The Mechanism of Gold(I)-Catalyzed Hydroalkoxylation of Alkynes: An Extensive Experimental Study
作者:Alexander Zhdanko、Martin E. Maier
DOI:10.1002/chem.201303795
日期:2014.2.10
An extensiveexperimentalstudy of the mechanism of gold(I)‐catalyzed hydroalkoxylation of internal alkynes has been conducted by using NMR spectroscopy. This study was focused on the organogold intermediates, observations of actual catalytic intermediates in situ, and the reaction kinetics that are involved in this reaction. Based on the experimental results, a complete mechanistic picture was established
heterolytic cleavage of 4′-DNA radical 1 and the regioselective attack of nucleophiles at the intermediate DNA radicalcation 3, the chemistry of model radical 8 was studied. It turned out that the heterolytic cleavage in water is favored over homolysis because of the effective solvation of the ions 9 and 10. The regioselectivity of the nucleophilic attack at radicalcation 10 can be explained with the
Macrocyclic Ghrelin Receptor Antagonists and Inverse Agonists and Methods of Using the Same
申请人:Hoveyda Hamid R.
公开号:US20110105389A1
公开(公告)日:2011-05-05
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (GRLN, growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, obesity and obesity-associated disorders, appetite or eating disorders, addictive disorders, cardiovascular disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders, central nervous system disorders and inflammatory disorders.
[EN] PROCESS OF PREPARING (1R, 4R, 5S)-4-(2-CHLOROETHYL)-1-((S)-((S)-CYCLOHEX-2-EN-1-YL)(HYDROXY)METHYL)-5-METHYL-6-OXA-2-AZABICYCLO[3.2.0]HEPTANE-3,7-DIONE(SALINOSPORAMIDE A; MARIZOMIB)<br/>[FR] PROCÉDÉ DE PRÉPARATION DE (1R, 4R, 5S)-4-(2-CHLOROÉTHYL)-1-((S)-((S)-CYCLOHEX-2-EN-1-YL)(HYDROXY) MÉTHYL)-5-MÉTHYL-6-OXA-2-AZABICYCLO[3.2.0]HEPTANE-3,7-DIONE(SALINOSPORAMIDE A ; MARIZOMIB)
申请人:CELGENE INT II SARL
公开号:WO2021076629A1
公开(公告)日:2021-04-22
The present invention is directed to a process for the synthesis of (1R, 4R, 5S)-4-(2- chloroethyl)-1-((S)-((S)-cyclohex-2-en-1-yl)(hydroxy)methyl)-5-methyl-6-oxa-2- azabicyclo[3.2.0]heptane-3,7-dione; compound 1 (salinosporamide A, marizomib): (Compound 1).
Continuous process for the preparation of random conjugated diene/vinyl arene copolymers
申请人:Polimeri Europa S.p.A.
公开号:EP1829906A1
公开(公告)日:2007-09-05
Continuous process carried out in the presence of at least two reactors in series, for the preparation of statistical vinyl arene/conjugated diene copolymers, the vinyl arene content ranging from 15 to 50% by weight, by means of the copolymerization under isothermal conditions in a hydrocarbon solvent, at a temperature ranging from 30 to 120°C, of vinyl arene/conjugated diene monomers, in the presence of at least one initiator and a 2-methoxy ethyl tetra-hydrofuran (THFA-ethyl) modifier.