ISSN:
1573-3904
Keywords:
BQ-123
;
Endothelin
;
Cyclic peptides
;
HBTU
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Summary An efficient and generally applicable method for the synthesis of head-to-tail cyclic peptides with HBTU (2-(1H-benzotriazol-1-yl)-1,1,3, 3-tetramethyluronium hexafluorophosphate) has been developed. The utility of this approach was exemplified with the multigram preparation of a potent endothelin receptor-selective (ETA) antagonist BQ-123 (cyclo[-d-Trp-d-Asp-Pro-d-Val-Leu-]). This methodology can be readily applied to the small-and largescale synthesis of other head-to-tail cyclic peptides.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00132759
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