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Synthesis of 3 H, 14 C and 2 H 4 labelled SCH 211803
Author(s) -
Hesk D.,
Voronin K.,
McNamara P.,
Royster P.,
Koharski D.,
Hendershot S.,
Saluja S.,
Truong V.,
Chan T. M.
Publication year - 2007
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.1206
Subject(s) - chemistry , yield (engineering) , tritiated water , nuclear chemistry , radiochemistry , specific activity , tritium , formaldehyde , carbon 14 , medicinal chemistry , organic chemistry , materials science , nuclear physics , metallurgy , enzyme , quantum mechanics , physics
[ 3 H]SCH 211803, at a specific activity of 1.56 Ci/mmol, was prepared by direct exchange with tritiated water and platinum metal. [ 2 H 4 ]SCH 211803 was prepared from [ 2 H]formaldehyde in a seven step synthesis in 10% yield. [ 14 C]SCH 211803 was prepared from N ‐benzyl‐4‐hydroxy[2‐ 14 C]piperidine in a four‐step synthesis in 35% radiochemical yield. Additionally a high specific activity batch of [ 3 H]SCH 211803 was prepared by Ru(Ph 3 P) 3 Cl 2 catalysed exchange with 90 at% tritiated water to a specific activity of 35 Ci/mmol. Copyright © 2007 John Wiley & Sons, Ltd.