Invention Grant
- Patent Title: Directed synthesis of oligophosphoramidate stereoisomers
- Patent Title (中): 导向合成寡聚氨基磷酸酯立体异构体
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Application No.: US14026936Application Date: 2013-09-13
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Publication No.: US08853132B2Publication Date: 2014-10-07
- Inventor: Dieter Heindl , Dirk Kessler , Angelika Roesler , Christoph Seidel , Wilma Thuer
- Applicant: Roche Diagnostics Operations, Inc.
- Applicant Address: US IN Indianapolis
- Assignee: Roche Diagnostics Operations, Inc.
- Current Assignee: Roche Diagnostics Operations, Inc.
- Current Assignee Address: US IN Indianapolis
- Agency: Roche Diagnostsics Operations, Inc.
- Priority: EP08020625 20081127; EP08022319 20081223
- Main IPC: C07F9/6558
- IPC: C07F9/6558 ; G01N33/53 ; C07F9/655

Abstract:
The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.
Public/Granted literature
- US20140045719A1 DIRECTED SYNTHESIS OF OLIGOPHOSPHORAMIDATE STEREOISOMERS Public/Granted day:2014-02-13
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