| 摘要 |
The present invention provides a process for preparing a peptide of formula (I): <?in-line-formulae description="In-line Formulae" end="lead"?>Sub-[L]-[N(R<SUP>1</SUP>)-A-C(O)]<SUB>p</SUB>-[NH-A-C(O)]<SUB>n+m</SUB>-OH (I) <?in-line-formulae description="In-line Formulae" end="tail"?> comprising: (a) reacting an immobilized compound of formula (II): <?in-line-formulae description="In-line Formulae" end="lead"?>Sub-(L)-[N(R<SUP>1</SUP>)-A-C(O)]<SUB>p</SUB>-[NH-A-C(O)]<SUB>n</SUB>-OH (II) <?in-line-formulae description="In-line Formulae" end="tail"?> with an amino acid ester or peptide derivative of formula (III): <?in-line-formulae description="In-line Formulae" end="lead"?>H-[NH-A-C(O)]<SUB>m</SUB>-O(tBu) (III) <?in-line-formulae description="In-line Formulae" end="tail"?> in the presence of a coupling agent to yield a peptide compound of general formula (IV): <?in-line-formulae description="In-line Formulae" end="lead"?>Sub-[L]-[N(R<SUP>1</SUP>)-A-C(O)]<SUB>p</SUB>-[NH-A-C(O)]<SUB>n+m</SUB>-O(tBu) (IV); <?in-line-formulae description="In-line Formulae" end="tail"?> (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.
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