CAS: 115551-33-2; 6-Amino-2,3-Difluorophenol

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82419-26-9 163734-01-8 53981-25-2

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CAS号82419-26-9 2,3-二氟-6-硝基苯酚 | CAS号868735-81-3 1-(苄氧基)-2,3-二氟-4-硝基苯 | CAS号144298-04-4 N-(3,4-二氟苯基)氨基甲酸叔丁酯 | CAS号82419-35-0 氟嗪羧酸 | CAS号82419-36-1 氧氟沙星 | CAS号100986-86-5 R-9-氟-2,3-二氢-3-...

📜2,3-二氟-6-硝基苯酚置于palladium On Carbon,氢气体系中,用 乙醇 用作溶剂,20.0 °C,100.0 Kpa 条件下,反应 7.0H,以95%的收率获得6-氨基-2,3-二氟苯酚
参考文献:氟喹啉恶嗪衍生物作为细菌拓扑异构酶ia抑制剂的合成,评估和comfa研究
标题:氟喹啉恶嗪衍生物作为细菌拓扑异构酶ia抑制剂的合成,评估和comfa研究
摘要:迫切需要具有新颖靶标和作用机理的新型抗菌剂,以解决有问题的细菌感染和增加抗生素耐药性.拓扑异构酶ia代表了一个有吸引力的且尚未开发的抗菌靶标,因此,人们越来越有兴趣开发用于抗菌治疗的选择性和有效的拓扑异构酶i抑制剂.根据我们的初步生物学筛选,发现氟喹啉吩恶嗪1是一种针对大肠杆菌的低微摩尔抑制剂.拓扑异构酶ia.在文献中,研发了氟喹啉吩恶嗪类似物作为抗菌剂和抗癌剂,但是,它们对拓扑异构酶i的抑制作用尚未得到充分开发,并且几乎没有可用的结构活性关系(sar).非常好的1对拓扑异构酶i抑制活性和sar的缺乏促使我们设计和合成了一系列氟喹吩恶嗪类似物,以系统地评估sar,并探查了氟喹吩恶嗪核心对拓扑异构酶i酶靶识别的结构元素.在这项研究中,设计,合成和评估了一系列氟喹啉吩恶嗪类似物,作为拓扑异构酶i抑制剂和抗菌剂.基于靶标的测定表明,氟喹啉恶嗪衍生物具有9-Nh2和/或6-取代的胺官能团通常表现
Doi:10.1016/j.Ejmech.2016.09.053

专利信息

专利号:US-5521310-A
优先权日:1992-10-07
标 题 :Process to obtain benzoxazines to be used for the synthesis of ofloxazine, levofloxazine and derivatives
发明人：CARRETERO GONZALVEZ JUAN-CARLO; VICIOSO SANCHEZ MERCEDES; GARCIA RUANO JOSE-LUIS
权利人:ETILO DERIVADOS
摘要:A process to obtain benzoxazines useful for the synthesis of Ofloxazine, Levofloxazine and derivatives. The benzoxacines (I) where Xb is an halogen and R 1 is H, alkyl or alkenyl of up to 6 atoms of C or aryl, can be obtained by means of cycling a compound of formula (II) through the reaction with triphenylphosphine and ethyl azodicarboxilate. The compounds of formula (II) can be obtained through the reaction of a compound (III) with an adequate epoxide. Through the use of the adequate chiral epoxide it is possible to obtain the enantiomerically desired intermediate and, therefore and selectively, it is possible to obtain the desired final product with the adequate enantiomeric form without the need to carry out a resolution stage. n The Compounds (I) are useful and key intermediates for the synthesis of the antimicrobials Oflixazine and Levofloxazine. ##STR1##

专利号:ES-2069500-B1
优先权日:1992-10-07
标题 :IMPROVEMENTS INTRODUCED IN THE PURPOSE OF THE SPANISH PATENT N 9201983 FOR 'PROCEDURE TO OBTAIN USEFUL BENZOXAZINES FOR THE SYNTHESIS OF OFLEXACINE, LEVOFLOXACIN AND DERIVATIVES.

专利号:WO-9407873-A1
优先权日:1992-10-07
标题 :Process for obtaining benzoxazines useful for the synthesis of ofloxacin, levofloxacin and derivatives thereof

专利号:AU-674542-B2
优先权日:1992-10-07
标题 :Process for obtaining benzoxazines useful for the synthesis of ofloxacin, levofloxacin and derivatives thereof

专利号:EP-0619311-A1
优先权日:1992-10-07
标题 :Process for obtaining benzoxazines useful for the synthesis of ofloxacin, levofloxacin and derivatives thereof

专利号:CA-2125287-A1
优先权日:1992-10-07
标 题 :Process to obtain benzoxazines to be used for the synthesis of ofloxazine, levofloxazine and derivatives