| 主权项 |
1. A lysine-resin conjugate comprising a resin and a lysine or a lysine derivative of the formula I: wherein W is an acid sensitive or thermal sensitive resin, or a resin that is both acid and thermal sensitive toward cleavage of the lysine or lysine derivative from the resin; R is selected from the group consisting of —OH, a carboxyl protecting group, —NH2, —O—C1-6 alkyl, —O—C2-6 alkenyl, —O-tri-C1-3 alkyl silyl, a peptide residue selected from the group consisting of -Pro-OH, -Pro-NH2, -Pro-O—C1-6 alkyl, -Pro-O—C2-6alkenyl, -Pro-O-tri-C1-3 alkylsilyl, Thr(Pr1), -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-OH, -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-NH2, -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-O—C1-6 alkyl, -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-O—C2-6 alkenyl, -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-O-tri-C1-3 alkylsilyl, -Thr(Pr1)-OH, -Thr(Pr1)-NH2, -Thr(Pr1)-O—C1-6 alkyl, -Thr(Pr1)-O—C2-6 alkenyl and -Thr(Pr1)-O-tri-C1-3alkylsilyl, a peptide residue comprising 1 to 200 amino acids comprising optionally protected side chain and optionally protected terminal carboxyl group, and a peptide residue selected from the group consisting of SEQ ID NOs: 1, 3, 4, 5, 6, 7, 8, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35 and 36; wherein Pr1 is an —OH protecting group and each Pr2 and Pr3 is independently hydrogen or a guanidine protecting group; and P is hydrogen, an amino protecting group, an N-terminus peptide residue comprising 1 to 200 amino acids comprising optionally protected side chain and optionally protected terminal amino group, wherein the N-terminus peptide residue comprises a C-terminus and an N-terminus, and a peptide residue selected from the group consisting of SEQ ID NOs: 1, 3, 4, 5, 6, 7, 8, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35 and 36; provided that when R is selected from the group consisting of —OH, a carboxyl protecting group, —NH2, —O—C1-6 alkyl, —O—C2-6 alkenyl, —O-tri-C1-3 alkyl silyl, a peptide residue selected from the group consisting of -Pro-OH, -Pro-NH2, -Pro-O—C1-6 alkyl, -Pro-O—C2-6 alkenyl, -Pro-O-tri-C1-3 alkylsilyl, Thr(Pr1), -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-OH, -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-NH2, -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-O—C1-6 alkyl, -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-O-C2-6 alkenyl, -Thr(Pr1)-Arg(Pr2)-Arg(Pr3)-O-tri-C1-3 alkylsilyl, -Thr(Pr1)-OH, -Thr(Pr1)-NH2, -Thr(Pr1)-O—C1-6 alkyl, -Thr(Pr1)-O—C2-6 alkenyl and -Thr(Pr1)-O-tri-C1-3 alkylsilyl, and a peptide residue comprising 1 to 200 amino acids comprising optionally protected side chain and optionally protected terminal carboxyl group, then P is not hydrogen or an amino protecting group. |
