| 5'-O-(Dimethoxytrityl)-6-N-Benzoyl-2'-deoxyadenosine,as an oligonucleotide in antisense drug research in the key pharmaceutical intermediates,plays a very important role in anti-virus,the treatment of hypertension,cancer treatment and so on.The synthesis of oligonucleotides intermediate research,has broad prospects.Using 2'-deoxyadenosine as raw material,6-N-Benzoyl-2'-deoxyadenosine and 5'-O-(Dimethoxytrityl)-6-N-Benzoyl-2'-deoxyadenosine,which is the important key monomer of antisense drug,were synthesized with an improved experiemental method. The high purity(HPLC)≧98.5%,simple operation,low cost and the elevated benefit are propitious to industrialization.The successful research into the synthesis of this intermediate will greatly promote the development of antiense drug.Furthermore,in the course of the experiment,hexamethyldisilane as a protective reagent is an innovative synthetic route.To adenosine as raw materials,using the improved synthesis methods of 2'-deoxyadenosine,prepared the two derivatives of adenosine—6-N-Benzoyl-adenosine and 5'-O-(Dimethoxytrityl)-6-N-Benzoyl-adenosine,purity and yield up to the synthesis of requirements,have a certain economic value and practical significance.The intermediate route of the process will be successfully developed to a certain extent,promoted the anti-sense drug development. |
