INTERMEDIATES FOR LHRH ANTAGONIST SYNTHESIS, PROCESS FOR THE PRODUCTION, AND PROCESS FOR LHRH ANTAGONIST PRODUCTION
申请人:Rasmussen Jon H.
公开号:US20080306242A1
公开(公告)日:2008-12-11
The peptides Ac-D-2Nal-D-4ClPhe-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 P
1
-Ser(P
2
)-MMeTry(P
3
)-D-Lys(Nic)-Leu-Lys(iPr,P
4
)-Pro-D-AlaNH
2
and P
1
-Ser(P
2
)-NMeTry(P
3
)-D-Asn-Leu-Lys(iPr,P
4
)-Pro-D-AlaNH
2
.
肽类Ac-D-2Nal-D-4ClPhe-D-3Pal-OH和Boc-D-2Nal-D-4ClPhe-D-3Pal-OH是在与适当的七肽耦合时有用的中间体,特别是与七肽P1-Ser(P2)-MMeTry(P3)-D-Lys(Nic)-Leu-Lys(iPr,P4)-Pro-D-AlaNH2和P1-Ser(P2)-NMeTry(P3)-D-Asn-Leu-Lys(iPr,P4)-Pro-D-AlaNH2耦合时,在LHRH类似物的合成中。