公开(公告)号：EP1546090B1

公开(公告)日：2009-06-24

申请号：EP03798091.9

申请日：2003-09-25

申请人： NOVO NORDISK A/S

发明人： DÜNWEBER, Dorte, Lunöe ,  JENSEN, Inge, Holm ,  HANSEN, Louis, Brammer

IPC分类号： C07C235/72 ,  C07K1/06 ,  G01N33/68 ,  A61K38/28 ,  C07K14/605 ,  C07K14/62

CPC分类号： G01N33/6842 ,  C07K1/1077 ,  C07K14/57563 ,  C07K14/605 ,  C07K14/62 ,  G01N33/68

摘要： The present invention provides a method for acylating one or more amino groups of a peptide where the acylation reaction is to be performed in an aqueous mixture containing less than 10 %w/w aprotic polar solvent.

公开(公告)号：EP1546090A2

公开(公告)日：2005-06-29

申请号：EP03798091.9

申请日：2003-09-25

申请人： NOVO NORDISK A/S

发明人： DÜNWEBER, Dorte, Lunöe ,  JENSEN, Inge, Holm ,  HANSEN, Louis, Brammer

IPC分类号： C07C235/72 ,  C07K1/06 ,  G01N33/68 ,  A61K38/28 ,  C07K14/605 ,  C07K14/62

CPC分类号： G01N33/6842 ,  C07K1/1077 ,  C07K14/57563 ,  C07K14/605 ,  C07K14/62 ,  G01N33/68

摘要： The present invention provides a method for acylating one or more amino groups of a peptide where the acylation reaction is to be performed in an aqueous mixture containing less than 10 %w/w aprotic polar solvent. a) reacting the peptide having at least one free amino group with an acylating agent of the general formula I wherein n, is 0-8 R1is COOR4; R2 is a lipophilic moiety; R3 together with the carboxyl group to which R3 is attached designate a reactive ester or a reactive N-hydroxy imide ester; and R4 is selected from hydrogen, C1-12-alkyl and benzyl, under basic conditions in an aqueous mixture;