Verfahren zur Herstellung eledoisinwirksamer Verbindungen

1,139,333. N - Acylated hexapeptides. SCHERING A.G. 19 April, 1966 [21 Sept., 1965], No. 17114/66. Addition to 1,054,191. Heading C2C. Compounds of the general formula R-Ala-Phe-L-α-aminoacyl-Gly-Leu-Met-NH 2 where R is a formic or nicotinic acid residue or a functionally substituted residue of an organic carboxylic acid except the residue of a natural, non-acylated amino acid, and "α-α-aminoacyl" represents Leu or Val residues are prepared by linking by a conventional method of peptide synthesis the individual amino acids and the acid R.OH or in any specific case a reactive derivative thereof. A functionally substituted residue of an organic carboxylic acid is an acyl group additionally substituted by carbonyl, carboxyl, halogen, hydroxyl, or non α-positioned amino group. The following starting materials and intermediates are prepared: For-Ala-Phe-OMe and - NHNH 2 , nicotinoyl - Ala - Phe - OMe and - NHNH 2 , AC - Lys(BOC) - NHNH 2 . BOC - Lys(Ac)OH, BOC - Lys - (Ac) - ONP and BOC- #-Acap-OH (where For = formyl, Ac=acetyl and #-Acap = #-aminocaproic acid).