Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof
申请人:Merck & Co., Inc.
公开号:US06642237B1
公开(公告)日:2003-11-04
&ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.
Novel and facile synthesis of β-(4-azuleno[1,2-b]thienyl)- and β-(4-azuleno[2,1-b]thienyl)-α,β-unsaturated ketones by intramolecular tropylium ion-mediated furan ring-opening reaction
The novel and efficient methods for the synthesis of β-(4-azuleno[1,2-b]thienyl)-α,β-unsaturatedketones (1) and β-(4-azuleno[2,1-b]thienyl)-α,β-unsaturatedketones (2) have been described. Refluxing the dichloromethane solutions of 2-tropylio-3-(2-furyl)thiophene tetrafluoroborates (3) or 3-tropylio-2-(2-furyl)thiophene tetrafluoroborates (4) afforded (1) and (2), respectively, in moderate yields
合成β-(4-azuleno [1,2- b ]噻吩基)-α,β-不饱和酮(1)和β-(4-azuleno [2,1- b ]噻吩基)的新颖有效方法已经描述了-α,β-不饱和酮(2)。回流2-对甲苯基-3-(2-呋喃基)噻吩四氟硼酸酯(3)或3-对甲苯基-2-(2-呋喃基)噻吩四氟硼酸酯(4)的二氯甲烷溶液,分别得到(1)和(2)。中等产量。该反应涉及分子内的yl离子介导的呋喃开环反应。
Synthesis of Unsymmetrical 3,6-Disubstituted Pyridazines. A Palladium-Catalyzed Approach from 3-Iodopyridazines
作者:Tandy L. Draper、Thomas R. Bailey
DOI:10.1021/jo00108a049
日期:1995.2
A versatile and efficient method for the synthesis of benz[a]azulenic enones starting from readily available o-(2-furyl)cycloheptatrienylbenzenes
A facile, one-pot synthesis of β-(benz[a]azulen-10-yl)-α,β-unsaturatedketones from the corresponding o-(2-furyl)cycloheptatrienylbenzenes is reported. A mechanism involving a novel ring-opening cyclisation reaction by the intramolecular attack of the tropylium ion to the 2-position of the furan ring is proposed.
据报道,由相应的邻-(2-呋喃基)环庚三烯基苯可方便地一锅合成β-(苯并[ a ] azulen-10-基)-α,β-不饱和酮。提出了一种涉及新的开环环化反应的机理,该环化反应是由对苯二甲基离子的分子内攻击呋喃环的2位引起的。
An efficient novel synthesis of β-(azuleno[1,2-b]benzothienyl)- and β-(azuleno[2,1-b]benzothienyl)-α,β-unsaturated ketones by the tropylium ion-mediated intramolecular furan ring-opening reaction and X-ray investigation of methyl ketone derivative1
Intramolecular reaction of 2-tropylio-3-(5-substituted 2-furyl)benzothiophenes (3), prepared from the corresponding 2-cycloheptatrienyl-3-(5-substituted 2-furyl)benzothiophenes (2), afforded the beta-(azuleno[1,2-b]benzothienyl)-alpha,beta-unsaturated ketones (4), which are otherwise difficult to obtain, in moderate yields. The reaction involves a ring-opening process of the furan ring by intramolecular