| 摘要 |
<p>A process for the production of cladribine, 2-chloro-2'-deoxyadenosine, is provided which involves the direct glycosylation of 2-chloro-6-aminopurine with 1-chloro-2-deoxy-3,5-di-O-p-toluoyl-α-D-erythropentofuranose. The process is carried out by first forming the sodium salt of 2-chloro-6-aminopurine and allowing the sodium salt to react with 1-chloro-2-deoxy-3,5-di-O-p-toluoyl-α-D-erythropentofuranose in the presence of a moderately polar solvent such as acetone. The final product, cladribine, is produced by removal of the p-toluoyl groups by the action of methanolic ammonia or methanolic sodium methoxide.</p> |
