Invention Grant
- Patent Title: Process for the preparation of enantiomerically-enriched cyclopropylalanine derivates
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Application No.: US09957549Application Date: 2001-09-20
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Publication No.: US06635784B2Publication Date: 2003-10-21
- Inventor: Sheryl Davis Debenham , Neil Warren Boaz
- Applicant: Sheryl Davis Debenham , Neil Warren Boaz
- Main IPC: C07C6974
- IPC: C07C6974

Abstract:
Disclosed are processes for the preparation of enantiomerically-enriched cyclopropylalanine derivatives by the hydrogenation of certain enamides in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst and certain novel enamide ester compounds which are intermediates in the processes. The processes include novel 2-step and 3-step processes for the preparation of enantiomerically-enriched cyclopropylalanine derivatives. The two-step process comprises the steps of reacting cyclopropanecarboxaldehyde with a substituted phosphorylglycine to afford an enamide ester which then is hydrogenated in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst. The three-step process comprises the steps of forming an azlactone from an N-acylglycine and cyclopropanecarboxaldehyde, converting the azlactone to the aforesaid enamide which then is hydrogenated in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst.
Public/Granted literature
- US20020049331A1 Process for the preparation of enantiomerically-enriched cyclopropylalanine derivates Public/Granted day:2002-04-25
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