Cohen B I, May P S, McSherry C K, Mosbach E H
Steroids. 1982 Dec;40(6):701-11. doi: 10.1016/0039-128x(82)90011-3.
Bile acid amides and oxazolines were synthesized by a sequence of steps involving the reaction of the free bile acid with formic acid to yield the formyloxy derivative, preparation of the formyloxy acid chloride, condensation of the acid chloride with 2-amino-2-methyl-1-propanol to give the amide and, finally, cyclization of the amide with thionyl chloride to give the oxazoline. The oxazolines were characterized by physical constants, thin layer and gas-liquid chromatography and identified by elemental analysis and gas-liquid chromatography-mass spectrometry. Some of the bile acid oxazoline derivatives alter the activity of bacterial 7-dehydroxylases in vitro, and inhibit the growth of certain anaerobic bacteria in pure culture.
胆汁酸酰胺和恶唑啉是通过一系列步骤合成的，这些步骤包括游离胆汁酸与甲酸反应生成甲酰氧基衍生物、制备甲酰氧基酰氯、酰氯与2-氨基-2-甲基-1-丙醇缩合得到酰胺，最后酰胺与亚硫酰氯环化得到恶唑啉。通过物理常数、薄层色谱和气液色谱对恶唑啉进行了表征，并通过元素分析和气液色谱-质谱进行了鉴定。一些胆汁酸恶唑啉衍生物在体外改变细菌7-脱羟基酶的活性，并抑制纯培养中某些厌氧菌的生长。
