Heeres J, Mostmans J H, Cutsem J V
J Med Chem. 1977 Nov;20(11):1511-6. doi: 10.1021/jm00221a032.
Synthesis of 1-[2-(arylalkyl)-2-phenylethyl]-1H-imidazoles was accomplished starting from the corresponding phenylacetonitriles. Via successive alkylation, conversion to the corresponding ester, and sodium borohydride-lithium iodide reduction, beta-phenylalcanols were obtained. These alcohols were mesylated and then refluxed with imidazole in dimethylformamide to yield the title compounds, which were active in vitro against dermatophytes, yeasts, other fungi, and gram-positive bacteria. Some were also active in vivo against Candida albicans.
1-[2-(芳基烷基)-2-苯乙基]-1H-咪唑的合成是从相应的苯乙腈开始的。通过连续烷基化、转化为相应的酯以及硼氢化钠-碘化锂还原反应，得到了β-苯烷醇。这些醇经甲磺酰化，然后在二甲基甲酰胺中与咪唑回流，得到标题化合物，它们在体外对皮肤癣菌、酵母、其他真菌和革兰氏阳性菌具有活性。一些化合物在体内对白色念珠菌也有活性。
