Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne
摘要:
A new strategy was developed to prepare in a very efficient and convergent manner C-terminal modified tripeptides with high affinities for the Grb2-SH2 domain. Using Pd(PPh3)(2)Cl-2 as catalyst, selected naphthyl iodides and triflates were coupled to Ac-Pmp(t-Bu)(2)-Ac(6)c-Asn-NH(prop-2-ynyl). The resulting alkyne derivatives were hydrogenated and deprotected to afford potent Grb2-SH2 inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.
Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne
摘要:
A new strategy was developed to prepare in a very efficient and convergent manner C-terminal modified tripeptides with high affinities for the Grb2-SH2 domain. Using Pd(PPh3)(2)Cl-2 as catalyst, selected naphthyl iodides and triflates were coupled to Ac-Pmp(t-Bu)(2)-Ac(6)c-Asn-NH(prop-2-ynyl). The resulting alkyne derivatives were hydrogenated and deprotected to afford potent Grb2-SH2 inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.
A new strategy was developed to prepare in a very efficient and convergent manner C-terminal modified tripeptides with high affinities for the Grb2-SH2 domain. Using Pd(PPh3)(2)Cl-2 as catalyst, selected naphthyl iodides and triflates were coupled to Ac-Pmp(t-Bu)(2)-Ac(6)c-Asn-NH(prop-2-ynyl). The resulting alkyne derivatives were hydrogenated and deprotected to afford potent Grb2-SH2 inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.