| 摘要 |
A compound represented by the general formula (III) which serves as an intermediate of an oligonucleotide analog having stable and excellent antisense or antigene activity or having excellent activity as a detection reagent (probe) for a specific gene or as a primer for the initiation of amplification of a specific gene can be produced at high yields regardless of the type of nucleobase by a method comprising reacting a compound represented by the general formula (II) or a salt thereof with a trimethylsilylated compound obtained from a compound represented by the general formula (IVb), wherein X, Y, Z, A, R, and B are as defined in claim 1. |
| 主权项 |
1. A method of producing a compound of formula (III): or a salt thereof, comprising reacting a compound of formula (IVb): with a trimethylsilylating agent to produce a trimethylsilylated compound; and reacting the trimethylsilylated compound with a compound of formula (II): or a salt thereof, wherein A is an alkylene group having 1 to 4 carbon atoms; B is a purin-9-yl group or a purin-9-yl group having one or more substituents selected from group α; X, Y, and Z are each independently a protective group for the hydroxy group; R is a silyl protective group; R4, R5, and R6 are each independently a hydrogen atom, a hydroxy group, a protected hydroxy group, an alkoxy group having 1 to 4 carbon atoms, a mercapto group, a protected mercapto group, an alkylthio group having 1 to 4 carbon atoms, an amino group, a protected amino group, an amino group substituted by one or more alkyl groups having 1 to 4 carbon atoms, an alkyl group having 1 to 4 carbon atoms, or a halogen atom; and group α is a hydroxy group, a protected hydroxy group, an alkoxy group having 1 to 4 carbon atoms, a mercapto group, a protected mercapto group, an alkylthio group having 1 to 4 carbon atoms, an amino group, a protected amino group, an amino group substituted by one or more alkyl groups having 1 to 4 carbon atoms, an alkyl group having 1 to 4 carbon atoms, and a halogen atom. |
