INTERMEDIATE FOR THE PREPARATION OF IODOURACIL DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF

摘要

An intermediate for the preparation of iodouracil derivatives is provided to improve preparation yield of iodouracil derivatives with increased in vivo stability against thymidine phorphorylase, so that the iodouracil derivatives are useful for confirming expression of HSV1-tk gene in gene therapy. An intermediate for the preparation of iodouracil derivatives represented by the formula(10), wherein R^1 is C1-C6 alkyl or C1-C6 alkoxy; and R^2 is hydrogen, methyl or methoxy, is prepared by reacting compounds represented by the formula(6) with compounds represented by the formula(7a) in tetrahydrofuran-dimethylsulfoxide(THF-DMSO) in the presence of tetrakis(triphenylphosphine)palladium(0).