专利号:US-5169935-A 优先权日:1990-06-20 标 题:Method of making peptides 发明人:HOEGER CARL A; THEOBALD PAULA G; PORTER JOHN S; RIVIER JEAN E F 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:Methods for making peptides of a suitable length for solid phase synthesis, which peptides include in their sequence a pair of residues of a different character which have acylated side chains and a residue which has an N-alkylated side chain. A peptide intermediate is constructed on the resin using commercially available starting materials. The N-terminus can be acylated by removing the alpha -amino protecting group and acylating under standard conditions. First primary amino protecting groups included in those residues to be acylated are removed, and acylation is effected, preferably by using a carboxypyridine or a similar heterocyclic acylating agent. Following such side chain acylation, a second protecting group included in the residue to be N-alkylated is removed, and the N-alkylation reaction is carried out while the peptide remains on the resin using a borohydride and an appropriate aldehyde or ketone. Following cleavage from the resin and removal of any protecting groups still remaining, the peptide is appropriately purified, thus requiring only a single purification to be carried out while forming a synthetic peptide including residues for which the modified amino acids are not readily commercially available.
参考文献:10.1023/a:1023348928376 摘要:Brown GR, Sutcliffe IC, Cummings SP. Combined solvent and water activity stresses on turgor regulation and membrane adaptation in Oceanimonas baumannii ATCC 700832. Antonie Van Leeuwenhoek. 2003;83(3):275–83. doi: 10.1023/a:1023348928376.