摘要 |
For the preparation of anti-depressants such as paroxetine, novel intermediates are optically-enriched compounds of formula (1), wherein Ar is a C6-20 aryl group; and R<1> and R<2> are independently H, alkyl or aryl. These compounds may be prepared by reduction of the corresponding 1,4-dihydropyridine-3-aldehyde, e.g. using hydrogen and a catalyst. The aldehyde may be prepared by hydrolytic cleavage of an aminal obtainable by the reaction of 3-pyridinecarboxaldehyde and a chiral C-2 symmetric diamine, and then stereoselective introduction of the Ar and COCHR<1>R<2> groups.
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申请人 |
CHIROSCIENCE LIMITED;ADGER, BRIAN, MICHAEL;POTTER, GERARD, ANDREW;FOX, MARTIN, EDWARD |
发明人 |
ADGER, BRIAN, MICHAEL;POTTER, GERARD, ANDREW;FOX, MARTIN, EDWARD |