| 摘要 |
<p>1329618 Peptides FARBWERKE HOECHST AG 29 Oct 1970 [31 Oct 1969] 51462/70 Heading C2C A peptide (I) X-Tyr-Ser-Met-Glu-His-Phe- Arg - Trp - Gly - Lys - Pro - Val - Gly - Lys - Lys- Y - NH - (CH 2 ) n - NH 2 in which X is a #- alanyl,γ-aminobutyryl, D-seryl, #-hydroxypropionyl or n-alkoxycarbonyl residue (alkyl containing 1-4 C), Y is lysine or ornithine and n is 2-6, are prepared by reacting A-Tyr-Ser- Met - Glu(OtBu) - His - Phe - Arg - Tyr - GlyOH in which A is BOC-#-alanyl, BOC-y-aminobutyryl, BOC-D-seryl, #-hydroxypropionyl or n-alkoxycarbonyl with H-Lys(BOC)-Pro-Val- Gly - Lys(BOC) - Lys(BOC) - Y(BOC) - NH- (CH 2 ) n -NHBOC in the presence of a carbodiimide and a component capable of forming an active ester and of pK of 4-8, and subsequently removing the protective groups by strong acid. The following starting materials are prepared: Z- and H-Lys(BOC)NH-(CH 2 ) 4 -NH-BOC, Z- and H-Lys(BOC)-Pro-Val-Gly-Lys(BOC)Lys- (BOC) - Lys(BOC)NH-(CH 2 ) 4 NHBOC, #- hydroxypropionyl - Tyr - Ser - Met - Glu(OtBu)- His - Phe - Arg - Trp - Gly - OH, EtOC - Tyr- Ser - Met - Glu(OtBu) - His - Phe - Arg - Trp- GlyOH, BOC -γ- Abu - Tyr - Ser - Met - Glu- (OtBu) - His - Phe - Arg - Trp - GlyOH, Z- and H-Orn(BOC)-NHCH 2 CH 2 NHBOC, Z - Lys- (BOC) - Pro - Val - Gly - Lys(BOC) - Lys(BOC)- Orn(BOC)NH(CH 2 ) 2 NHBOC, Z- and H-Lys- (BOC) - NH(CH 2 ) 6 NHBOC and BOC - NH- (CH 2 ) n - NHBOC, where n is 2, 3, 4, 5 and 6. Pharmaceutical compositions having ACTH activity contain peptides (I) and a carrier.</p> |
