Patent ID: 7884202
Filing Date: 2011-02-08
Classification: C07D

Abstract:
1. A process for producing a nucleobase having a perfluoroalkyl group, the process comprising: carrying out a reaction of a compound represented by the general formula (3): wherein R 2 is a hydrogen atom, an optionally substituted C1-C6 alkyl group or a protecting group for nitrogen, R 3 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, a protecting group for nitrogen, or a pentose residue, and R 4 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted C1-C4 alkoxy group, an optionally substituted amino group, a carboxy group, an optionally substituted carbamoyl group, or an optionally substituted C2-C5 alkoxycarbonyl group; a compound represented by the general formula (4): wherein R 5 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, a protecting group for nitrogen, or a pentose residue, R 6 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted amino group, a carboxy group, an optionally substituted carbamoyl group, or an optionally substituted C2-C5 alkoxycarbonyl group, and each of R 7 and R 8 is a hydrogen atom or a protecting group for nitrogen; a compound represented by the general formula (5): wherein R 9 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, a protecting group for nitrogen, or a pentose residue, R 10 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted amino group, a carboxy group, an optionally substituted carbamoyl group, or an optionally substituted C2-C05 alkoxycarbonyl group, and each of R 11 and R 12 is a hydrogen atom or a protecting group for nitrogen; a compound represented by the general formula (6): wherein R 13 is a hydrogen atom, an optionally substituted C1-C6 alkyl group or a protecting group for nitrogen, R 14 is a hydrogen atom, an optionally substituted C1-C6 group, a protecting group for nitrogen, or a pentose residue, and each of R 15 and R 16 is a hydrogen atom or a protecting group for nitrogen; a compound represented by the general formula (7): wherein R 17 is a hydrogen atom, an optionally substituted C1-C6 alkyl group or a protecting group for nitrogen, and R 18 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, a protecting group for nitrogen, or a pentose residue; or a compound represented by the general formula (8): wherein R 19 is a hydrogen atom, an optionally substituted C1-C6 alkyl group or a protecting group for nitrogen, R 20 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, a protecting group for nitrogen, or a pentose residue, and R 21 is a hydrogen atom, an optionally substituted C1-C6 alkyl group or a protecting group for nitrogen, with a perfluoroalkyl halide represented by the general formula (2): wherein Rf is a C1-C6 perfluoroalkyl group and X is a halogen atom, in the presence of a sulfoxide represented by the general formula (1): wherein each of R