A method of preparing a β-turn peptidomimetic cyclic compound of formula the method comprising steps of: (a) providing a protected linear peptidomimetic compound of formula (b) cyclizing in a solution phase the protected linear peptidomimetic compound of formula to form a protected β-turn peptidomimetic cyclic compound of formula by an intramolecular aromatic nucleophilic substitution, (c) deprotecting an amino acid side chain protecting group in the protected β-turn peptidomimetic cyclic compound of formula wherein: R 1 and R 3 are independently hydrogen, C 1 to C 6 alkyl, aryl, or an amino acid side chain substituent of a natural or unnatural amino acid; R 2 and R 4 are independently hydrogen or C 1 to C 6 alkyl, or R 1 and R 2 together with the carbon atom to which they are attached form a cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl group, or R 3 and R 4 together with the carbon atom to which they are attached form a cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl group; R 5, R 6 and R 7 are independently hydrogen or C 1 to C 6 alkyl; Y is selected from the group consisting of hydrogen, -NO 2, - COOR 8, -OC(R 8) 3, - SO 3 R 8, and -SO 2 R 8; each R 8 is alkyl or aryl; X is selected from the group consisting of O, N, S, P, Se, C, C 1 to C 6 alkylene, SO, SO 2 and NH; Z is selected from the group consisting of F, CI, Br and I; R 11 and R 13 are independently hydrogen or a protecting group; W 1 and W 3 are independently an amino acid side chain substituent of a natural or unnatural amino acid, less a hydrogen atom at the point of attachment to R 11 and R 13 respectively; n is 0, 1, 2, 3, 4 or 5; and L 2 is H, NH 2, OH, SH, COOH, NH-CH 2 -COOH, C 1 to C 6 alkyl, or C 1 to C 6 aryl. (a) providing a protected linear peptidomimetic compound of formula (b) cyclizing in a solution phase the protected linear peptidomimetic compound of formula to form a protected β-turn peptidomimetic cyclic compound of formula by an intramolecular aromatic nucleophilic substitution, (c) deprotecting an amino acid side chain protecting group in the protected β-turn peptidomimetic cyclic compound of formula wherein: R 1 and R 3 are independently hydrogen, C 1 to C 6 alkyl, aryl, or an amino acid side chain substituent of a natural or unnatural amino acid; R 2 and R 4 are independently hydrogen or C 1 to C 6 alkyl, or R 1 and R 2 together with the carbon atom to which they are attached form a cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl group, or R 3 and R 4 together with the carbon atom to which they are attached form a cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl group; R 5, R 6 and R 7 are independently hydrogen or C 1 to C 6 alkyl; Y is selected from the group consisting of hydrogen, -NO 2, - COOR 8, -OC(R 8) 3, - SO 3 R 8, and -SO 2 R 8; each R 8 is alkyl or aryl; X is selected from the group consisting of O, N, S, P, Se, C, C 1 to C 6 alkylene, SO, SO 2 and NH; Z is selected from the group consisting of F, CI, Br and I; R 11 and R 13 are independently hydrogen or a protecting group; W 1 and W 3 are independently an amino acid side chain substituent of a natural or unnatural amino acid, less a hydrogen atom at the point of attachment to R 11 and R 13 respectively; n is 0, 1, 2, 3, 4 or 5; and L 2 is H, NH 2, OH, SH, COOH, NH-CH 2 -COOH, C 1 to C 6 alkyl, or C 1 to C 6 aryl. R 1 and R 3 are independently hydrogen, C 1 to C 6 alkyl, aryl, or an amino acid side chain substituent of a natural or unnatural amino acid; R 2 and R 4 are independently hydrogen or C 1 to C 6 alkyl, or R 1 and R 2 together with the carbon atom to which they are attached form a cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl group, or R 3 and R 4 together with the carbon atom to which they are attached form a cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl group; R 5, R 6 and R 7 are independently hydrogen or C 1 to C 6 alkyl; Y is selected from the group consisting of hydrogen, -NO 2, - COOR 8, -OC(R 8) 3, - SO 3 R 8, and -SO 2 R 8; each R 8 is alkyl or aryl; X is selected from the group consisting of O, N, S, P, Se, C, C 1 to C 6 alkylene, SO, SO 2 and NH; Z is selected from the group consisting of F, CI, Br and I; R 11 and R 13 are independently hydrogen or a protecting group; W 1 and W 3 are independently an amino acid side chain substituent of a natural or unnatural amino acid, less a hydrogen atom at the point of attachment to R 11 and R 13 respectively; n is 0, 1, 2, 3, 4 or 5; and L 2 is H, NH 2, OH, SH, COOH, NH-CH 2 -COOH, C 1 to C 6 alkyl, or C 1 to C 6 aryl.