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Process for producing aminophosphonic acid derivative

外国特許コード F110003946
整理番号 E07605WO
掲載日 2011年7月7日
出願国 欧州特許庁(EPO)
出願番号 05720123
公報番号 1724275
公報番号 1724275
出願日 平成17年3月7日(2005.3.7)
公報発行日 平成18年11月22日(2006.11.22)
公報発行日 平成27年4月8日(2015.4.8)
国際出願番号 JP2005003851
国際公開番号 WO2005085262
国際出願日 平成17年3月7日(2005.3.7)
国際公開日 平成17年9月15日(2005.9.15)
優先権データ
  • 2005JP003851 (2005.3.7) WO
  • 特願2004-065251 (2004.3.9) JP
発明の名称 (英語) Process for producing aminophosphonic acid derivative
発明の概要(英語) 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).
特許請求の範囲(英語) [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).
  • 出願人(英語)
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
  • 発明者(英語)
  • KOBAYASHI SHU
国際特許分類(IPC)
欧州特許分類/主・副
  • B01J031/18B
  • C07B053/00
  • C07F009/38A1
  • C07F009/38A7
  • C07F009/40A1
  • C07F009/40A7
  • L01J531/16
指定国 Contracting States: CH DE FR GB LI
参考情報 (研究プロジェクト等) ERATO KOBAYASHI Highly Functionalized Reaction Environments AREA
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