IMIDAZOLE DERIVATIVES, PROCESS FOR PRODUCTION THEREOF, AND USE THEREOF

摘要

Disclosed are imidazole derivatives represented by formula [I]: wherein R is a hydrogen atom or wherein R<2> is a hydrogen atom or a hydroxy protecting group, R<2> protecting either a single hydroxy or two hydroxies together when R<2> is a hydroxy protecting group, and R<3> is a hydrogen atom or OR<2>; A is CONH2 or CN; and R<1> is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl. Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position. Furthermore, the compounds have remarkable antitumor activities and therefore can provide novel antitumor agents.