CAS: 147149-98-2; 4-Amino-2-(Trifluoromethyl)Pyridine

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2-氯-6-三氟甲基吡啶置于palladium On Activated Charcoal 二甲基十二/十四烷基叔胺,氢气,双氧水,溶剂黄146体系中,用 乙醇,乙酸甲酯 用作溶剂,化学反应 2.25H,反应生成2-三氟甲基-4-氨基吡啶
参考文献:使用蛋白质晶体结构设计胸苷酸合酶抑制剂:一类新的5-取代的喹唑啉酮的合成和生物学评价.
标题:使用蛋白质晶体结构设计胸苷酸合酶抑制剂:一类新的5-取代的喹唑啉酮的合成和生物学评价.
摘要:描述了新型胸苷酸合酶(ts)抑制剂的设计,合成和生物学评估.通过对蛋白质-配体结构的重复晶体学分析来进行分子设计.在该项目开始时,我们专注于大肠杆菌ts,5'-氟脱氧尿酸(5-Fdump)和经典的含谷氨酸叶酸类似物的高分辨率三元晶体复合物的叶酸辅因子结合位点.一种新型化合物的初步三元晶体结构已成功解决.通过分析该初始复合物,进行了进一步的结构修饰,并开发了一系列活性5-(芳硫基)喹唑啉酮.合成策略基于各种芳基硫代阴离子置换喹唑啉酮5位上的卤素.测试化合物对纯化的大肠杆菌和/或人ts的抑制作用,并在体外测定针对三种肿瘤细胞系的细胞毒性.用几种抑制剂观测到了重要的胸腺嘧啶核苷保护作用,表明ts是细胞内活性位点.
Doi:10.1021/jm00058A010

专利信息

专利号:WO-2025012368-A1
优先权日:2023-07-12
标题:Synthesis of 2-(trifluoromethyl)pyridin-4-amine
发明人：KANDUKURI SANDEEP REDDY; SMITS HELMARS
权利人:SYNGENTA CROP PROTECTION AG
摘要:A process for the preparation of a 2-trifluoromethyl-4-aminopyridine compound of formula (IV) or a salt thereof is provided.

专利号:US-9751851-B2
优先权日:2013-09-20
标 题:Molecules and compositions that inhibit gram negative bacteria and their uses
发明人：BASSLER BONNIE L; SEMMELHACK MARTIN F; DRESCHER KNUT; SIRYAPORN ALBERT; CONRAD-MILLER LAURA C; O'LOUGHLIN COLLEEN T
权利人:UNIV PRINCETON; BASSLER BONNIE L; SEMMELHACK MARTIN F; DRESCHER KNUT; SIRYAPORN ALBERT; MILLER LAURA C; O'LOUGHLIN COLLEEN T
摘要:Antivirulence strategies to combat Pseudomonas aeruginosa , are described. One strategy encompasses synthesis of a series of compounds that inhibit the production of pyocyanin, a redox-active virulence factor produced by this pathogen. A related strategy encompasses synthesis of compounds that inhibit the two P. aeruginosa quorum-sensing receptors, LasR and RhlR, inhibit production of pyocyanin, and inhibit biofilm formation.

专利号:EP-3686190-A1
优先权日:2013-07-11
标 题 :Synthesis of therapeutically active compounds

专利号:US-9815842-B2
优先权日:2014-05-28
标题 :Pyrazolo pyrimidine derivatives and their use as MALT1 inhibitors
发明人：SOLDERMANN CAROLE PISSOT; QUANCARD JEAN; SCHLAPBACH ACHIM; SIMIC OLIVER; TINTELNOT-BLOMLEY MARINA; ZOLLER THOMAS
权利人:SOLDERMANN CAROLE PISSOT; QUANCARD JEAN; SCHLAPBACH ACHIM; SIMIC OLIVER; TINTELNOT-BLOMLEY MARINA; ZOLLER THOMAS; NOVARTIS AG
摘要:The present invention describes new pyrazolo-pyrimidine derivatives which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.

专利号:CN-114773148-A
优先权日:2019-11-13
标题 :Method for the synthesis of 2,3-dichloro-1,1,1-trifluoropropane and 2-chloro-1,1,1-trifluoropropene

专利号:WO-2023134686-A1
优先权日:2022-01-11
标题:Preparation method for 1,3,5-triazine derivative
发明人：HUANG TICONG; WU XIAOLEI; WANG SHANG; ZANG HAISHAN; QIN ZHIDONG; ZHANG HONGYING; CAI YAO; ZHAO RUI; LIU FEI
权利人:CHIA TAI TIANQING PHARMACEUTICAL GROUP CO LTD
摘要:The present invention relates to the field of drug synthesis, particularly, to a preparation method for a 1,3,5-triazine derivative, more particularly, to a preparation method for 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazine-2-amine. The preparation method has the advantages of short route, simple operation, and high yield, and is more suitable for use in industrial production.