| 摘要 |
<p>A method for preparing 2'-deoxy-2',2'-difluorocytidine is provided to mass-produce the 2'-deoxy-2',2'-difluorocytidine with high purity easily by reacting 2-(2'-deoxy-2',2'-difluoro-D-ribofuranosyl)-1-methylpyridinium para toluene sulfonate with nucleobase. A method for preparing 2'-deoxy-2',2'-difluorocytidine represented by a formula(1) comprises the steps of: (a) reacting a lactol compound represented by a formula(6) with 2-fluoro-1-methylpyridinium para toluene sulfonate represented by a formula(5) to obtain 2-(2'-deoxy-2',2'-difluoro-D-ribofuranosyl)-1-methylpyridinium para toluene sulfonate represented by a formula(3); and (b) after mixing the compound of the formula(3) and nucleobase represented by a formula(4) with a reaction solvent such as hexamethyldisilazane, benzene, toluene, xylene, substituted benzene, diphenylether, substituted diphenylether, biphenyl, substituted biphenyl, C6-14 alkane, substituted C6-14 alkane and a mixture thereof to obtain a nucleoside compound represented by a formula(2), deprotecting the compound of the formula(2) to obtain the compound of the formula(1). In the formulae, R^1 and R^2 are independent from each other and are selected from a group(1), a group(2) or a group(3); R^3 is H, cyano, halogen, carboalkoxy, phenyl, nitro, C1-3 alkoxy, C1-3 alkyl, C1-3 dialkylamino, or a phenyl substituted by at least one selected from the group consisting of H, cyano, halogen, carboalkoxy, phenyl, nitro, C1-3 alkoxy, C1-3 alkyl, and C1-3 dialkylamino; Z is alkyl; and P is an amino protecting group.</p> |
