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Synthesis of the tritium labelled ß-casomorphine analogues 3H-Phe-Pro-Gly-OH and 3H2-Tyr-Pro-3H-Phe-pyrrolidide

✍ Scribed by J. Oehlke; I. Born; K. Neubert; E. Mittag; H. Niedrich

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
365 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The precursor peptides H‐Phe(I)‐Pro‐Gly‐OH (III) and H‐Tyr(I~2~)‐Pro‐Phe(I)‐pyrrolidide (VIII) were synthesized by stepwise elongation from the C‐terminal end and by coupling of Boc‐Tyr(I~2~)‐Pro‐OH with H‐Phe(I)‐pyrrolidide and following deprotection of the Boc‐residue respectively. Catalytic dehalotritiation yielded tritated peptides with specific radioactivities of 450 and 1500 GBq/mmol respectively. Cleavage of ^3^H~2~‐Tyr‐Pro‐^3^H‐Phe‐pyrrolidide by dipeptidylpeptidase IV resulted in fragments with specific radioactivities of 950 (^3^H~2~‐Tyr‐Pro) and 590 GBq/mmol (^3^H‐Phe‐pyrrolidide).

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