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Process for producing aminophosphonic acid derivative

Foreign code F110003946
File No. E07605WO
Posted date Jul 7, 2011
Country EPO
Application number 05720123
Gazette No. 1724275
Gazette No. 1724275
Date of filing Mar 7, 2005
Gazette Date Nov 22, 2006
Gazette Date Apr 8, 2015
International application number JP2005003851
International publication number WO2005085262
Date of international filing Mar 7, 2005
Date of international publication Sep 15, 2005
Priority data
  • 2005JP003851 (Mar 7, 2005) WO
  • P2004-065251 (Mar 9, 2004) JP
Title Process for producing aminophosphonic acid derivative
Abstract To present a reaction system that efficiently catalyzes an enantio selective asymmetric nucleophilic addition reaction of an alpha -iminophosphonic acid ester.
An optically active alpha -amino-gamma -oxophosphonic acid derivative is produced through an asymmetric addition reaction of an alpha -iminophosphonic acid ester and a nucleophilic agent (for example, a silyl enol ether).
Scope of claims [claim1]
1. A production method for aminophosphonic acid derivatives represented by the formula below: (see diagramm) wherein, R **1 to R **7 are as defmed below, wherein the production method comprises reacting an alpha -iminophosphonate ester represented by the formula below (see diagramm) wherein R **1 represents an alkyl group and R **2 represents a protective group for an amino group, and a nucleophilic agent that is a silyl enol ether represented by the formula below (see diagramm) wherein R **5 and R **6, may be identical or different, represent hydrogen atoms, alkyl groups, aryl groups or aralkyl groups, R **7 represents an alkyl group, aryl group, aralkyl group, alkoxy group or sulfide group represented by -SR **9, wherein R **9 represents an alkyl group, and R **8, may be identical or different, represents an alkyl group, in the presence of a chiral copper catalyst represented by the formula below (see diagramm) wherein R **3 and R **4, may be identical or different, represent an aryl group or an aralkyl group.
[claim2]
2. The production method of claim 1, wherein a compound having an activated proton is added to the reaction medium as an additive, wherein the compound having an activated proton is selected from water, alcohols or carboxylic acids.
[claim3]
3. The production method of claim 2, wherein the additive is hexafluro isopropyl alcohol (HFIP).
  • Applicant
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
  • Inventor
  • KOBAYASHI SHU
IPC(International Patent Classification)
Reference ( R and D project ) ERATO KOBAYASHI Highly Functionalized Reaction Environments AREA
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