1,4-Oxaselenin derivatives, the method thereof and antitumor agents containing them

摘要

PURPOSE: 1,4-oxaselenine derivatives, a preparation method thereof and an anticancer agent containing the same as an active ingredient are provided, thereby the compound can be useful for treatment and prevention of various cancers including uterine cancer and ovarian cancer. CONSTITUTION: The 1,4-oxaselenine derivatives is represented by the following formula(1), wherein Ar is phenyl, 4-methoxyphenyl and 4-chlorophenyl. The method for preparing the 1,4-oxaselenine derivatives comprises the steps of: (i) adding phenyl acetylene(1), butyllithium and selenium into THF to produce lithium phenylethaneselenoate(2), adding 2-bromoacetophenone(3) into the lithium phenylethaneselenoate(2), and reacting them at -78 deg. C to produce 3-selena-4-pentyne-1-on derivatives(4a-4c); and (ii) reacting 3-selena-4-pentyne-1-on derivatives with AgNO3 and LDA to produce 1,4-oxaselenine derivatives.