Methods of producing phosphitylated compounds

Provided are methods of producing phosphitylated compounds, including 3'-O-phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of: (1) acid-base complexes...

Full description

Saved in:
Bibliographic Details
Main Authors CHRISTIAN WERNER, FRANC NERENZ, ANDREAS KANSCHIK-CONRADSEN
Format Patent
LanguageEnglish
Published 09.09.2003
Edition7
Subjects
Online AccessGet full text

Cover

Loading…
More Information
Summary:Provided are methods of producing phosphitylated compounds, including 3'-O-phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of: (1) acid-base complexes derived from an amine base of Formula II wherein R3, R4, R5, R6, and R7 are independently hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, C7-C10 aralkyl, C1-C10 heteroalkyl, or C1-C10 heteroaryl, and at least one of R3, R4, R5, R6, and R7 is not hydrogen; (2) zwitterionic amine complexes; and (3) combinations of two or more thereof, to produce a phosphitylated compound. Further provided are methods for purifying phosphitylated compounds comprising the steps of providing a phosphitylated compound in a solution solvent, contacting said phosphitylated compound with a precipitation solvent, and precipitating said phosphitylated compound.
Bibliography:Application Number: AU20030217706