申请人:Gutheil G. William
公开号:US20080039612A1
公开(公告)日:2008-02-14
The present invention provides a process for preparing a peptide of formula (I):
Sub-[L]-[N(R
1
)-A-C(O)]
p
—[NH-A-C(O)]
n+m
—OH (I)
comprising: (a) reacting an immobilized compound of formula (II):
Sub-(L)-[N(R
1
)-A-C(O)]
p
—[NH-A-C(O)]
n
—OH (II)
with an amino acid ester or peptide derivative of formula (III):
H—[NH-A-C(O)]
m
—O(tBu) (III)
in the presence of a coupling agent to yield a peptide compound of general formula (IV):
Sub-[L]-[N(R
1
)-A-C(O)]
p
—[NH-A-C(O)]
n+m
—O(tBu) (IV);
(b) removing the tBu (t-butyl) group to produce a solid-support bound carboxylic acid or peptide derivative of general formula (I); wherein n is a positive integer, e.g., 1-10, preferably 1-5; m is a positive integer, and P is 0-1.