| 摘要 |
he preparation of any compound of the following generic structure: (chemical formula) wherein: R1 and R2 are substituents described in the main text. Cycl- is a group represented by either of the following formulae: (chemical formulas) wherein: R3 to R8, X and Y are substituents described in the main text. The dashed bond represents a bond selected from the group consisting of consequetive carbon-carbon double bond. The above described compounds may be used for the treatment of cancer. The preparation method consists of coupling of the amine group of phosphinyl glycine ester with the carboxylic group of an aminoacid, and the successively coupling of the above formed compound with the formyl-Cycl derivative. Finally the deprotection of theaminoacid and the formation of dehydro-diketopiperazine employing mild alkaline conditions. The method is extended for the preparation of individual derivatives or libraries of dehydro-diketopiperazines described from the general formula I, employing a solid supported phosphonate of the general formula (chemical formula) wherein: Res, Prot and R is described in the main text. |
