| 摘要 |
<p>PURPOSE:To obtain the subject compound useful as an allergic reaction blocker, etc., on an industrial scale at a low cost by reacting an NG-nitro-L-arginine benzyl ester with an amino acid having protected amino group, removing the amino-protecting group, repeating the above process and finally deprotecting the product. CONSTITUTION:The objective pentapeptide of formula IV can be produced by converting N-t-butoxycarbonyl-L-proline to a mixed acid anhydride or an active ester, reacting with an NG-nitro-L-arginine benzyl ester of formula I (Bzl is benzyl), deprotecting the amino group, reacting with an activated N-t- butoxycarbonyl-beta-benzyl-L-aspartic acid to obtain a protected tripeptide, deprotecting the amino group, reacting with activated N-t-butoxycarbonyl-L- serine to obtain a protected tetrapeptide, deprotecting the amino group of the tetrapeptide, reacting with N-benzyloxycarbonyl-beta-benzylaspartic acid to obtain a protected pentapeptide of formula II and deprotecting the product.</p> |
