专利号:US-5602231-A 优先权日:1991-06-14 标题 :Process for making peptides 发明人:COTTON RONALD; GILES MICHAEL B 权利人:ZENECA LTD 摘要:A process for the solid phase synthesis of peptides containing a C-terminal aza-amino acid, for example the decapeptide goserelin, which comprises: (i) reacting an active ester or imidazolide of an N-protected aza-amino acid either with an appropriate reactive solid support in the case of the synthesis of a peptide containing a C-terminal aza-amino acid, or with a peptide which is attached to a solid support in the case of the synthesis of a peptide containing a non-C-terminal aza-amino acid; (ii) carrying out further conventional solid phase peptide synthesis steps to add sequentially further amino acids, to form a peptide with the required amino acid sequence bound to the solid support; (iii) cleaving the peptide from the solid support, and optionally (iv) reacting the product so formed with hydrazine to remove any acyl groups which have been formed on serine, arginine, tyrosine, threonine or hydroxyproline during the synthesis.
专利号:US-5510460-A 优先权日:1991-06-14 标 题:Peptide process 发明人:HAYWARD CHRISTOPHER F 权利人:ZENECA LTD 摘要:A process for the solid phase synthesis of peptides containing an aza-amino acid, for example the decapeptide goserelin, which comprises: (i) assembling all the amino acids of the peptide except the C-terminal aza-amino acid by conventional solid phase synthesis; (ii) cleaving the peptide from the support with hydrazine or a substituted hydrazine; and (iii) reacting the hydrazide thus released with a cyanate ion.