[EN] MACROCYCLIC INHIBITORS OF PEPTIDYLARGININE DEIMINASES<br/>[FR] INHIBITEURS MACROCYCLIQUES DE PEPTIDYLARGININE DÉIMINASES
申请人:GILEAD SCIENCES INC
公开号:WO2021222353A1
公开(公告)日:2021-11-04
The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.
Mild partial deoxygenation of esters catalyzed by an oxazolinylborate-coordinated rhodium silylene
作者:Songchen Xu、Jeffery S. Boschen、Abhranil Biswas、Takeshi Kobayashi、Marek Pruski、Theresa L. Windus、Aaron D. Sadow
DOI:10.1039/c5dt02844b
日期:——
of organic carbonyl compounds with silanes to give hydrosilylation products or deoxygenation products. The pathway to these reactions is primarily influenced by the degree of substitution of the organosilane. Reactions with primary silanes give deoxygenation of esters to ethers, amides to amines, and ketones and aldehydes to hydrocarbons, whereas tertiary silanes react to give 1,2-hydrosilylation of
亲电,配位不饱和的铑配合物的硼酸联恶唑啉,恶唑啉配位亚甲硅烷基,和N-杂环卡宾供体支持[κ 3 -N,硅,C-值PhB(OX ME2)(OX ME2 SiHPh)进出口的Mes }铑(H)CO] [HB(C 6 F 5)3 ](2,Ox ME2 = 4,4-二甲基-2-恶唑啉; Im Mes = 1-mesitylimidazole)由中性铑甲硅烷基PhB(Ox ME2)2 Im Mes } RhH(SiH 2 Ph)CO(1)和B(C 6 F 5)3。在这种不寻常的恶唑啉配位亚甲硅烷基结构2是由一个未观察异构体的阳离子铑亚甲硅基物种的重排提议形式[值PhB(OX ME2)2林的Mes } RhH的(SiHPh)CO] [HB(C 6 ˚F 5)3 ]由H抽象生成。复杂2催化有机羰基化合物与硅烷的还原反应,生成氢化硅烷化产物或脱氧产物。这些反应的途径主要受有机硅烷取代度的影响。与伯硅
GLYCOSIDASE INHIBITORS AND METHODS OF SYNTHESIZING SAME
申请人:Pinto M. Brian
公开号:US20070244184A1
公开(公告)日:2007-10-18
The compounds of the present invention relate to chain-extended and chain-modified analogues of salacinol, including embodiments where the sulfate moiety has been substituted with a carboxylate or phosphate moiety. In other embodiments the sulfate moiety has been shifted by one carbon atom in the zwitterionic structure. In another embodiment the polyhydroxylated side chain may be replaced with a lipophilic alkyl chain and a suitable counterion. The invention also encompasses methods for synthesizing the salacinol analogues and using the analogues for enzyme inhibition applications.
A Triruthenium Carbonyl Cluster Bearing a Bridging Acenaphthylene Ligand: An Efficient Catalyst for Reduction of Esters, Carboxylic Acids, and Amides by Trialkylsilanes
An efficient reduction of carboxylic acids, esters, and amides with trialkylsilanes is accomplished using a triruthenium carbonyl cluster bearing a bridging acenaphthylene ligand, (mu(3),eta(2):eta(3):eta(5)-acenaphthylene)Ru(3)(CO)(7), as the catalyst. Preactivation of the catalyst by hydrosilanes accelerates the reactions. Sterically small trialkylsilanes are effective in these reactions. Reduction
This invention relates to the direct grafting of a calixarene mostly onto the surface of a material, as well as to a grafting process, and certain calixarene intermediates useful for carrying the grafting process.