| 摘要 |
<p>PURPOSE:To prepare the titled peptide with suppressed side reactions, by protecting the amino group of starting compound having omega-amino group and/or alpha-amino group using a novel protecting group which can be eliminated be mild acid treatment, and subjecting the protected compound to peptide condensation, etc. CONSTITUTION:A peptide having omega-amino group and/or alpha-amino group is prepared by (1) protecting the omega-amino group and/or alpha-amino group of the starting compound containing omega-amino group and/or alpha-amino group with 4-methoxy- 2,3,6-trimethylbenzenesulfonyl group, (2) subjecting the product to peptide condensation, and (3) eliminating the protecting group with an acide (e.g. trifluoroacetic acid). The amino acid is e.g. a lysine derivative of formula (at least one of R and R1 is 4-methoxy-2,3,6-trimethylbenzenesulfonyl group and the other is other protecting group or H). The elimination of the protecting group can be carried out economically in the presence of thioanisole.</p> |
