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Production method for aminophosphonic acid derivatives

外国特許コード F110003807
整理番号 E07605WO
掲載日 2011年7月5日
出願国 アメリカ合衆国
出願番号 59196405
公報番号 20070142658
公報番号 7375244
出願日 平成17年3月7日(2005.3.7)
公報発行日 平成19年6月21日(2007.6.21)
公報発行日 平成20年5月20日(2008.5.20)
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
  • 特願2004-065251 (2004.3.9) JP
  • 2005WO-JP03851 (2005.3.7) WO
発明の名称 (英語) Production method for aminophosphonic acid derivatives
発明の概要(英語) (US7375244)
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 comprising reacting an alpha -iminophosphonate ester represented by the formula
wherein R1 represents an alkyl group and R2 represents a protective group for an amino group, and a nucleophilic agent in the presence of a chiral copper catalyst represented by the formula
wherein R3 and R4, may be identical or different, represent an aryl group or an aralkyl group.
[claim2]
2. The production method of claim 1, wherein the nucleophilic agent is a silyl enol ether represented by the formula
wherein R5 and R6, may be identical or different, represent hydrogen atoms, alkyl groups, aryl groups or aralkyl groups, R7 represents an alkyl group, aryl group, aralkyl group, alkoxy group or sulfide group represented by -- SR9, wherein R9 represents an alkyl group or an aryl group, and R8, may be identical or different, represents an alkyl group or a phenyl group.
[claim3]
3. The production method of claim 1, wherein a compound having an activated proton is added to the reaction medium as an additive.
[claim4]
4. The production method of claim 3, wherein the additive is hexafluoro isopropyl alcohol (HFIP).
[claim5]
5. The production method of claim 1, wherein the aminophosphonic acid derivative is represented by the formula
wherein, R1 represents an alkyl group, R2 represents a protective group for an amino group, R3 and R4, which may be identical or different, each represent an aryl group or an aralkyl group, R5 and R6, which may be identical or different, each represent hydrogen atoms, alkyl groups, aryl groups or aralkyl groups, and R7 represents an alkyl group, aryl group, aralkyl group, alkoxy group or sulfide group represented by -- SR9, wherein R9 represents an alkyl group or an aryl group.
[claim6]
6. The production method of claim 2, wherein a compound having an activated proton is added to the reaction medium as an additive.
[claim7]
7. The production method of claim 6, wherein the additive is hexafluoro isopropyl alcohol (HFIP).
[claim8]
8. The production method of claim 2, wherein the aminophosphonic acid derivative is represented by the formula
wherein, R1 represents an alkyl group, R2 represents a protective group for an amino group, R3 and R4, which may be identical or different, each represent an aryl group or an aralkyl group, R5 and R6, which may be identical or different, each represent hydrogen atoms, alkyl groups, aryl groups or aralkyl groups, and R7 represents an alkyl group, aryl group, aralkyl group, alkoxy group or sulfide group represented by -- SR9, wherein R9 represents an alkyl group or an aryl group.
[claim9]
9. The production method of claim 3, wherein the aminophosphonic acid derivative represented by the formula
wherein, R1 represents an alkyl group, R2 represents a protective group for an amino group, R3 and R4, which may be identical or different, each represent an aryl group or an aralkyl group, R5 and R6, which may be identical or different, each represent hydrogen atoms, alkyl groups, aryl groups or aralkyl groups, and R7 represents an alkyl group, aryl group, aralkyl group, alkoxy group or sulfide group represented by -- SR9, wherein R9 represents an alkyl group or an aryl group.
[claim10]
10. The production method of claim 4, wherein the aminophosphonic acid derivative represented by the formula
wherein, R1 represents an alkyl group, R2 represents a protective group for an amino group, R3 and R4, which may be identical or different, each represent an aryl group or an aralkyl group, R5 and R6, which may be identical or different, each represent hydrogen atoms, alkyl groups, aryl groups or aralkyl groups, and R7 represents an alkyl group, aryl group, aralkyl group, alkoxy group or sulfide group represented by -- SR9, wherein R9 represents an alkyl group or an aryl group.
  • 発明者/出願人(英語)
  • KOBAYASHI SHU
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
国際特許分類(IPC)
参考情報 (研究プロジェクト等) ERATO KOBAYASHI Highly Functionalized Reaction Environments AREA
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