- Aldehyde-mediated bioconjugation: Via in situ generated ylides
-
A technically simple approach for rapid, high-yielding and site-selective bioconjugation has been developed for both in vitro and cellular applications. This method involves the generation of maleimido-phosphonium ylides via 4-nitrophenol catalysis under physiological conditions followed by their Wittig reactions with aldehyde-appended biomolecules.
- Parmar, Sangeeta,Pawar, Sharad P.,Iyer, Ramkumar,Kalia, Dimpy
-
supporting information
p. 14926 - 14929
(2019/12/24)
-
- Carbonylation of functionalized diamine diols to cyclic ureas: Application to derivatives of DMP 450
-
Synthesis of the cyclic urea core structure of the HIV protease inhibitor DMP 450 has been achieved via W(CO)6/I2-catalyzed carbonylation of diamine intermediates. Carbonylations of related functionalized diamines to derivatives of the DMP 450 core structure were also examined. Selected diamine diol substrates could be converted to the cyclic urea core structure by catalytic carbonylation without protection of the diol functionality.
- Darko, Ampofo K.,Curran, F. Chris,Copin, Chloé,McElwee-White, Lisa
-
experimental part
p. 3976 - 3983
(2011/06/25)
-
- COMPOSITIONS AND METHODS FOR CYCLOFRUCTANS AS SEPARATION AGENTS
-
The present invention relates to derivatized cyclofructan compounds, compositions comprising derivatized cyclofructan compounds, and methods of using compositions comprising derivatized cyclofructan compounds for chromatographic separations of chemical species, including enantiomers. Said compositions may comprise a solid support and/or polymers comprising derivatized cyclofructan compounds.
- -
-
Page/Page column 45-49; 55
(2010/12/31)
-
- Development of new HPLC chiral stationary phases based on native and derivatized cyclofructans
-
An unusual class of chiral selectors, cyclofructans, is introduced for the first time as bonded chiral stationary phases. Compared to native cyclofructans (CFs), which have rather limited capabilities as chiral selectors, aliphatic-and aromatic-functionalized CF6s possess unique and very different enantiomeric selectivities. Indeed, they are shown to separate a very broad range of racemic compounds. In particular, aliphatic-derivatized CF6s with a low substitution degree baseline separate all tested chiral primary amines. It appears that partial derivatization on the CF6 molecule disrupts the molecular internal hydrogen bonding, thereby making the core of the molecule more accessible. In contrast, highly aromaticfunctionalized CF6 stationary phases lose most of the enantioselective capabilities toward primary amines, however they gain broad selectivity for most other types of analytes. This class of stationary phases also demonstrates high "loadability" and therefore has great potential for preparative separations. The variations in enantiomeric selectivity often can be correlated with distinct structural features of the selector. The separations occur predominantly in the presence of organic solvents.
- Sun, Ping,Wang, Chunlei,Breitbach, Zachary S.,Zhang, Ying,Armstrong, Daniel W.
-
experimental part
p. 10215 - 10226
(2010/05/01)
-
- Synthesis of a peptidomimetic HCMV protease inhibitor library
-
The human cytomegalovirus (HCMV) protease catalyzes the maturational process of the herpes virus assembly protein and plays a key role during the manufacture of viral capsid, and so is an attractive target for potential anti-herpes-virus agents with novel structures and new mechanisms. In this work, a peptidomimetic skeleton was designed and a chemical library containing 32 compounds with different substitutions on the skeleton was prepared by the oxidation of a precursor library, which was constructed from four types of building blocks: 4 carboxylic acids, 2 amines, 2 aldehydes and 2 isocyanides, based on multicomponent condensation following liquid phase strategies. The syntheses of the key building block isocyanides are presented.
- Xu, Ping,Lin, Wenwei,Zou, Xiaomin
-
p. 1017 - 1026
(2007/10/03)
-
- Solvent-free synthesis of tartramides under microwave activation
-
The preparation of aliphatic, aromatic or functionalized tartramides directly from tartaric acid and amines under microwave activation is described. The inexpensive, solvent free and fast reaction conditions are the important features of the procedure.
- Massicot,Plantier-Royon,Portella,Saleur,Sudha
-
p. 2441 - 2444
(2007/10/03)
-
