Methods for preparing internally constrained peptides and peptidomimetics

A method of preparing a compound of Formula II:

• wherein
• R is hydrogen, an amino acid side chain, an alkyl group, or an aryl group;
• R1 is an amino acid side chain, an alkyl group, or an aryl group;
• R2 is an amino acid, peptide, OR, CH2NH2, an alkyl group, an aryl group, or a group of formula:
• wherein R7 is an amino acid, peptide, OR, CH2NH2, an alkyl group, or an aryl group;
• R3 is an amino acid, peptide, OR, CH9Mi2, an alkyl group, an aryl group, hydrogen, or a group of formula
• is a single or double carbon-carbon bond;
• is a single bond and is cis or trans when is a double bond;
• n is 1 or 2;
• and m is any number, said method comprising:
• providing a compound of Formula I:
• and
• reacting said compound of Formula I under conditions effective to produce a compound of Formula II;
• wherein said reacting comprises a ring-closing metathesis reaction.