Somatostatin analogs synthesis

Guggenberg von E, Mikolajczak R, Janota B et al (2004) Radiopharmaceutical development of a freeze-dried kit formulation for the preparation of [Tc-99m-EDDA-HYNIC-D-Phe(l),Tyr(3)]-oc-treotide, a somatostatin analog for tumor diagnosis. J Pharm Sciences 93 2497-2506 Harris TD, Sworin M, Williams N et al (1999) Synthesis of stable hydrazones of a hydrazinonicotinyl-modified peptide for the preparation of " Tc-labelled radiopharmaceuticals. Bioconjug Chem 10 808... 

D. F. Veber, Design of a highly active cyclic hexapeptide analog of somatostatin, in Peptides, Synthesis, Structure and Function. Proceedings of the Seventh American Peptide Symposium,... 

Reductive amination was the first method described for amine production on solid phase. It was first mentioned in 1987 by Coy et al. [260,261]. They used a combination of Na(CN)BH3 and HOAc for the subsequent reduction of intermediately formed imides in the synthesis of somatostatin octapep-tide analogs. Due to its early development, this alkylation method has found entry to the synthesis of diverse substance classes like N-terminal-modified peptides, carbohydrate mimetics [262], glycopeptides [263,264], oligonucleotides [265], and of course polyamines [174,175,222,232,248,266,267]. For the same reasons as the amide reduction approach, it is powerful enough to be used in the production of several compound libraries [177,262-264, 268]. 

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