Method for inverse solid phase synthesis of peptides
The present invention provides a process for preparing a peptide of formula (I): Sub-[L]-[NH-A-C(O)] n+m -OH (I) comprising: (a) reacting an immobilized compound of formula (II): Sub-(L)-[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...
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| Format: | Patent |
| Sprache: | eng |
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| Zusammenfassung: | The present invention provides a process for preparing a peptide of formula (I):
Sub-[L]-[NH-A-C(O)]
n+m
-OH (I)
comprising:
(a) reacting an immobilized compound of formula (II):
Sub-(L)-[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]-[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. |
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