[Et<sub>3</sub>NH][HSO<sub>4</sub>]-catalyzed eco-friendly and expeditious synthesis of thiazolidine and oxazolidine derivatives
作者:Ali Mohammed Malla、Mehtab Parveen、Faheem Ahmad、Shaista Azaz、Mahboob Alam
DOI:10.1039/c4ra15590d
日期:——
reports a facile and green approach for the synthesis of thiazolidine/oxazolidine derivatives 4(a–u) in excellent yields (92–98%) with high purity. The protocol involves a one-pot three-componentreaction of substituted 1,3-diketones 1(a–g), cyanates 2(a–c) and ethylchloroacetate (3) in ionicliquid [Et3NH][HSO4] under solvent-free conditions. The notable feature of this pathway is that the ionic liquid
Four ammonium and imidazolium ionic liquids (ILs) have been synthesized and screened against the T98G cell line (brain cancer) and HEK normal cells. Treatment induced metabolic cell death (MTT), growth inhibition, clonogenic inhibition were studied as cellular response parameters. Treatment with ILs enhanced growth inhibition and cell death in a concentration dependent manner in both the T98G and HEK cell lines. At higher concentrations (>0.09 mg/mL) the cytotoxic effects of the ILs were highly significant. An inhibitory effect on clonogenic capacity was also observed after cell treatment. Amongst all ILs; IL 4 (BMIMCl) exhibited potent activity against T98G brain cancer cells. Despite potent in-vitro activity, all ILs exhibited less cytotoxicity against the normal human HEK cells at all effective concentrations.
[EN] SUBSTITUTED PIXYL PROTECTING GROUPS FOR OLIGONUCLEOTIDE SYNTHESIS<br/>[FR] GROUPES SUBSTITUES DE PROTECTION DE PIXYLE DESTINES A UNE SYNTHESE D'OLIGONUCLEOTIDES
申请人:ISIS PHARMACEUTICALS INC
公开号:WO2005077966A1
公开(公告)日:2005-08-25
The present invention describes an improved hydroxyl protecting group of formula (1), wherein R2 and R7 are specified substituents and Q is O, S, NR10 or N(C=O)R10.
The invention encompasses a process for purifying a peptide comprising loading a peptide onto a RP-HPLC column; washing the column with an aqueous solution of a pharmaceutically acceptable counterion salt; and eluting the peptide from the column with a solvent mixture of a organic solvent and an acid of the pharmaceutically acceptable counterion, wherein the aqueous solution has a pH of at least about 6.
Compounds of formula (I), salts thereof, and compositions and uses thereof are described. The compounds are useful as V1a vasopressin agonists, for the treatment of, e.g., complications of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites.