Deprotection of the post-cleavage for the convergent synthesis of proteins by chemical ligation sulfur.

摘要

Compound of formula: Xaai- ... -Xaam- (CH-R) -CO-OC * H [(CH2) n-R '] - Y wherein: Xaa i is a protected or unprotected amino acid for i = 1 am; m is an integer between 2 and 200; n is an integer between 1 and 10; C * is a chiral carbon atom in R or S configuration, and substantially free from the opposite configuration; R is a side chain of an amino acid; R '' is -SR '', Y is an electron withdrawing group selected from the group consisting of Rc, C1-3 alkyl substituted with 1 to 3 groups Rc, -C (O) -Rd, -S (O) p-C1-3alkyl substituted with 0 to 3 groups Rc, and an aryl substituted with 1 to 3 groups Rc; each Rc group is independently a member selected from the group consisting of halogen, polyhaloalkyl, substituted or unsubstituted benzyl, substituted aryl or unsubstituted -C (O) NH2, -C (O) -NHHN2, -S (O ) 2NH2, substituted or unsubstituted hydroxylamine, cyano, nitro and quaternary ammonium salts; p is an integer between 1 and 2; Rd is a member selected from the group consisting of hydrogen, -N (Re) 2, OR e and -SR e; each Re is independently selected from the group consisting of hydrogen element, C1-3 alkyl substituted with 0 to 3 groups R, and -SO2-C1-3 alkyl substituted with 1 to 3 groups Rc; alternatively, in the case where two R groups are present, together with the atom to which they are attached can form a non-aromatic heterocyclic 5- to 6-membered containing 1 to 3 heteroatoms each independently selected from the group consisting of N, O and S, substituted with 0 to 3 groups Rc, and wherein R '' is a member selected from the group consisting of ethyl, t-butyl and substituted phenyl.