📜4-溴苯胺置于盐酸,Sodium Nitrite,Tin(II) Chloride Dihdyrate体系中,用 水 作为反应溶剂,化学反应 2.33H,反应生成 4-溴苯肼盐酸盐 参考文献:Synthesis,Crystal Structure And Fungicidal Activities Of New Type Oxazolidinone-Based Strobilurin Analogues 标题:Synthesis,Crystal Structure And Fungicidal Activities Of New Type Oxazolidinone-Based Strobilurin Analogues 摘要:一系列基于噁唑烷酮的斯特罗比尔素类类似物通过3-(2-溴甲基苯基)噁唑烷-2-酮与1-取代苯基-2H-吡唑-3-酮的反应有效合成.它们的结构通过^1H-NMR,^13C-NMR,元素分析和质谱进行确认和表征.此外,目标化合物3-(2-((1-苯基-2H-吡唑-3-基氧)甲基)苯基)噁唑烷-2-酮的晶体结构通过单晶x射线衍射法确定.这些化合物的生物测定结果表明,某些含有n-取代苯基2H-吡唑环的噁唑烷-2-酮衍生物对灰色稻斑病菌(m. Grisea)在1 G.l^-1的剂量下表现出潜在的体内杀真菌活性. DOI:10.5012/bkcs.2010.31.11.3341
专利信息
专利号:US-11040938-B2 优先权日:2016-07-27 标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts 发明人:MA BING; PAN SHUAI 权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH 摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:US-2025115551-A1 优先权日:2023-10-03 标 题:Synthesis of ras inhibitors 发明人:LI YI; MENDOZA BENJAMIN; NAGANATHAN SRIRAM; WANG ROSS; YI YI; BALLMER STEVEN G; DAVIDSON JAMES; HUANG XIAOJUN 权利人:REVOLUTION MEDICINES INC 摘要:The present invention relates to Ras inhibitors, intermediates in the synthesis thereto, and methods for preparing the Ras inhibitors and the intermediates.
专利号:US-2022356182-A1 优先权日:2009-03-27 标题 :Inhibitors of hepatitis c virus replication 发明人:COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-7442802-B2 优先权日:2002-06-27 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-11053243-B2 优先权日:2009-03-27 标 题:Inhibitors of hepatitis C virus replication 发明人:COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOIL RICHARD; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-9090661-B2 优先权日:2009-03-27 标 题:Inhibitors of hepatitis C virus replication 发明人:COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
参考标题:Tert- Butyl Iodide Mediated Reductive Fischer Indolization Of Conjugated Hydrazones 作者:Yuta Ito,Masafumi Ueda,Norihiko Takeda,Okiko Miyata |发布日期:2016.2.18 摘要:Available N‐aryl Conjugated Hydrazones With Tert‐butyl Iodide Has Been Developed. In This Reaction, Tert‐butyl Iodide Is Used As Anhydrous Hi Source, And The Generated Hi Acts As A Brønsted Acid And A Reducing Agent. This Operationally Simple Method Allows Access To Various Indole Derivatives. Furthermore, The Procedure Can Be Applied To The Synthesis Of Biologically Active Compounds.
合成参考文献
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 46. 摘要:Krishnamoorthy, R., Science of Synthesis Knowledge Updates, (2013) 1, 464.