A new procedure is described for the synthesis of octreotide and its analogs using p-carboxybenzaldehyde as a linker to anchor Fmoc-threoninol to solid phase resins. Fmoc-threoninol reacted with p-carboxybenzaldehyde to form Fmoc-threoninol p-carboxybenzacetal in 95% yield. The Fmoc-threoninol p- carboxybenzacetal was coupled to an amine-resin and octreotides were successfully synthesized with yields of 74-76%.
All Science Journal Classification (ASJC) codes
- Drug Discovery
- Organic Chemistry