THE SYNTHESIS OF [C-14] PANTOPRAZOLE - SK-AND-F 96022Z - AN H+/K+ ATPASE INHIBITOR

被引:5
作者
CROWE, AM
JOHNSTON, CEA
LAWRIE, KWM
SAUNDERS, D
机构
[1] SmithKline Beecham Research, Welwyn, AL6 9AR, Frythe
[2] SmithKline Beecham Research, Harlow, Essex, CM19 5AD, Coldharbour road
[3] SmithKline Beecham Research, Harlow, Essex, CM19 5AD, Coldharbour road
关键词
C-14 H+/K+ ATPASE INHIBITOR; PANTOPRAZOLE; PROTON PUMP INHIBITOR; C-14; PYRIDINE; LITHIATION;
D O I
10.1002/jlcr.2580310511
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Pantoprazole 1, SK&F 96022Z, an H+/K+ ATPase inhibitor has been prepared, radiolabelled with carbon-14, in two positions, for drug metabolism studies. [Benzimidazole 2-C-14]pantoprazole in 4 steps from potassium ethyl, [C-14]xanthate, and [pyridylmethyl-C-14]pantoprazole from cuprous [C-14]cyanide in 8 steps. The overall radiochemical yields of these syntheses were 37.9% and 5.2% respectively.
引用
收藏
页码:409 / 416
页数:8
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