Intermediates for lhrh antagonist synthesis, process for...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/083 (2006.01) C07K 5/08 (2006.01) C07K 5/087 (2006.01) C07K 7/23 (2006.01)

Patent

CA 2471723

The novel tripeptides Ac-D-2Nal-D-4ClPh-D-3Pal-OH and Boc-D-2Nal-D-4ClPhe-D- 3Pal-OH are intermediates useful in the synthesis of LHRH analogs by coupling with suitable heptapeptides, in particular with the heptapeptides P1-Ser(P2)- NMeTyr(P3)-D-Lys(Nic)-Leu-Lys(iPr,P4)-Pro-D-AlaNH2 and P1-Ser(P2)-NMeTyr(P3)-D- Asn-Leu-Lys(iPr,P4)-Pro-D-AlaNH2.

Les nouveaux tripeptides Ac-D-2Nal-D-4ClPh-D-3Pal-OH et Boc-D-2Nal-D-4ClPhe-D-3Pal-OH sont des intermédiaires utilisés dans la synthèse d'analogues de la gonadolibérine (LHRH) par couplage avec des heptapeptides appropriés, notamment les heptapeptides P?1¿-Ser(P?2¿)-NMeTyr(P?3¿)-D-Lys(Nic)-Leu-Lys(iPr,P?4¿)-Pro-D-AlaNH¿2? et P?1¿-Ser(P?2¿)-NMeTyr(P?3¿)-D-Asn-Leu-Lys(iPr,P?4¿)-Pro-D-AlaNH¿2?.

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