专利号:US-6258323-B1 优先权日:1998-11-16 标题:Apparatus and method used in multiple, simultaneous synthesis of general compounds 发明人:HORMANN ROBERT EUGENE; GILBERT DARYL EUGENE; SIOMA EDWARD MICHAEL 权利人:ROHM & HAAS 摘要:The apparatus and method of the present invention provides for conducting simultaneous multiple synthesis of general compounds, which often takes place under varied uneven conditions requiring heating, cooling, agitation, reagent/solvent additions to the reactor contents at each reaction vessel location, supply and maintenance of inert atmosphere and means to facilitate the reflux of the reactor contents. Thus, it becomes necessary to monitor and control the reaction conditions during the simultaneous multiple synthesis of general compounds. The apparatus allows the user to connect various independently controlling and conveying means to each reaction vessel through multiple ports provided on a stopper mounted on each reaction vessel. The apparatus of the present invention permits user to readily access the reaction vessels without interrupting the reactions occurring in the adjacent reaction vessels. The unique geometry and shape of the stopper allows positioning of multiple ports, while still providing the stopper with a compact size. As a result, a large array of reaction vessels can be accommodated in the device of the present invention without significantly increasing the overall size of the apparatus. Some of the general compounds that can be readily synthesized by the apparatus and the method of the present invention include inorganic compounds as well as organic compounds, such as oligomers, polymers, agricultural chemicals, drugs, peptides and oligonucleotides.
专利号:WO-2024133619-A1 优先权日:2022-12-23 标 题 :New process for the manufacture of mdm2-p53 antagonists 发明人:SHAO JIDONG; XIAO QING; Zhang Dihan; ZHU ZHIBIN 权利人:BOEHRINGER INGELHEIM INT 摘要:This invention relates to a novel process for the synthesis of substituted aniline of formula (1) or salts thereof via hydroxy-indolinone of formula (13). The process of this invention is palladium free and uses oxygen as green and save oxidant for the copper promoted ring- opening of a hydroxy-indolinone bicycle to a tetra substituted aniline.
专利号:WO-2022222272-A1 优先权日:2021-04-19 标 题 :Synthesis process of 2-methyl-3-methoxybenzoic acid 发明人:GENG JINGKUN; Fang Zheneng; YAO LINXI; JI PINJUN; ZHANG YANCHAO; MIAO JUNHUI; WANG BOTAO 权利人:JIANGSU YONGAN CHEMICAL CO LTD 摘要:Disclosed is a synthesis process of 2-methyl-3-methoxybenzoic acid. The synthesis process comprises the following steps: (1) a reductive hydrogenation reaction, involving: using 2-methyl-3-nitrobenzoic acid or methyl 2-methyl-3-nitrobenzoate as a raw material, methanol as a solvent, hydrogen as a hydrogen source and palladium on carbon or platinum on carbon as a catalyst to prepare 3-amino-2-methylbenzoic acid or methyl 3-amino-2-methylbenzoate by means of hydrogenation reduction; (2) a one-pot reaction of diazotization, hydrolysis and esterification, involving: using the reduction product as a raw material and methanol as a solvent to prepare methyl 3-hydroxy-2-methylbenzoate by means of diazotization, hydrolysis and esterification reactions under the action of a diazotization reagent; (3) a methylation reaction, involving: using methyl 3-hydroxy-2-methylbenzoate as a raw material and dimethyl sulfate as a methylation reagent to prepare methyl 3-methoxy-2-methylbenzoate by means of a methylation reaction in the presence of an alkali; and (4) a hydrolysis reaction, involving: mixing methyl 3-methoxy-2-methylbenzoate with an alkali and water, and heating same for hydrolysis, cooling same after the reaction is completed, adjusting the pH to 1-3 with an acid to precipitate a product, followed by filtering and drying same to obtain 3-methoxy-2-methylbenzoic acid.
专利号:US-5846993-A 优先权日:1992-12-22 标题:HIV protease inhibitors 发明人:DRESSMAN BRUCE A; FRITZ JAMES E; KALDOR STEPHEN W; KALISH VINCENT J; REICH SIEGFRIED HEINZ; TATLOCK JOHN H; RODRIGUEZ MICHAEL J 权利人:AGOURON PHARMA 摘要:HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
专利号:US-6271235-B1 优先权日:1992-12-22 标题:HIV protease inhibitors 发明人:DRESSMAN BRUCE A; FRITZ JAMES E; KALDOR STEPHEN W; KALISH VINCENT J; REICH SIEGFRIED HEINZ; RODRIGUEZ MICHAEL J; SHEPHERD TIMOTHY A; TATLOCK JOHN H; JUNGHEIM LOUIS NICKOLAUS 权利人:AGOURON PHARMA 摘要:HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
专利号:CN-113511968-A 优先权日:2021-04-19 标 题 :A kind of synthesis technique of 2-methyl-3-methoxybenzoic acid
参考文献:10.1055/s-0035-1560181 摘要:Lützen A, Jarzebski A, Bannwarth C, Tenten C, Benkhäuser C, Schnakenburg G, Grimme S. Synthesis, Chiral Resolution, and Absolute Configuration of Functionalized Tröger’s Base Derivatives: Part III. Synthesis. 2015 Aug 28;47(20):3118–32. doi: 10.1055/s-0035-1560181.