📜N-(2-乙基苯基)甲酰胺置于[双(三氟乙酰氧基)碘]苯体系中,用 1,2-二氯乙烷 作为反应溶剂,化学反应 0.03H,反应生成 异氰酸2-乙基苯酯 参考文献:Synthesis Of Unsymmetrical Phenylurea Derivatives Via Oxidative Cross Coupling Of Aryl Formamides With Amines Under Metal-Free Conditions 标题:Synthesis Of Unsymmetrical Phenylurea Derivatives Via Oxidative Cross Coupling Of Aryl Formamides With Amines Under Metal-Free Conditions 摘要:通过使用高价碘试剂作为外部氧化剂,在非常好的产率下,将n-芳基甲酰胺直接转化为相应的苯基脲衍生物,通过形成异氰酸酯中间体实现. DOI:10.1039/c4Nj01668H
专利号:US-10801022-B2 优先权日:2015-04-14 标 题:Method for solid-phase synthesis of DNA encoded compound library 发明人:LI JIN; Wan jinqiao; LIU GUANSAI; DOU DENGFENG 权利人:HITGEN LTD; HITGEN INC 摘要:The present invention provides a method of solid-phase synthesis of DNA-encoded compound library. The method includes following steps: a) reacting solid carrier G-1 with linker molecule L-1 to prepare L-G-1; b) reacting DNA with linker molecule L-0 to prepare L-2; c) reacting L-G-1 with L-2 to prepare L-G-2; d) removing protection group of the L-G-2 and obtaining L-G-2-1; e) reacting the L-G-2-1 with synthetic building block and performing DNA encoding; and f) removing the solid carrier and obtaining the DNA-encoded compound library. Compared with the prior art, the present invention can complete post-treatment purification of the reaction only by filtration and irrigation processes for several times. The present invention is simple to operate, can shorten the production cycle of DNA encoded compound library with more than 50%, significantly increases the production efficiency and the unicity as well as the purity of the final products.
专利号:US-4341898-A 优先权日:1981-05-18 标题:Synthesis of isocyanates from nitroalkanes 发明人:MILLIGAN BARTON; PINSCHMIDT JR ROBERT K 权利人:AIR PROD & CHEM 摘要:A process for the preparation of aromatic isocyanates from nitroalkanes. A nitromethyl aromatic compound of the general formula: wherein R and R1 represent hydrogen, halogen, a C1-C5 alkyl radical, a C1-C4 alkoxy radical, nitro, isocyanato, an alkoxycarbonylamino, or nitromethyl radical, with R and R1 being the same or different, is heated in the presence of an effective amount of a Lewis acid or Bronsted acid substance to effect a dehydrogenation-isomerization reaction to yield an aromatic isocyanate of the general formula: The product of the reaction may be recovered as the aromatic isocyanate or the alcohol adduct, a carbamate.
专利号:WO-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 权利人:LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:EP-3284851-B1 优先权日:2015-04-14 标 题 :Method for solid-phase synthesis of dna-encoded chemical library