Timmons C, McPherson L M, Chen D, Wei H-X, Li G
Department of Chemistry and Biochemistry, Texas Tech University, Lubbock, TX 79409-1061, USA.
J Pept Res. 2005 Nov;66(5):249-54. doi: 10.1111/j.1399-3011.2005.00294.x.
Manganese (IV) oxide was found to catalyze the diamination reaction of alpha,beta-unsaturated esters and ketones with N,N-dichloro-p-toluenesulfonamide and acetonitrile as the halogen and nitrogen sources. The reaction is convenient to be conducted by simply mixing three reactants in the presence of manganese dioxide catalyst and 4 A molecular sieves, and provides an easy access to 1-p-toluenesulfonyl-3-trichloromethyl-4,5-imidazoline derivatives, which are useful building blocks for peptidomimetic studies.
发现二氧化锰可催化α,β-不饱和酯和酮与N,N-二氯对甲苯磺酰胺及乙腈(作为卤素和氮源)的双胺化反应。该反应操作简便,只需在二氧化锰催化剂和4A分子筛存在下将三种反应物简单混合即可进行,并能方便地得到1-对甲苯磺酰基-3-三氯甲基-4,5-咪唑啉衍生物,这些衍生物是用于拟肽研究的有用构件。