Tserng K Y, Klein P D
J Lipid Res. 1977 Jul;18(4):491-5.
The facile synthesis of lithocholic acids sulfates by a procedure that produced the desired products in over 90% yield is described. Lithocholic acid sulfate and glycolithocholic acid sulfate were synthesized by reacting lithocholic acid or glycolithocholic acid with sulfur trioxide-triethylamine complex in dimethylformamide for 0.5-1 hr. Taurolithocholic acid sulfate was obtained by conjugating lithocholic acid sulfate with taurine in dimethylformamide at 90 degrees C for 0.5 hr. The one-pot synthesis of taurolithocholic acid sulfate starting from lithocholic acid is also described. This procedure, which generated lithocholic acid sulfate in situ, produced taurolithocholic acid sulfate in 98% yield, compared to an overall yield of less than 10% obtained by previously published procedures.
本文描述了通过一种能以超过90%的产率得到所需产物的方法简便合成硫酸石胆酸。硫酸石胆酸和硫酸甘氨石胆酸是通过使石胆酸或甘氨石胆酸与三氧化硫 - 三乙胺络合物在二甲基甲酰胺中反应0.5 - 1小时合成的。硫酸牛磺石胆酸是通过在90℃下使硫酸石胆酸与牛磺酸在二甲基甲酰胺中缀合0.5小时获得的。还描述了从石胆酸一锅法合成硫酸牛磺石胆酸的方法。该方法原位生成硫酸石胆酸，硫酸牛磺石胆酸的产率为98%，而此前发表的方法的总产率不到10%。
