2-DEOXY-3-ETHYNYL-BETA-D-RIBOFURANOSYL DERIVATIVE

摘要

PROBLEM TO BE SOLVED: To provide the subject new nucleic acid derivative consisting of a specific 2-deoxy-3-ethynyl-β-D-ribofuranosyl derivative, exhibiting extremely strong cytocidal activity and excellent antitumor activity and useful as an antitumor agent, etc. SOLUTION: This derivative is a new 2-deoxy-3-ethynyl-β-D-ribofuranosyl derivative expressed by the formula I (B is a nucleic acid base which may have substituent) and its ester easily decomposable in vivo or its pharmacologically permissible salt. The derivative has excellent antitumor activity and is useful as an antitumor agent, etc. The compound can be produced by reacting a compound of the formula II (R1 and R2 are each a trialkylsilyl) with an acylating agent in a solvent in the presence of a basic catalyst, desilylating the obtained acylated product, reacting the resultant compound of the formula III (Acyl is an acyl) with a tributyltin halide in the presence of azoisobutyronitrile to eliminate the 2-OH group and deacylating the product.