N2-(1-CARBOXY-3-PHENYLPROPYL)-L-LYSIN DERIVATIVE AND PRODUCTION OF LYSINOPURYL USING SAID COMPOUND

摘要

NEW MATERIAL:Compounds expressed by formula I (R<1> is protecting group; R<2> is H, alkyl, etc.; X is CN, etc.; * represents S-configuration to asymmetric carbon). formula II (Y is CN, etc.) and formula III (R<3> is H, alkyl, etc.). EXAMPLE:N<2>-[1(s)-Cyano-3-phenylpropyl]-N<6> trifluoroacetyl-L-lysin, N-carboxy anhydride thereof and N<2>-[1(s)-carbamyl-3-phenylpropyl]-N<6>-trifluoroacetyl-L-lysin- L-proline. USE:An intermediate for antihypertensive. PREPARATION:beta-Phenylpropionaldehyde is reacted with prussic acid and a compound expressed by formula IV to afford the compound expressed by formula V wherein X is CN in formula I. A compound expressed by formula II is reacted with a compound expressed by formula VI to give the compound expressed by formula VII wherein Y is X in formula III, which is further hydrolyzed to provide the compound expressed by formula VIII useful as antihypertensive.