| 摘要 |
<p><P>PROBLEM TO BE SOLVED: To provide a method for producing 4'-C-ethynyl-2'-deoxypurine nucleoside by using 2'-deoxypurine nucleoside as a starting material. <P>SOLUTION: This method for producing 4'-C-ethynyl-2'-deoxypurine nucleoside is provided by oxidizing a hydroxymethyl group at the 4' position of a compound expressed by formula [VII] to an aldehyde group, then converting it to a bromovinyl group, converting again to an ethynyl group by treating with a strong base to obtain a compound expressed by formula [VIII], then removing blocking groups at 3' and 5' positions of the compound to obtain a compound of which R is H, further phosphorylating as desired to obtain a compound expressed by formula [I]. In each of the above formulae, B is a purine (including azapurine or deazapurine) base; R is H or phosphate residue; and R2 to R4 are each a protecting group. <P>COPYRIGHT: (C)2004,JPO</p> |
