An improved synthesis of [24-14C]cholic acid, and its application to the synthesis of [14C]SCH 209702 (Syn3).: Synthesis of [2H8]SCH 209702

被引:3
作者
Ren, Sumei [1 ]
McNamara, Paw [1 ]
Kahairski, Davd [1 ]
机构
[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA
关键词
24-(14)C]cholic acid; bile acid; SCH; 209702; Syn3; carbon-14; synthesis;
D O I
10.1002/jlcr.1509
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
An efficient synthesis of [24- (14)C]cholic acid from potassium [(14)C]cyanide has been developed. The key intermediate, 23-chloro-3 alpha, 7 alpha, 12 alpha-triformyloxynorcholane, was synthesized by degradation of triformyl protected cholic acid. Different degradation conditions were explored. The synthesis of [(14)C]SCH 209702 from 23-chloro-3 alpha, 7 alpha, 12 alpha-triformyloxynorcholane and potassium [(14)C]cyanide is described. The synthesis of [(2)H(8)]SCH 209702 from [(2)H(4)]cholic acid is also presented.
引用
收藏
页码:231 / 235
页数:5
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