CAS: 403-24-7; 2-Fluoro-4-Nitrobenzoic Acid

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CAS号1427-07-2 2-氟-4-硝基甲苯 | CAS号34667-88-4 2-氟-4-硝基苯腈 | CAS号392-09-6 2-氟-4-硝基苯甲酸甲酯 | CAS号446-31-1 4-氨基-2-氟苯甲酸 | CAS号210416-38-9 4-[(4-carboxy-3... | CAS号660432-43-9 2-氟-4-硝基苄醇 | CAS号73792-06-0 4-氨基-2-氟苯甲酸乙酯 | CAS号73792-08-2 4-氨基2-氟苯甲酸甲酯 | CAS号53312-80-4 2-氟-4-氨基苯腈 | CAS号157665-46-8 2-氟-4-硝基苯甲酸叔丁酯 | CAS号140373-77-9 4-氨基-2-氟苯甲酸叔丁酯

2-氟-4-硝基甲苯置于potassium Permanganate,四丁基氯化铵体系中,用 水,叔丁醇 作为反应溶剂,化学反应 8.0H,反应生成 2-氟-4-硝基苯甲酸
参考文献:探索四氢异喹啉硫代乙内酰脲支架可阻断雄激素受体作为有效的抗前列腺癌药物
标题:探索四氢异喹啉硫代乙内酰脲支架可阻断雄激素受体作为有效的抗前列腺癌药物
摘要:前列腺癌(pc)是全球范围内与癌症相关的男性死亡的主要原因,因此不断需要鉴定新的和改良的有效抗pc分子.基于enzalutamide结构和我们的前期工作合理设计了新颖的四氢异喹啉硫代乙内酰脲支架,从而发现了一系列新的抗增殖化合物.与恩杂鲁胺相比,几种新的类似物显示出改善的雄激素受体(ar)拮抗活性,同时保持了对lncap细胞(富含ar)相对于du145细胞(ar缺乏)更高的选择性毒性.实际上,化合物55通过削弱ar不清楚的易位性而显示出有希望的体外抗肿瘤活性.更重要的是55与我们的前期工作中报道的化合物1相比,具有更好的药代动力学特性.这些结果证明了向新的和改进的ar拮抗剂的开发迈出的一步.
DOI:10.1016/j.Ejmech.2017.10.031

专利信息

专利号:WO-2020248278-A1
优先权日:2019-06-14
标题:Method for continuous synthesis of substituted benzoic-acid organic substance
发明人：HONG HAO; ZHANG ENXUAN; LU JIANGPING; LIU ZHIQING; LI CHAO; TANG YANG
权利人:JINLIN ASYMCHEM LABORATORIES CO LTD
摘要:The present invention provides a method for the continuous synthesis of a substituted benzoic-acid organic substance. The continuous synthesis method comprises: in the presence of catalyst and organic solvent, the organic matter represented by formula (I) and oxygen are continuously inputted to a continuous reaction apparatus for continuous oxidation reaction to obtain a substituted benzoic-acid organic substance, which is discharged continuously, the substituted benzoic-acid organic substance having the structure represented by formula (II). Oxygen is a green reagent and is inexpensive and readily available; a large amount of wastewater, waste gas, and solid waste is not generated after the reaction, and the system is easy to handle. The use of a continuous reaction operation can reduce the risk of flash distillation and explosion of solvent due to a high concentration of oxygen in a batch reaction. Under the same oxidation conditions, the continuous preparation process can reduce the escape of oxygen, greatly increasing the oxygen utilization rate and also simplifying the operation, improving the safety of the reaction and the yield of the substituted benzoic-acid organic substance.

专利号:WO-2013056547-A1
优先权日:2011-10-22
标题 :Synthesis of a group of hydantoin derivatives and use thereof
发明人：CHEN DEGUI
权利人:CHEN DEGUI
摘要:Provided in the present invention are the pharmaceutical composition, synthesis procedure and medicinal use of a group of HYDANTOIN derivatives. Since these compounds have an inhibiting effect on an androgen receptor, the compounds can be used to treat prostate cancer and other diseases and physiological disorders related to androgen receptor activity.

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:US-2025129050-A1
优先权日:2022-01-26
标 题 :Synthesis of a kif18a inhibitor
发明人：CAILLE SEBASTIEN; GREENE DANIEL GERARD; CORBETT MICHAEL THOMAS; WEI CAROLYN
权利人:AMGEN INC
摘要:The present invention relates to improved preparation of a KIF18A inhibitor having the chemical structure Compound (1), or a salt thereof Compound (la); wherein HA is as defined herein; and key intermediates thereof, i.e., Compound (2a), Compound (3a), Compound (5) or a salt thereof, and Compound (6a) or a hydrate thereof, of the formulae: Compound (2a); Compound (3a); Compound (5) or a salt thereof; and Compound (6a) or a hydrate thereof, preferably Compound (6a-1). The present invention further relates to solid form of Compound (6a), preferably the crystalline hydrate form of Compound (6a-1).

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-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.