CAS: 3034-48-8; 2-Bromo-5-Nitrothiazole

上下游产品

CAS号121-66-4 2-氨基-5-硝基噻唑 | CAS号71-41-0 正戊醇 | CAS号96-50-4 2-氨基噻唑 | CAS号21166-17-6 2-Anilino-5-nit... | CAS号3034-49-9 2(3H)-Thiazolon... | CAS号61-57-4 尼立达唑 | CAS号133311-51-0 2-溴-5-苯基噻唑 | CAS号14527-46-9 5-硝基噻唑 | CAS号960-34-9 4-氨基-N-(5-硝基-2-... | CAS号61962-58-1 4-[(5-nitro-1,3... | CAS号39259-57-9 2-(1-methylimid... | CAS号40045-50-9 SU3327 | CAS号53316-72-6 Acetamide,N-[4-...

2-氨基-5-硝基噻唑置于氢溴酸,Sodium Nitrite体系中,化学反应 4.0H,以65%的收率获得2-溴-5-硝基噻唑
参考文献:旋转酶atpase结构域作为抗结核药物的发现平台:硝噻唑基羧酰胺类似物的基于结构的设计和铅优化
标题:旋转酶atpase结构域作为抗结核药物的发现平台:硝噻唑基羧酰胺类似物的基于结构的设计和铅优化
摘要:在这项研究中,我们探索了药物开发不足的分枝杆菌促旋酶atpase(gyrb)域,以此为模板对我们内部(bits Pilani)化合物进行结构化虚拟筛选,以发现针对结核分枝杆菌(m.Tb.)的新抑制剂.通过结合分子对接和药物化学策略,进一步确定鉴定出的命中基因,以获得优化的类似物,该类似物表现出相当高的体外酶功效和针对m.Tb的杀菌特性.高37Rv株.通过差示扫描荧光法实验重新确定了配体对gyrb结构域的结合亲和力.进一步评估herg毒性(先前报道的n-连接的氨基哌啶类似物的主要限制)表明,这些分子完全没有心脏毒性,这是该类别中的一项重大成就.
Doi:10.1002/cmdc.201402035

专利信息

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.

专利号:US-6323366-B1
优先权日:1997-07-29
标 题:Arylamine synthesis
发明人：WOLFE JOHN P; AHMAN JENS; SADIGHI JOSEPH P; SINGER ROBERT A; BUCHWALD STEPHEN L
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present invention provides a method for the preparation of a wide range of primary arylamines. The arylamines are prepared in two efficient, straightforward transformations: 1) an activated aryl group and an imine group are combined, in the presence of a transition metal catalyst, under conditions wherein the transition metal catalyst catalyzes the formation of a carbon-nitrogen bond between the activated carbon of the arene and the imine nitrogen; and 2) the resulting N-aryl imine is transformed, via any of a number of standard protocols, to the primary arylamine. The method of the invention may also be exploited in the preparation of vinylamines.

专利号:US-6562844-B2
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.

专利号:US-7002020-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
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.

专利号:RU-2049782-C1
优先权日:1989-04-24
标 题:Thiazole derivatives, method of their synthesis, method of struggle against fungi