Multicore indazolinone library
AssigneeUniversity Court of the University of St Andrews
InventorsNicholas Westwood, Nicholas Isambert
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Abstract
There is provided a method to convert O-functionalized indazolinone-derivatives to the corresponding N2-functionalized indazolinone derivatives, by use of microwave energy or a transition metal catalyst. A preferred catalyst is palladium tetrakis. The method described allows the creation of a library of chemical compounds which can be screened for biological activity.
Claims26
A method of converting an O-functionalised indazolinone-derivative into the corresponding N2-functionalised isomer, the method comprising the step of exposing the O-functionalised indazolinone-derivative to microwave energy or a transition metal catalyst.
(canceled)
A library comprising indazolinone-derivatives comprising compounds of at least one of the following general formulae:
- wherein R1 and R3 are each independently selected from the group consisting of an alkyl, aminoalkyl, acylamino, acyloxy, alkoxycarbonyl, alkoxy, alkylaryl, hydroxyalkyl, thioalkyl, acyl, amino, hydroxy, thio, aryloxy, arylalkoxy, hydrogen, alkynyl, halogen, cyano, sulfhydryl, carbamoyl, nitro, trifluoromethyl, or heterocyclyl group;
- L is a linking group;
- and
- X is a solid support.
A method of constructing a library of isolated compounds comprising the steps of:
- i) exposing an O-functionalised indazolinone-derivative to microwave energy or a transition metal catalyst to form N2-functionalised indazolinone-derivative;
- and
- ii) diversifying said N2-functionalised indazolinone-derivative at selected reactive moieties to generate a library of compounds.
Dependencies are inferred from the claim text.