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Title:
PHOSPHINOAMIDITE CARBOXYLATES AND ANALOGS THEREOF IN THE SYNTHESIS OF OLIGONUCLEOTIDES HAVING REDUCED INTERNUCLEOTIDE CHARGE
Document Type and Number:
WIPO Patent Application WO2002032912
Kind Code:
A3
Abstract:
Phosphinoamidite carboxylates and analogs are provided that have the structure of formula (I) wherein R<1>, R<2>, R<3>, R<4>, 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.

Inventors:
DELLINGER DOUGLAS J (US)
Application Number:
PCT/US2001/032465
Publication Date:
March 13, 2003
Filing Date:
October 16, 2001
Export Citation:
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Assignee:
DELLINGER DOUGLAS J (US)
International Classes:
C07H19/10; C07H19/20; C07H21/00; (IPC1-7): C07H21/00; C07H19/04; C07H21/02; C07H21/04; C07H19/00; C07C301/00; C07C313/00; C07C229/00; C07F9/02
Domestic Patent References:
WO1993010140A11993-05-27
Foreign References:
US4056673A1977-11-01
Other References:
NOVIKOVA Z.S.: "Reactivity of diphosphorus III-substituted acetic esters", THURNAL OBSHCHEI KHIMII, vol. 46, no. 10, 1976, pages 2128 - 2131, XP002956883
See also references of EP 1334111A4
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