ANTISENSOLIGODEOXYRIBONUCLEOTIDE AND HIV ACTIVITY INHIBITOR CONTAINING THE SAME NUCLEOTIDE AS ACTIVE INGREDIENT

摘要

NEW MATERIAL:An oligodeoxyribonucleotide expressed by the formula [P(S) is S atom bonded through a double bond to P atom of internucleotide part; P(O) is O atom bonded through a double bond to P atom of internucleotide part]. USE:A HIV activity inhibitor useful as a treating agent of AIDS. PREPARATION:An alcohol expressed by the formula [R1 is C(CX3)3, CH(CX3)2 (X is halogen), etc.] is reacted with a compound expressed by the formula R2OPCl2 (R2 is 1-6C alkyl) to afford a new phosphite compound expressed by the formula (R1O)2P(OR2). Then, a nucleotide unit having a base suitable for target sequence is introduced into a solid phase carrier on which nucleotide is fixed to carry out condensation reaction. Then, capping of unreacted 5'-OH and solid phase carrier is carried out using the above-mentioned phosphite compound as a capping agent. The reaction is successively repeated to synthesize the objective sequence having a base sequence and then sulfur oxidation and final deprotection are carried out.