Abstract：Ten 2,5-diketopiperazine derivatives(4a~4j, 4c,4f and 4i were novel compounds) in yield of 54.2～75.7％ were synthesized by Aldol reaction of N,N-diacetyl-2,5-diketopiperazine, arylaldehyde and RX by onepot method, using DMF as the solvent and Cs2CO3 as the alkali. The structures were confirmed by 1H NMR， 13C NMR and ESI-MS. Preliminary biological activities tests indicated that (Z)-1-acetyl-4-allyl-3-(naphthalen-1-ylmethylene)piperazine-2,5-dione(4c) exhibited better cytotoxic activities against U937, Hela and Du145 cell lines.
李晋昇， 廖升荣， 汤勇， 刘永宏. 2,5-二酮哌嗪衍生物的一锅法合成及其细胞毒活性[J]. 合成化学, 2015, 23(12): 1095-1099.
LI Jin-sheng, LIAO Sheng-rong, TANG Yong, LIU Yong-hong. Synthesis and Cytotoxic Activities of 2,5-Diketopiperazine Derivatives by One-pot Method. Chinese Journal of Synthetic Chemistry, 2015, 23(12): 1095-1099.