专利号:US-2017190670-A1 优先权日:2014-07-11 标题:Improved process for the preparation of enzalutamide 发明人:HIRPARA SANJAY; SHRAWAT VIMAL KUMAR; POTHURAJU RAJU; TRIPATHI CHANDRESH KUMAR; AKSHAYKANT CHATURVEDI 权利人:SHILPA MEDICARE LTD 摘要:The present application relates to an improved process for preparation of Enzalutamide (I). n n n n n n n n n n The present application also relates to an improved process for the preparation of substantially pure Enzalutamide (I) having purity of greater than 99.5%. n The present application also relates to a novel process for the preparation of Enzalutamide intermediate useful in the industrially viable synthesis of Enzalutamide.
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:WO-2025024697-A1 优先权日:2023-07-27 标 题:Intermediates for synthesizing exatecan mesylate 发明人:GOEDDEL DAVID; WALKER JAMES; WRIGHT AUSTIN; REDFERN LOUIS 权利人:SIGMA ALDRICH CO LLC 摘要:Intermediates useful in the preparation of exatecan mesylate and related compounds. Further provided are methods for preparing these compounds. Also provided is an improved, scalable synthesis of exatecan mesylate using the provided intermediates. The synthesis of exatecan mesylate utilizes a convergent approach, involving fewer steps and utilizing fewer reagents and increasing efficiency.
专利号:US-6743811-B2 优先权日:1999-07-28 标 题:Oxazalidinone compounds and methods of preparation and use thereof 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; GADWOOD ROBERT C 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.
专利号:US-12162815-B2 优先权日:2018-07-09 标 题 :Crystalline 2-fluoro-3-nitrotoluene and process for the preparation thereof 发明人:BRASOLA ELENA; DI SILVESTRO MARCO 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A; AMGEN INC 摘要:The present invention refers to a crystalline 2-fluoro-3-nitrotoluene compound of formula (I), and a process for the preparation thereof. Furthermore, the present invention relates to a process for the synthesis of a compound of formula (II) or salts thereof by means of the crystalline 2-fluoro-3-nitrotoluene.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
摘要:McMurtrey, K. B.; Sanford, M. S., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 562. 摘要:Wang, X.; Hu, J., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2.