GR77072

Bicyclic compounds of the general formula (I), wherein Y and Y represent a removable carbonyl protecting group, and Q is a C1-5 alkyl group or a substituted benzyl group, are prepared in such a way that a) a compound of the general formula (V), wherein Y and Y are as defined above and R' is a r...

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Hauptverfasser: DR.P.HUSZTHY, J.NYITRAI, G.SMIG, J.FETTER, DR.L SZPORNY, G.HORNYAK, K. ZAUER, DR.G.DOLESCHALL, K. HARSANYI G. FEKETE, T. GIZUR, KAROLY LEMPERT, G. HAJOS
Format: Patent
Sprache:eng
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Zusammenfassung:Bicyclic compounds of the general formula (I), wherein Y and Y represent a removable carbonyl protecting group, and Q is a C1-5 alkyl group or a substituted benzyl group, are prepared in such a way that a) a compound of the general formula (V), wherein Y and Y are as defined above and R' is a removable amido protecting group other than phenyl group, is activated on the carboxy group and then reacted with a salt of a malonic acid hemiester, wherein the alcohol component is a C1-5 aliphatic alcohol or a substituted benzyl alcohol, the resulting new compound of the general formula (IV), wherein R', Q, Y and Y are as defined above, is reacted with a sulfonic azide in the presence of a tertiary amine, or b) a compound of the general formula (V) is activated on its carboxy group and reacted then with a diazoacetic acid ester, thereafter the R' protecting group of a resulting new compound of the general formula (III> is removed, and the resulting compound of the general formula (II> is subjected to ring closure to form the desired end-product.