ANTISENSE OLIGONUCLEOTIDE, NUCLEOSIDE AND INTERMEDIATE FOR PRODUCING THE SAME, ITS SYNTHESIS, OLIGONUCLEOTIDE SYNTHESIZING UNIT AND ITS SYNTHESIS

摘要

PROBLEM TO BE SOLVED: To obtain the subject new nucleic acid having nuclease resistance and suppressing manifestation of a gene to cause a disease, containing a deoxyuridine having a carboxylic acid ester, etc., at its 5-position, and an N,N- dimethylaminohexyl-carbamoyl group. ;SOLUTION: This antisense oligonucleotide comprises a nucleoside containing a carboxylic acid ester or an aminohexylcarbamoyl group at its 5-position of deoxyuridine or its derivative and a nucleoside of 5-(N,N-dimethylaminohexyl) carbamoyl-2'-deoxyuridine or its derivative as constituent components. The oligonucleotide shows resistance to hydrolysis with nuclease, forms a complementary bond which is specific to a target mRNA and thermodynamically stable, controls the manifestation of a gene to cause a disease and is useful for treating the disease such as viral infectious disease, a cancer, etc. The nucleoside is obtained by reacting 5-iodo-2'-deoxyuridine with trifluoroethanol and carbon monoxide in the presence of a catalyst.;COPYRIGHT: (C)1997,JPO