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An efficient strategy for the large-scale synthesis of head-to-tail cyclic peptides

✍ Scribed by John X. He; Wayne L. Cody; Annette M. Doherty

Publisher
Springer Netherlands
Year
1994
Tongue
English
Weight
427 KB
Volume
1
Category
Article
ISSN
1573-3149

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✦ Synopsis

An efficient and generally applicable method for the synthesis of head-to-tail cyclic peptides with HBTU (2-( lHbenzotriazol-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 (ET,,) antagonist BQ-123 (cy&[-D-Trp-D-Asp-Pro-D-val-Leu-1). This methodology can be readily applied to the small-and largescale synthesis of other head-to-tail cyclic peptides.

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