COMPOSÉ DE TYPE DÉHYDROPHÉNYLAHISTINE SUBSTITUÉ PAR DU DEUTÉRIUM, SON PROCÉDÉ DE PRÉPARATION ET UTILISATION DANS LA PRÉPARATION D'UN MÉDICAMENT ANTITUMORAL
Marine Biomedical Research Institute of Qingdao Co. Ltd.
发明人:
申请号：
EP16802509.6
公开号：
EP3312163A4
申请日:
2016.05.27
申请国别(地区):
EP
年份:
2019
代理人:
摘要：
Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehyd- rophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound.
