REGIOSPECIFIC DEUTERIATION AND TRITIATION OF VARIOUS DRUGS USING A HOMOGENEOUS RHODIUM TRICHLORIDE CATALYST

被引:47
作者
HESK, D
JONES, JR
LOCKLEY, WJS
机构
[1] FISONS PLC,DIV PHARMACEUT,RES & DEV LABS,BAKEWELL RD,LOUGHBOROUGH LE11 ORH,LEICS,ENGLAND
[2] UNIV SURREY,DEPT CHEM,GUILDFORD GU2 5XH,SURREY,ENGLAND
关键词
D O I
10.1002/jps.2600800917
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The deuteriation and tritiation of a number of drugs containing carboxyl, amide, aralkylamine, and anilide functional groups have been investigated using homogeneous rhodium trichloride as a catalyst. Good incorporation of deuterium was observed and the regiospecificity for ortho exchange was very high for most of the drugs studied. Similarly, with tritium, good incorporation (specific activities) and regiospecificities were achieved in many cases. Satisfactory results were also obtained from the small number of heterocyclic-containing drugs that were included in the present study.
引用
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页码:887 / 890
页数:4
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