COMPOUND LIBRARY PREPARATION PROCESS

摘要

The present invention relates to the preparation of a compound library comprising the following steps:
i. Having available at least two different compounds each comprising at least a dioxaborolane or dioxaborinane ring. In said compounds:
the boron of the dioxaborolane or dioxaborinane ring is directly linked to a carbon atom of a hydrocarbon radical;at least one carbon atom of the dioxaborolane or dioxaborinane ring is monosubstituted, the other carbon atoms of the dioxaborolane or dioxaborinane ring being non-substituted or monosubstituted;in at least two compounds, the hydrocarbon radicals linked to the boron are different;in at least two compounds, the substituents carried by at least one of the carbon atoms of the dioxaborolane or dioxaborinane rings are different and/or the size of the boronic ester ring is different;ii. Reacting the compounds of step (i.) and forming, by a boronic ester metathesis reaction, the library comprising at least four different compounds.

The present invention also relates to a compound library.

主权项

1. A process, comprising the preparation of a compound library, wherein the library is prepared by a process comprising the following steps:
i. Having available at least two different compounds each comprising at least a dioxaborolane or dioxaborinane ring, forming a boronic ester function. In said compounds:
the boron of the dioxaborolane or dioxaborinane ring is directly linked to a carbon atom of a hydrocarbon radical;at least one carbon atom of the dioxaborolane or dioxaborinane ring is monosubstituted, the other carbon atoms of the dioxaborolane or dioxaborinane ring being non-substituted or monosubstituted;in at least two compounds, the hydrocarbon radicals linked to the boron are different;in at least two compounds, the substituents carried by at least one of the carbon atoms of the dioxaborolane or dioxaborinane rings are different and/or the size of the boronic ester ring is different; ii. Reacting the compounds of step (i.) and forming, by a boronic ester metathesis reaction, the library comprising at least four different compounds, each having at least one substituents of a dioxaborolane or dioxaborinane ring different and/or a boronic ester ring of a different size compared to another compound.