A novel synthetic route to ethyl 3-substituted-trans-2,3-difluoro-2-acrylates and their reactions with nucleophiles
作者:Qisheng Zhang、Long Lu
DOI:10.1016/s0040-4039(00)01517-3
日期:2000.10
Reaction of a variety of trans-1-trimethylsilyl-1,2-difluoroalkenes with ethyl chloroformate in the presence of potassium fluoride gave the corresponding ethyl 3-substituted-trans-2,3-difluoro-2-acrylates in good yields, which reacted with a variety of nucleophiles such as hydrazine hydrate, amidines and thiourea etc. in the presence of bases to afford the corresponding 4-fluoropyrazole, 5-fluoropyrimidine
在氟化钾的存在下,各种反式-1-三甲基甲硅烷基-1,2-二氟烯烃与氯甲酸乙酯反应,得到相应的3-取代的-反式-2,3-二氟-2-丙烯酸乙酯,它们反应了在碱存在下,用多种亲核试剂如水合肼,am和硫脲等与亲核试剂反应,以高收率得到相应的4-氟吡唑,5-氟嘧啶和5-氟-2-尿嘧啶衍生物。