| 摘要 |
<p>NEW MATERIAL:The titled compound of formula I [R1 is naphthyl or group of formula II (R6 and R7 are H, F, OH, lower alkoxyl, etc.; when one of R6 and R7 is H or OH, the other is group other than H); R4 is 3-4C alkyl or 3-guanidinopropyl]. EXAMPLE:(2S,3R)-3-Amino-2-hydroxy-4-(4'-methoxyphenyl)butanoyl-(S)-leu cine. USE:A medicine capable of inhibiting aminopeptidase B in the same manner as Bestatin [chemical name: (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-S- leucine] having an immunological enhancing action and a cancer inhibitory effect. PROCESS:The reaction product between a compound of formula III (R2 is protected amino group) and a compound of formula IV (R3 is H or ester residue) is reduced by the catalytic reduction, and the resultant product is condensed with a compound of formula V. The protecting group is then removed to afford the compound of formula I.</p> |
