2-溴-4-氟苯甲醛置于水,氧气,Sodium Hydroxide体系中,50.0 °C,101.33 Kpa 条件下,反应 10.0H,以78%的收率获得2-溴-4-氟苯甲酸 参考文献:可回收的ag / C 3 N 4催化剂催化醛的好氧氧化为羧酸 标题:可回收的ag / C 3 N 4催化剂催化醛的好氧氧化为羧酸 摘要:醛的氧化是合成羧酸的有效方法.在此,我们希望报告一种简单,有效且可回收的方案,该方案通过在温和的条件下使用c 3 N 4负载的银纳米颗粒(ag / C 3 N 4)作为催化剂将醛有氧氧化为羧酸.在标准条件下,可以以非常好至优异的收率获得相应的羧酸.此外,Ag / C3N4便于回收,可以重复使用三次,收率令人满意. Doi:10.2174/1570178617999200807210137
专利号:US-11465970-B2 优先权日:2017-12-14 标题 :Method for synthesis of Roxadustat and intermediate compounds thereof 发明人:XU YONGXIANG 权利人:NANJING CAVENDISH BIO ENGINEERING TECH CO LTD; XU YONGXIANG; NANJING CAVENDISH BIO ENG TECH CO LTD 摘要:The present application provides a method for synthesis of Roxadustat. A compound as represented by formula (VIII) is used as a raw material, and is reacted with phenol, a vinyl-containing ether, an acid, hydroxylamine, and then the product is reacted with glycine. In addition, the present application also provides intermediate compounds as represented by formula (IX), formula (XI), formula (XII), formula (IV), and formula (V) for synthesis of Roxadustat. Herein, details of the substituents involved in formula (VIII), formula (IX), formula (XI), and formula (XII) are stated in the description
专利号:US-8106031-B2 优先权日:2006-05-02 标题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-7968752-B2 优先权日:2003-06-16 标 题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-2022073513-A1 优先权日:2018-12-29 标题:1h-pyrrolo[2,3-b]pyridine derivatives and related compounds as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases 发明人:CHEN YI 权利人:NEWAVE PHARMACEUTICAL INC 摘要:The present invention relates to compounds of Formula (II) and more preferably to 1H-pyrrolo[2,3-b]pyridine derivatives of formula (III) and related compounds. The variables are defined in the claims. The compounds are BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis of exemplary compounds as well as pharmacological data thereof (pages 61 to 72; examples 1 to 4; tables). An exemplary compound is e.g. 4-(4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl]piperazin-1-yl)-2-[methyl(1H-pyrrolo[2,3-b]pyridin-5-yl)phosphoroso]-N-[3-nitro-4-[(oxan-4-yl methyl)amino]benzenesulfonyl]benzamide (example 1).
专利号:WO-2020248279-A1 优先权日:2019-06-14 标 题 :Continuous synthesis method for substituted benzoate organic matter 发明人:HONG HAO; LU JIANGPING; ZHANG ENXUAN; LIU ZHIQING; LI CHAO 权利人:JINLIN ASYMCHEM LABORATORIES CO LTD 摘要:The present invention provides a continuous synthesis method for a substituted benzoate organic matter. The continuous synthesis method comprises: in the presence of a catalyst and an organic solvent, continuously feeding an organic matter as represented by formula (I) and oxygen into a continuous reaction device for continuous oxidation reaction to obtain a substituted benzoate organic matter, and performing continuous discharge, wherein the substituted benzoate organic matter has a structure as represented by formula (II). Oxygen is a green reagent, and is cheap and easy to obtain; the present invention would not produce a large amount of waste gas, waste water, and waste residues after the completion of reaction, and the system is easy to handle. The use of continuous reaction operation can reduce the risk of solvent flash evaporation explosion due to high concentration oxygen in batch reactions. Under the same oxidation conditions, the use of a continuous preparation process can reduce the escape of oxygen, greatly increase the utilization of oxygen, simplify the operation, and improve the reaction safety and the yield of substituted benzoate organic matters.
专利号:US-2024400552-A1 优先权日:2016-11-11 标题 :Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
[参考文献]: Bernd Drner, Et Al. Radiosynthesis And In Vivo Evaluation Of 1-[参考文献]: Christian Wolf, Et Al. Regioselective Copper-Catalyzed Amination Of Bromobenzoic Acids Using Aliphatic And Aromatic Amines. J Org Chem. 2006 Apr 14;71(8):3270-3.
合成参考文献
摘要:Sanford, M. S.; Cook, A., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 204.