Title:
METHOD OF SYNTHESIZING Α-AMINO ACID DERIVATIVE WITH Α-ALKYL SIDE CHAIN SUBSTITUTION
Document Type and Number:
WIPO Patent Application WO/2016/197580
Kind Code:
A1
Abstract:
The present invention discloses a method of synthesizing an α-amino acid derivative with α-alkyl side chain substitution. The method comprises: reacting an alkene with 9-bbn at 0-80˚C for 0.5-12 h, and then adding an imine to react at 0-90˚C for 12-48 h with the presence of a transition metal salt, a base and an organic solvent to generate an α-amino acid derivative. In the present invention, an alkene is employed to in-situ generate an alkyl boron reagent, wherein the reaction condition is mild and the alkaline can be selected from a wide range. For the existing synthesis methods, a strict anhydrous and anaerobic condition is required, complex reaction operations are involved, and a low temperate is needed for the reaction to occur, thus causing a high cooling cost. On the contrary, the present invention does not require an anhydrous and anaerobic condition, and the reaction can occur at the room temperature or a slightly higher temperature.
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Inventors:
ZENG WEI (CN)
XIAO XINSHENG (CN)
LU XIAOXIA (CN)
XIAO XINSHENG (CN)
LU XIAOXIA (CN)
Application Number:
PCT/CN2015/098519
Publication Date:
December 15, 2016
Filing Date:
December 23, 2015
Export Citation:
Assignee:
UNIV SOUTH CHINA TECH (CN)
International Classes:
C07C227/10; C07C229/18; C07C229/28; C07C229/36; C07C333/24
Foreign References:
| CN105017043A | 2015-11-04 | |||
| CN103524541A | 2014-01-22 |
Other References:
SINGH, N. ET AL.: "Highly Diastereoselective Radical Addition to Glyoxylate Imines of Chiral Amines without Additional Heteroatoms", TETRAHEDRON LETTERS, vol. 45, no. 14, 31 December 2004 (2004-12-31), pages 2911 - 2913, XP004495677
TSUNA, K. ET AL.: "Synthesis of Medium-Sized Carbocyclic Ketones via the Intramolecular B-Alkyl Liebeskind-Srogl Coupling Reaction", TETRAHEDRON LETTERS, vol. 52, no. 52, 4 November 2011 (2011-11-04), pages 7202 - 7205, XP028596975
TSUNA, K. ET AL.: "Synthesis of Medium-Sized Carbocyclic Ketones via the Intramolecular B-Alkyl Liebeskind-Srogl Coupling Reaction", TETRAHEDRON LETTERS, vol. 52, no. 52, 4 November 2011 (2011-11-04), pages 7202 - 7205, XP028596975
Attorney, Agent or Firm:
GUANGZHOU HUAXUE INTELLECTUAL PROPERTY AGENCY CO., LTD (CN)
广州市华学知识产权代理有限公司 (CN)
广州市华学知识产权代理有限公司 (CN)
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