糠酸(呋喃甲酸)置于硫酸,肼体系中,用 甲醇 用作溶剂,化学反应生成2-呋喃甲酰肼 参考文献:Synthesis,Characterization,And Nonlinear Optical Properties Of Some New Series Ofs-(5-Aryl-1,3,4-Oxadiazol-2-yl) 2-Chloroethanethioate Derivatives 标题:Synthesis,Characterization,And Nonlinear Optical Properties Of Some New Series Ofs-(5-Aryl-1,3,4-Oxadiazol-2-yl) 2-Chloroethanethioate Derivatives 摘要:在本研究中,合成了一些新型 S-(5-芳基-1,3,4-噁二唑-2-基)2-氯乙酸硫酯(3A-3E)衍生物,并研究了它们对光学性质的影响.它们还通过元素分析和多种光谱方法进行表征,包括ftir,$^{1}$h NMR,$^{13}$c NMR 和 Uv-Vis 技术.通过z扫描方法,在532 Nm波长下使用连续波激光二极管测量了3A-3E在二氯甲烷中的非线性折射指数.化合物的非线性折射系数获得了 ${10}^{11}\,\,{m}^2{/w}$ 级别.考虑到这些化合物的适当非线性,它们可以被视为生物光学和光子应用的非常好候选者.所有合成的化合物(3A-3E)也被评估了其抗菌和抗真菌活性.生物活性测定显示,与作为对照药物的恩诺沙星和两性霉素相比,合成化合物对测试的细菌大肠杆菌和真菌曲霉菌展示了不同程度的抑制区. Doi:10.3906/kim-1811-54
专利号:WO-2012127472-A1 优先权日:2011-03-22 标题:Process and intermediates for the preparation of preladenant and related compounds 发明人:MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI 权利人:MAPI PHARMA LTD; MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI 摘要:The present invention describes processes for the synthesis of 2-(furan-2-yl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]piperazin-l-yl] ethyl]-7H-pyrazolo[ 4,3-e ][1,2,4]- triazolo[1,5c] pyrimidin-5-amine (Preladenant) represented by the structure of formula (1 ), and solvates and salts thereof, especially salts with pharmaceutically acceptable acids. The process of the present invention is useful not only for Preladenant production, but also for the preparation of other biologically active compounds of general formula (17), such as A2a receptor antagonists used for the treatment of central nervous system diseases, among others. The present invention further relates to certain intermediates formed in such processes.
专利号:US-2023407352-A1 优先权日:2020-10-30 标题:Method for the Production of Thiocarbamate Derivatives A2AR Inhibitors 发明人:JIAO XUECHENG; DELIGNY MICHAEL; CROSIGNANI STEFANO; JIANG XIANGJUN 权利人:iTeos Belgium SA 摘要:The present disclosure relates to synthesis of enantiomerically rich key drug intermediates as a means for manufacturing of thiocarbamate derivatives as A2A adenosine receptor (A2AR) inhibitors. More particularly, the present disclosure provides a viable efficient technology using enzymatic biotransformation process which utilizes cheaper substrate for production of high value key intermediates for A2AR inhibitors.
专利号:US-4713383-A 优先权日:1984-10-01 标 题:Triazoloquinazoline compounds, and their methods of preparation, pharmaceutical compositions, and uses 发明人:FRANCIS JOHN E; GELOTTE KARL O 权利人:CIBA GEIGY CORP 摘要:[1,2,4]triazolo[1,5-c]quinazoline compounds of the formula wherein R1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R2 is hydrogen or lower alkyl; X is oxygen or NR3, R3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N-R3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N-R3.
专利号:WO-2023191400-A1 优先权日:2022-04-01 标题:Ethyl piperidine triazolo triazine derivatives, synthesis method therefor, and pharmaceutical composition containing same for prevention or treatment of cancer 发明人:JI SEUNGHEE; BYUN JOONSEOK; KIM JIWON; KIM DOYOUNG; KIM SEOHYUN; LEE JONGHYUN; JUNG SEUNGHEE; CHOI JONGRYOUL; KO DONG-HYUN; KIM DONGKYU; SON SEO HYUN; KANG JI YOON; JANG HYU JEONG; AHN SANG YEOP; KIM JI YONG; LEE SEO JIN 权利人:HK INNO N CORP; FUTURE MEDICINE CO LTD 摘要:The present invention relates to an ethyl piperidine triazolo triazine derivative, a synthesis method therefor, and a pharmaceutical composition including same for the prevention or treatment of cancer. Acting as an antagonist on an adenosine A2A receptor (A2AR), the derivative can exhibit efficacy for the prevention or treatment of various A2AR-related diseases, specifically, various cancers. When used in combination therapy with an immune checkpoint inhibitor, the derivative is expected to exhibit a remarkable synergistic effect in terms of anticancer activity.
专利号:US-2024335420-A1 优先权日:2021-08-02 标题:N-acylhydrazone compounds capable of inhibiting nav 1.7 and/or nav 1.8, processes for the preparation thereof, compositions, uses, methods for treatment using same and kits 发明人:BARREIRO GABRIELA; SANT'ANA DANILO PEREIRA DE; GAMBA LUIS EDUARDO REINA; FRAGA CARLOS ALBERTO MANSSOUR; BARREIRO ELIEZER JESUS DE LACERDA; LIMA LÃ?DIA MOREIRA 权利人:EUROFARMA LABORATORIOS S A; UNIV FEDERAL DO RIO DE JANEIRO UFRJ 摘要:N-Acylhydrazone compounds that are Nav 1.7 and/or Nav 1.8 inhibitors, including N-acylhydrazone compounds of Formula (I), wherein substituents R1 to R4 are independently selected from the groups defined in the specification, as well as to the processes for the preparation thereof, compositions comprising at least one of these compounds, uses, treatment methods for treating or preventing pain-related pathologies, and kits, useful in the fields of medicinal chemistry, organic synthesis, as well as in the treatment of pain-related disorders.
专利号:FR-2628428-A1 优先权日:1988-03-09 标题:PROCESS FOR THE PREPARATION OF TRANSITION METAL COMPLEXES USEFUL AS RADIOPHARMACEUTICAL PRODUCTS OR FOR THE SYNTHESIS OF NEW RADIOPHARMACEUTICAL PRODUCTS
[参考文献]: M Lever, Et Al. Optimal Conditions For 4-Hydroxybenzoyl- And 2-Furoylhydrazine As Reagents For The Determination Of Carbohydrates, Including Ketosamines. Anal Biochem. 1984 May 15;139(1):205-11.
合成参考文献
参考文献:10.1107/s1600536811008932 摘要:Xu J, Yue XY. (E)-4-{[2-(2-Furylcarbon-yl)hydrazinyl-idene]meth-yl}-2-meth-oxy-phenyl acetate. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o880. 参考文献:10.1107/s1600536811017260 摘要:Ngan NK, Wong RCS, Lo KM, Ng SW. Aqua[N′-(3-ethoxy-2-oxidobenzyl-κO)furan-1-carbohydrazidato-κ2N′,O]dioxidomolybdenum(VI)–4,4′-bipyridine (2/1). Acta Crystallogr E Struct Rep Online. 2011 May 14;67(6):m748. doi: 10.1107/s1600536811017260.