Department of Chemistry, The Johns Hopkins University, 3400 N. Charles Street, Baltimore, Maryland 21218, United States.
J Org Chem. 2011 Oct 7;76(19):8121-5. doi: 10.1021/jo201561t. Epub 2011 Aug 31.
5-(Z)-alkylidene-2-thioxo-1,3-thiazolidin-4-ones (rhodanine derivatives) were prepared by reaction of in situ generated dithiocarbamates with recently reported racemic α-chloro-β,γ-alkenoate esters. This multicomponent sequential transformation performed in one reaction flask represents a general route to this medicinally valuable class of sulfur/nitrogen heterocycles. Using this convergent procedure, we prepared an analogue of the drug epalrestat, an aldose reductase inhibitory rhodanine.
5-(Z)-亚烷基-2-硫代-1,3-噻唑烷-4-酮（罗昔丹衍生物）是通过原位生成的二硫代氨基甲酸盐与最近报道的外消旋α-氯代-β,γ-烯酸酯反应制备的。这种在一个反应烧瓶中进行的多组分顺序转化代表了通向这种具有医学价值的硫/氮杂环的一般途径。使用这种收敛程序，我们制备了药物依帕司他的类似物，一种醛糖还原酶抑制性罗昔丹。
