929200-21-5Relevant articles and documents
PREPARATION OF CLOPIDOGREL AND ITS ANALOGUES METHYL TETRAHYDROTHIENOPYRIDINE ACETATE COMPOUNDS
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Page/Page column 26, (2008/12/06)
The present invention disclosed a preparation method of Clopidogrel (X=2-Cl) and its analogues of methyl tetrahydrothienopyridine acetate (I) by using halogen phenyl acetonitrile (VIII) as starting material and tetrahydrothienopyridine acetonitrile (IV), tetrahydrothienopyridine acetate (V) as key intermediates, and further using kinetic resolution to prepare the optical active Clopidogrel and compounds of methyl tetrahydrothenopridine acetate of formula (XII). The Clopidogrel of present invention is a novel high effective and safety drug for inhibition of platelet aggregation. This invention applied systematic technique of racemization of unwanted optical active enantiomer, recover recycle and reuse of resolution agent etc., with greater economic advantages and suitable for commercial scale industrial production. Wherein: X represents atoms of hydrogen, fluorine, chlorine, bromine or iodine, M represents an alkali metal ion.
METHOD OF OBTAINING CLOPIDOGREL
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Page/Page column 10, (2008/06/13)
Separation of the camphorsulfonic salts of the compounds of formula (I) and (II) by one or more crystallizations from a mixture of two solvents, both R(-)-10-camphorsulfonic acid and its salts with the compounds of formula (I) and (II) being well soluble in at least one of the components, the formula of which can be indicated as RaOH, wherein Ra is a straight or branched C1 to C5 alkyl. In the other components, camphorsulfonic acid and its salts are less soluble; however, they dissolve compounds of formula (I) and (II) very well.