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Synfacts 2022; 18(04): 0445
DOI: 10.1055/s-0041-1737550
Peptide Chemistry

5-Nitro-4,6-dithiocyanatopyrimidine: A Novel Coupling Reagent for Peptide Synthesis

Contributor(s):
Hisashi Yamamoto
,
Isai Ramakrishna
Li Y, Li J, Bao G, Yu C, Liu Y, He Z, Wang P, Ma W, Xie J, Sun W, *, Wang R. * Lanzhou University and Institute of Materia Medica, Beijing, P. R. of China
NDTP Mediated Direct Rapid Amide and Peptide Synthesis without Epimerization.

Org. Lett. 2022;
24: 1169-1174
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Key words

coupling agents - amino acid activation - nitrodithiocyanato-pyrimidine - solid-phase synthesis

Significance

The development of novel and practically viable methods for forming peptide bonds is in high demand for peptide drug discovery. The authors have developed 5-nitro-4,6-dithiocyanatopyrimidine (NDTP) as a powerful coupling agent for peptide synthesis.


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Comment

NDTP-mediated peptide bond-forming reactions proceeded smoothly to deliver a series of peptides in high yields with excellent selectivities. NDTP is a mild, nonirritant, conveniently available, and recyclable reagent. Moreover, it is also compatible with Fmoc solid-phase peptide synthesis.


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Publication History

Article published online:
18 March 2022

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