Process for producing 3-amino-2-oxo-1-halogenopropane...

C - Chemistry – Metallurgy – 07 – C

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C07C 229/36 (2006.01) C07C 221/00 (2006.01) C07C 225/16 (2006.01) C07C 227/16 (2006.01) C07C 227/32 (2006.01) C07C 229/22 (2006.01) C07C 229/34 (2006.01) C07C 269/06 (2006.01) C07C 271/10 (2006.01) C07C 271/22 (2006.01) C07C 311/19 (2006.01) C07C 319/20 (2006.01) C07C 323/43 (2006.01) C07C 323/59 (2006.01) C07D 303/40 (2006.01) C07D 307/20 (2006.01) C07D 407/12 (2006.01) C07F 7/08 (2006.01)

Patent

CA 2190570

3-Amino-2-oxo-1-halogenopropane derivatives are prepared by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate with a halogenating agent for halogenation of the 2-position, or by reacting a protected amino acid with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3- oxo-2-halogenobutanoic acid ester derivative which is then hydrolyzed and decarboxylated. The 3-amino-2-oxo-1- halogenopropane derivatives obtained in accordance with the invention can easily be converted to 3-amino-1,2- epoxypropanes that are important as intermediates for pharmaceutical preparations including HIV protease inhibitors and certain enzyme inhibitors.

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