| 摘要 |
<p>PURPOSE:To obtain the titled compound in high yield without causing side reactions, by protecting the guanidino group of a raw material compound containing the guanidino group with a substituted benzenesulfonyl group, forming a peptide bond, and removing the protecting group with an acid. CONSTITUTION:A guanidino group in an arginine derivative of formulaI(R3 is methyl or methoxyl when R1, R2, R4 and R5 are methyl; R2 and R4 are h when R1, R3 and R5 are methoxyl; R6 is H or a protecting group of the alpha-amino group) which is a raw material compound containing the guanidino group is protected with a substituted benzenesulfonyl group of formula II to form a peptide bond. The protecting group is then removed with trifluoroacetic acid in the presence of thioanisole or anisole to afford the aimed peptide. EFFECT:The mild acid treatment, e.g. trifluoroacetic acid, is unsuitable for the wellknown removal of the guanidino group; however, the acid treatment is fully advance d under mild conditions in the case of the substituted benezenesulfonyl group used for the protection.</p> |
