METHODS OF PREPARATION OF DEHYDRO-DIKETOPIPERAZINES IN LIQUID PHASE OR OF SOLID SUPPORTED PHASE

摘要

The preparation of any compound of the generic structure (I); wherein: R<1> and R<2> are substituents described in the main text. Cycl- is a group represented by either of the formulae (a) and (b); wherein: R<3> to R<8>, X and Y are substituents described in the main text. The above described compounds may be used for the treatment of cancer. The preparation method consists of coupling of the amine group of phosphynilglycinate with the carboxylic group of an aminoacid, the successively coupling of the above formed compound with the formyl-Cycl derivative, the deprotection of the aminoacid and the formation of dehydro-diketopiperazine employing mild alkaline conditions. The method is extended for the preparation of individual derivatives or libraries of derivatives related to the above described compounds of the general formula (II), employing a solid supported phosphonate of the general formula (II), wherein: Res represents any polymer support (resin) with or without a linker, Prot represents any NH- protective group, R represents alkyl or alkyloxyalkyl groups.