Patent ID: 6570039
Filing Date: 2003-05-27
Classification: C07B,C07C,C07D

Abstract:
A process for producing N-protected &agr;-aminohalomethyl ketones of the following general formula (3): wherein A represents an unsubstituted or substituted alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 15 carbon atoms, an aralkyl group having 7 to 20 carbon atoms, an unsubstituted or substituted alkyl group having 1 to 10 carbon atoms which contains a hetero atom in the carbon skeleton, an aryl group having 6 to 15 carbon atoms which contains a hetero atom in the carbon skeleton, or an aralkyl group having 7 to 20 carbon atoms which contains a hetero atom in the carbon skeleton; B1 represents a protecting group for the amino group; and X represents a halogen atom or &agr;-aminohalomethyl ketones of the following general formula (4): wherein A and X are as defined above, or salts thereof, which comprises the steps of reacting a 3-oxazolidin-5-one derivative of the following general formula (1): wherein R represents an unsubstituted or substituted aryl group or lower alkyl group, or a hydrogen atom, and A and B1 are as defined above with a halomethyl lithium to produce a reaction product; and then treating the reaction product with an acid.