Title:
ホスホジエステルを合成するためのプロセス
Document Type and Number:
Japanese Patent JP4014231
Kind Code:
B2
Abstract:
A process for preparing a phosphodiester of the formula: 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.
Inventors:
Amedio, John Sea.
Bernard, Paul Jay.
Fountain mark
Bernard, Paul Jay.
Fountain mark
Application Number:
JP54386798A
Publication Date:
November 28, 2007
Filing Date:
January 27, 1998
Export Citation:
Assignee:
Epics Pharmaceuticals, Inc.
International Classes:
C07F9/09; C07F9/117
Domestic Patent References:
| JP8508513A | ||||
| JP6508144A |
Foreign References:
| WO1996023526A1 |
Other References:
Alvan C. Hengge et al., Studies of Transition-State Structures in Phosphoryl Transfer Reactions of Phosphodiesters of p-Nitrophenol, J. AM. CHEM. SOC., 1995年, Vol.117, No.22, P.5919-5926
Yang Lu et al., A new, convenient and efficient procedure for the synthesis of phosphodiesters using chloro-N,N-diisopropylaminoalkyloxyphosphines, SYNTH. COMMUN., 1993年, Vol.23, No.14, P.1943-1946
Yang Lu et al., A new, convenient and efficient procedure for the synthesis of phosphodiesters using chloro-N,N-diisopropylaminoalkyloxyphosphines, SYNTH. COMMUN., 1993年, Vol.23, No.14, P.1943-1946
Attorney, Agent or Firm:
Hidesaku Yamamoto