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Facile solid phase synthesis of octreotide analogs using p-carboxybenzaldehyde as a novel linker to anchor Fmoc-threoninol to solid phase resins

✍ Scribed by Ying-Ta Wu; Hsing-Pang Hsieh; Chi-Yu Wu; Hui-Ming Yu; Shui-Tein Chen; Kung-Tsung Wang


Publisher
Elsevier Science
Year
1998
Tongue
French
Weight
138 KB
Volume
39
Category
Article
ISSN
0040-4039

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✦ Synopsis


A new procedure is described for the synthesis of octreotide and its analogs using p-carboxybenzaidehyde as a linker to anchor Fmoc-threoninol to solid phase resins. Fmoc-threoninol reacted with p-carboxybenzaldehyde to form Fmocthreoninol p-carboxybenzacetal in 95% yield. The Fmoc-threoninol pcarboxybenzacetal was coupled to an amine-resin and octreotides were successfully synthesized with yields of 74-76%.