lodocyclization of unsaturated tosylamides promoted by Oxone® oxidation of KI afforded, in good yields, N-tosyl iodopyrrolidines and piperidines. A new, simple method for the conversion of alcohols to tosylamides is presented.
通过 Oxone® 氧化 KI 促进的不饱和甲苯磺酰胺的碘环化以良好的收率提供了 N-甲苯磺酰基碘吡咯烷和哌啶。介绍了一种将醇转化为甲苯磺酰胺的简单新方法。
Enzyme-Triggered Enantioconvergent Transformation of Haloalkyl Epoxides
作者:Sandra F. Mayer、Andreas Steinreiber、Romano V. A. Orru、Kurt Faber
rac-trans-haloalkyl epoxides 1a−8a using the epoxide hydrolase activity of whole bacterial cells furnished the corresponding vicinal diols 1b−8b as intermediates; these (spontaneously) underwent ring closure to yield cyclic products 1c−6c through an enzyme-triggered cascade reaction. In particular, cis-configured substrates (1a, 3a, 5a, 7a) were transformed in an enantioconvergent fashion, which resulted
使用整个细菌细胞的环氧水解酶活性对 2,3-二取代外消旋-顺-和外消旋-反-卤代烷基环氧化物 1a-8a 进行生物催化水解,得到相应的邻位二醇 1b-8b 作为中间体;这些(自发地)经历闭环以通过酶触发的级联反应产生环状产物 1c-6c。特别是,顺式构型的底物(1a、3a、5a、7a)以对映收敛方式转化,导致从外消旋体中形成 100% des 和高达 92% ees 的单一立体异构产物。
Transition Metal-Catalyzed Intramolecular Cyclization of 1,5- and 1,6-Dienes via Direct Cleavage and Addition of the Carbon–Hydrogen Bond
Ruthenium- and rhodium-catalyzed intramolecular C–H/olefin coupling reactions of 1-(2-pyridyl)-, 1-(2-imidazolyl)-, and 1-(2-oxazolyl)-1,5-dienes proceeded in a regiospecific manner to give 5-membe...
Ultrasonic formation and reactions of sodium phenylselenide
作者:Steven V. Ley、lan A. O'Neil、Caroline M.R. Low
DOI:10.1016/s0040-4020(01)82086-x
日期:1986.1
Treatment of diphenyldiselenide with sodium metal in tetrahydrofuran under ultrasonic conditions conveniently gave a suspension of sodium phenylselenide which could be transferred by syringe or cannula and reacted with sulphonates, halides and epoxides.
[EN] IMPROVED CATIONIC LIPIDS AND METHODS FOR THE DELIVERY OF THERAPEUTIC AGENTS<br/>[FR] LIPIDES CATIONIQUES ET PROCÉDÉS AMÉLIORÉS POUR L'ADMINISTRATION D'AGENTS THÉRAPEUTIQUES
申请人:PROTIVA BIOTHERAPEUTICS INC
公开号:WO2011000106A1
公开(公告)日:2011-01-06
The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.