-imide elastomers.
专利号:WO-9102739-A1 优先权日:1989-08-11 标题:Synthesis of glycosides having predetermined stereochemistry 发明人:DANISHEFSKY SAMUEL J 权利人:UNIV YALE 摘要:Methods of stereoselectively preparing a substituted 1,2-anhydrosugar wherein a substituted glycal is converted into a 1,2-anhydrosugar that is utilized to glycosylate a hydroxyl group containing glycal, are disclosed. Methods of preparing a saccharide multimer wherein a nucleophile is reacted with a substituted 1,2-anhydrosugar having a plurality of non-participating substituents, are disclosed. In addition, methods of preparing stereospecific halo-substituted saccharide multimers by haloglycosylation of a glycosyl donor substituted glycal and a glycosyl acceptor glycal derivative in the absence of water and in the presence of a halonium ion, are disclosed. Methods of preparing stereospecific particle-linked halo-substituted saccharide multimers, by haloglycosylation of a particle-linked nucleophilic hydroxyl group with a substituted glycal and a halonium ion, are also disclosed.