📜Sodium 4-Fluorocinnamate置于草酰氯体系中,用 甲苯 用作溶剂,化学反应 1.5H,以90%的收率获得对氟肉桂酰氯 参考文献:Acrylamide Derivatives As Antiallergic Agents. I. Synthesis And Structure-Activity Relationships Of N-((4-Substituted 1-Piperazinyl)Alkyl)-3-(Aryl And Heteroaryl)Acrylamides. 标题:Acrylamide Derivatives As Antiallergic Agents. I. Synthesis And Structure-Activity Relationships Of N-((4-Substituted 1-Piperazinyl)Alkyl)-3-(Aryl And Heteroaryl)Acrylamides. 摘要:一系列新的丙烯酰胺衍生物(7-10)被合成.对这些化合物的抗过敏活性进行了评估,并考察了它们的结构-活性关系.化合物10D,即n[4-(4-二苯甲基-1-哌嗪基)丁基]3-(3-吡啶基)丙烯酰胺,在口服给药的大鼠被动皮肤过敏反应(pca)测试中显示出与酮替芬相当或更优越的抗过敏活性.与酮替芬不同,10D在体外对5-脂氧合酶的抑制活性比咖啡酸更强,而其体外抗组胺活性则弱于酮替芬.此外,它对大鼠肥大细胞释放组胺的抑制活性约为色甘酸二钠(dscg)的三分之二.化合物10D是一种有前途的多种过敏性疾病治疗药物. Doi:10.1248/cpb.37.100
专利号:US-4876280-A 优先权日:1988-03-10 标题 :Arylcyclohexane and arylcyclohexene analogs of mevalonolactone derivatives and their use 发明人:DAMON II ROBERT E 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein R1 is hydrogen, C1-3alkyl, n-butyl, i-butyl or t-butyl, R2 is hydrogen or C1-3alkyl, R3 is hydrogen or C1-3alkyl, R4 is hydrogen, C1-3alkyl, n-butyl, i-butyl or t-butyl, R5 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, fluoro, chloro, trifluoromethyl, phenoxy or benzyloxy, R6 is hydrogen, C1-3alkyl, C1-3alkoxy, fluoro, chloro, trifluoromethyl, phenoxy or benzyloxy, with the provisos that not more than one of R5 and R6 is trifluoromethyl, not more than one of R5 and R6 is phenoxy, and not more than one of R5 and R6 is benzyloxy, or R5 and R6 are attached to adjacent carbon atoms and taken together form a radical of the formula -CH=CH-CH=CH-, R6a is hydrogen, C1-2alkyl, fluoro or chloro, X is -CH2CH2- or wherein R7 is hydrogen or C1-3alkyl, and R8 is hydrogen, R9 or M, wherein R9 is a physiologically acceptable ester group, and M is a pharmaceutically acceptable cation, and the broken line represents a double ( pi ) bond or two hydrogen atoms (one on each carbon atom), the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:WO-2013144295-A1 优先权日:2012-03-30 标题 :Synthesis of 2-(3,4-difluorophenyl)cyclopropanamine derivatives and salts
参考标题:Discovery And Synthesis Of Novel Wogonin Derivatives With Potent Antitumor Activity In Vitro 作者:Jubo Wang,Raoling Ge,Xiaqiu Qiu,Xi Xu,Libin Wei,Zhiyu Li,Jinlei Bian |发布日期:2017.11 摘要:Effective Strategy To Obtain Novel Bioactive Compounds. Recently, Our Group Have Constructed A Wogonin-Scaffold Library With Substituents Diversity And Successfully Obtained A Series Of Potent Compounds. Herein, We Reported The Synthesis Of These Compounds And Evaluated The In Vitro Antitumor Activity Against A Panel Of Human Tumor Cell Lines. Most Of Them Showed Good Activity With A Broad Spectrum And
合成参考文献
摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2013) 2, 292.