Patent ID: 6228986
Filing Date: 2001-05-08
Classification: C07K

Abstract:
A process for preparing a macrocyclic compound of the formula: ##STR7##wherein:R.sub.1 is selected from the group consisting of naphthyl, diphenyl, and phenoxyphenyl;R.sub.2 is selected from the group consisting of C.sub.1 -C.sub.6 alkyl, benzyl, C.sub.1 -C.sub.6 alkylamino, CH.sub.2 SCH.sub.2 Ph, and CH.sub.2 (4-MeO)Ph;R.sub.3 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; andR.sub.4 is selected from the group consisting of hydrogen, phenyl, C.sub.1 -C.sub.6 alkyl;or R.sub.3 and R.sub.4 taken together form a 5-6 membered carbocyclic ring;which comprises:preparing a resin-bound protected dipeptide precursor of the formula: ##STR8##from a resin-bound orthogonally protected lysine residue by reductive alkylation of the .alpha.-nitrogen followed by acylation with an Fmoc-aminoacid to provide the protected dipeptide precursor; and removing the Fmoc-group, acylating with an appropriately substituted succinic anhydride, removing the methyltrityl-group followed by macrcocyclization to provide the desired macrocycle of formula I.