FACILE SOLID-PHASE SYNTHESIS OF OCTREOTIDE ANALOGS USING P-CARBOXYBENZALDEHYDE AS A NOVEL LINKER TO ANCHOR FMOC-THREONINOL TO SOLID-PHASE RESINS

Authors
WU YT HSIEH HP WU CY YU HM CHEN ST WANG KT
Citation
Yt. Wu et al., FACILE SOLID-PHASE SYNTHESIS OF OCTREOTIDE ANALOGS USING P-CARBOXYBENZALDEHYDE AS A NOVEL LINKER TO ANCHOR FMOC-THREONINOL TO SOLID-PHASE RESINS, Tetrahedron letters, 39(13), 1998, pp. 1783-1784
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Tetrahedron letters → ACNP
ISSN journal
00404039
Volume
39
Issue
13
Year of publication
1998
Pages
1783 - 1784
Database
ISI
SICI code
0040-4039(1998)39:13<1783:FSSOOA>2.0.ZU;2-K
Abstract
A new procedure is described for the synthesis of octreotide and its a nalogs using p-carboxybenzaldehyde as a linker to anchor Fmoc-threonin ol to solid phase resins. Fmoc-threoninol reacted with p-carboxybenzal dehyde to form Fmoc-threoninol p-carboxybenzacetal in 95% yield. The F moc-threoninol p-carboxybenzacetal was coupled to an amine-resin and o ctreotides were successfully synthesized with yields of 74-76%. (C) 19 98 Elsevier Science Ltd. All rights reserved.