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Direct separation of clopidogrel enantiomers by reverse-phase planar chromatography method using β-cyclodextrin as a chiral mobile phase additive

Antic D., Filipic S, Ivkovic B., Nikolic K, Agbaba D.

Acta Chromatographica

2011

Vol. 23, no. 2

235--245

A simple and rapid TLC method using β-cyclodextrin as a chiral mobile phase additive (CMPA) was developed for direct separation of S-clopidogrel and its impurity R-clopidogrel. The influence of different factors (stationary phases, organic modifiers, chiral selectors and their concentrations in the mobile phase, and optimal saturation time of the chamber) on enantioseparation was studied. The best resolution of clopidogrel enantiomers was achieved on Polygram®cel 300 Ac-10% plates using isopropanol-0.5 mM β-cyclodextrin (6:4, υ/υ) as mobile phase in TLC chamber previously equilibrated with the mobile phase for 20 min. The spots were detected under UV light and using iodine vapours. The method enables rapid separation of clopidogrel enantiomers and can be successfully used in control of stereoselective synthesis of clopidogrel and in control of its purity. Finally, the molecular modelling of the inclusion complexes between the analytes and α-, β-, and γ-cyclodextrin was performed to investigate the mechanism of the enantiorecognition.

Technologia wytwarzania wodorosiarczanu (+)-klopidogrelu

Balicki R.

Przemysł Chemiczny

2006

T. 85, nr 5

342-343

Opisano technologię wytwarzania wodorosiarczanu (+)-klopidogrelu opracowaną w Instytucie Farmaceutycznym. Podano też dane ogólne jego aktywności biologicznej i zastosowania w lecznictwie.

α-Amino-(2-chlorophenyl)acetic acid prepd. in 90% yield by boiling 2-chlorobenzaldehyde with NaCN and (NH4)2CO3 for 16 h was esterified with thionyl chloride in MeOH to yield Me α-amino-(2-chlorophenyl)acetate which was converted into the amine in 73%. The ester was alkylated with 2-(2-thienylethanol) tosylate to yield the aminoester in 60%. This was cyclized with paraformaldehyde to yield, via crystn of the hydrochloride, high-purity Me α-(4,5,6,7-tetrahydrothieno[3,2-b]pyrid-5-yl)-(2-chlorophenyl)acetate in 75% yield. The resulting racemate was sepd. by the use of (-)-camphorsulfonic acid to prep. 99% pure enantiomer and the (+)-camphorsulphonate was converted into the optically active base which was treated with H2SO4 to give clopidogrel hydrosulfate.