Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus esters
Patent
1997-04-11
1999-07-06
Ambrose, Michael G.
Organic compounds -- part of the class 532-570 series
Organic compounds
Phosphorus esters
536 2534, 556 26, 558169, C07F 9117, C07F 909
Patent
active
059199679
ABSTRACT:
A process for preparing a phosphodiester of the formula: ##STR1## is described that involves (1) reaction of a first alcohol with phosphorous trichloride to form a phosphorodichlorodite, (2) reaction of the phosphorodichlorodite with an amine to form a phosphorodiamidite, (3) reaction with a second alcohol (which may be the same as the first alcohol) to form a phosphoramidite diester, and finally, (4) hydrolysis and oxidation of the phosphoramidite to form the phosphodiester. R and R1 may represent aliphatic, aromatic, heterocyclic, peptidic, peptoid, deoxyribo- or ribonucleotidic or nucleosidic, or organic chelating moieties.
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Amedio John C.
Bernard Paul J.
Fountain Mark
Ambrose Michael G.
EPIX Medical, Inc.
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