Total solid-phase synthesis of 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid-functionalized peptides for radioimmunotherapy

James J. Peterson; Roger H. Pak; Claude F. Meares

doi:10.1021/bc980118t

Total solid-phase synthesis of 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid-functionalized peptides for radioimmunotherapy

James J. Peterson, Roger H. Pak, Claude F. Meares

Chemistry

Research output: Contribution to journal › Article › peer-review

44 Scopus citations

Abstract

A convenient approach to the functionalization of peptides with the macrocyclic 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA) moiety has been developed. Protected components (using tert-butyl or tert-butyloxycarbonyl groups) of both the peptide and the chelate were assembled on the same solid resin support. Deprotection and cleavage of the resin-bound DOTA-peptides were performed in one step using a trifluoroacetic acid cleavage mixture to yield free DOTA-peptide amides.

Original language	English (US)
Pages (from-to)	316-320
Number of pages	5
Journal	Bioconjugate Chemistry
Volume	10
Issue number	2
DOIs	https://doi.org/10.1021/bc980118t
State	Published - Mar 1999

ASJC Scopus subject areas

Chemistry(all)
Organic Chemistry
Clinical Biochemistry
Biochemistry, Genetics and Molecular Biology(all)
Biochemistry

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10.1021/bc980118t

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abstract = "A convenient approach to the functionalization of peptides with the macrocyclic 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA) moiety has been developed. Protected components (using tert-butyl or tert-butyloxycarbonyl groups) of both the peptide and the chelate were assembled on the same solid resin support. Deprotection and cleavage of the resin-bound DOTA-peptides were performed in one step using a trifluoroacetic acid cleavage mixture to yield free DOTA-peptide amides.",

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AU - Pak, Roger H.

AU - Meares, Claude F.

PY - 1999/3

Y1 - 1999/3

N2 - A convenient approach to the functionalization of peptides with the macrocyclic 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA) moiety has been developed. Protected components (using tert-butyl or tert-butyloxycarbonyl groups) of both the peptide and the chelate were assembled on the same solid resin support. Deprotection and cleavage of the resin-bound DOTA-peptides were performed in one step using a trifluoroacetic acid cleavage mixture to yield free DOTA-peptide amides.

AB - A convenient approach to the functionalization of peptides with the macrocyclic 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA) moiety has been developed. Protected components (using tert-butyl or tert-butyloxycarbonyl groups) of both the peptide and the chelate were assembled on the same solid resin support. Deprotection and cleavage of the resin-bound DOTA-peptides were performed in one step using a trifluoroacetic acid cleavage mixture to yield free DOTA-peptide amides.

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ER -

Total solid-phase synthesis of 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid-functionalized peptides for radioimmunotherapy

Abstract

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