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The synthesis of org 3770 labelled with 3 H, 13 C AND 14 C
Author(s) -
Kaspersen Frans M.,
Van Rooij Fons A. M.,
Sperling Eric G. M.,
Wieringa Joop H.
Publication year - 1989
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580270911
Subject(s) - chemistry , halogenation , tritium , chemical synthesis , stereochemistry , medicinal chemistry , radiochemistry , organic chemistry , biochemistry , physics , nuclear physics , in vitro
The syntheses of 1,2,3,4,10,14b‐hexahydro‐2‐methylpyrazino[2,1‐a]pyrido [2,3‐c][2]benzazepine (Org 3770) labelled with 3 H (and 2 H), 13 C and 14 C are described. Tritiated Org 3770 was prepared either by exchange under alkaline conditions with tritiated water or catalytic reductive dehalogenation of a chloro analogue with 3 H 2 . 13 C‐labelled material was obtained in a seven‐step synthesis starting from 13 C‐labelled benzene whereas 14 C‐Org 3770 was prepared in a three‐step synthesis starting with 14 CO 2 . All labelled compounds were analyzed by TLC, HPLC, MS and NMR.