The beta-D-enantiomer of FDOC (2',3'-dideoxy-5-fluoro-oxacytidine) exhibits potent anti-HIV-1 activity. It was obtained in optically pure form by employing a tandem kinetic resolution/chiral salt crystallization protocol. In addition, conditions were developed that allowed the unwanted butyrate ester of the L-enantiomer of FDOC to be racemized. This material could then be recycled in future res...

To evaluate and quantify Irinotecan (R-enantiomer) / related compound D in hydrochloride trihydrate API, a high stereo-specific liquid chromatography technique was developed validated. The partition accomplished on ChiralpakIC-3 (150 x 4.6 mm 3µm) through mobile fragment comprising 0.1 % v/v Formic acid water acetonitrile with 1mL/min, 250C, 20µL, 50C 370 nmas flow rate, column temparture, inje...

The enantioselective local disposition of semotiadil (R-enantiomer) and levosemotiadil (S-enantiomer) in rat liver was investigated in the single-pass perfusion system containing 1% bovine serum albumin (BSA). After an instantaneous injection of semotiadil, levosemotiadil, or Evans Blue (a marker of BSA), each outflow time profile from the liver was analyzed by a two-compartment dispersion mode...

The enantiomer separation by supercritical fl uid chromatography (SFC) of six profen drugs was investigated on the new generation of chiral columns from Daicel Corporation, that are packed with the immobilized polysaccharide-derived chiral stationary phases CHIRALPAK IA, CHIRALPAK IB, CHIRALPAK IC, and CHIRALPAK ID. Methanol, ethanol, 2-propanol and acetonitrile were used in combination with tr...

preparation of polymeric materials containing recognition sites of predetermined specificity. The resulting polymers retain a memoryfor the print molecule and can be used in the HPLCmodefor separation of structurally similar substances, and (in case of single enantiomer imprinting) resolution of the enantiomers of the print species10). Polymerisation of monomers, which are selected for their ab...

Drugs that target mitotic spindle proteins have been proven useful for tackling tumor growth. Eg5, a kinesin-5 family member, represents a potential target, since its inhibition leads to prolonged mitotic arrest through the activation of the mitotic checkpoint and apoptotic cell death. Monastrol, a specific dihydropyrimidine inhibitor of Eg5, shows stereo-specificity, since predominantly the (S...

Citalopram is marketed as a racemate (50:50) mixture of the S(+)-enantiomer and R(-)-enantiomer and the active S(+)-enantiomer (escitalopram) that possess inhibitory effects. Citalopram was introduced in Sweden in 1992 and is the most frequently used antidepressant to date in Sweden. In 2002, escitalopram was introduced onto the Swedish market for treatment of depression and anxiety disorders. ...

We address the purification of target enantiomer a chiral compound from its racemic mixture, through simulated moving bed (SMB) chromatography either as standalone or combined with recycle and racemization undesired enantiomer. carry out comparative assessment two processes focus on role kinetics, effect selectivity stationary phase, upstream symmetric synthesis racemate. The analysis is genera...

Axially chiral 5-methyl-2-(o-aryl)imino-3-(o-aryl)-thiazolidine-4-ones have been subjected to aldol reactions with benzaldehyde to produce secondary carbinols which have been found to be separable by HPLC on a chiral stationary phase. Based on the reaction done on a single enantiomer resolved via a chromatographic separation from a racemic mixture of 5-methyl-2-(α-naphthyl)imino-3-(α-naphthyl)-...

Production of optically pure products can be based on simple unselective synthesis of racemic mixtures combined with a subsequent separation of the enantiomers. However, this approach suffers from a 50% yield limitation which can be overcome by racemization of the undesired enantiomer and recycling. Application of biocatalyst for the racemization steps offers an attractive option for high-yield...