| 摘要 |
<p>PURPOSE:To obtain peptide having guanido group, by forming a peptide from a starting compound wherein the guanido group is protected by mesitylene-2-sulfonyl group, and by eliminating the protecting group with a methanesulfonic acid, etc. CONSTITUTION:One equivalent of a starting compound having a guanido group is reacted with 1-2 equivalents of a mesitylene-2-sulfonyl halogenide in the presence of a base to protect the guanido group with the mesitylene-2-sulfonyl group, and changed into a peptide. The protecting group is then eliminated by methanesulfonic or trifluoro-methanesulfonic acid in the presence of anisole to suppress side reactions due to cations formed. The desired guanido group-containing peptide is thus obtained. EFFECT:Neither impurity formation due to the side reactions nor necessity of special vessels in eliminating the protecting group.</p> |
