发明名称 PHOSPHINOAMIDITE CARBOXYLATES AND ANALOGS THEREOF IN THE SYNTHESIS OF OLIGONUCLEOTIDES HAVING REDUCED INTERNUCLEOTIDE CHARGE
摘要 <p>Phosphinoamidite carboxylates and analogs are provided that have the structure of formula (I) wherein R?1, R2, R3, R4¿, X, Y, Z and n are as defined herein. The compounds are useful as phosphitylating agents, e.g., in the phosphitylation of 3' and 5' hydroxyl groups of nucleosides and oligonucleotides. Also provided are phosphonocarboxylate and H-phosphonite carboxylate analogs of the compounds of formula (I). The compounds enable synthesis of phosphinocarboxylate and phosphonocarboxylate oligonucleotides having reduced internucleotide charge and enhanced nuclease resistance.</p>
申请公布号 WO2002032912(A2) 申请公布日期 2002.04.25
申请号 US2001032465 申请日期 2001.10.16
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