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由于13,14双氢 PG F_2α引人注目的生理活性,促使作者研究其相应的环丙基化合物即13,14双氢-13,14-次甲基前列腺素的合成。利用 Corey-中间体(I_a)以催化量醋酸钯和过量重氮甲烷试剂(Pd(OAc)_2/CH_2N_2]在双键上产生顺式加成,获得环丙酮化合物2a 和3a 混合物(2:1),产率92%。二者可用硅胶柱层析分开。2a 在异丙醇、四氢呋喃溶媒中,于0°用钠硼氢还原,得二个差向异构体的醇
Due to the striking physiological activity of 13,14 dihydrogen PG F_2α, the authors were prompted to study the synthesis of its corresponding cyclopropyl compound, 13,14 dihydro-13,14-methyleprostaglandin. The cis-addition of Corey-intermediate (I_a) to the double bond using a catalytic amount of palladium acetate and an excess of diazomethane reagent (Pd (OAc) 2 / CH_2N_2] gave a mixture of cyclopropanone compounds 2a and 3a ), Yield 92%, both separated by silica gel column chromatography.2a in isopropanol, tetrahydrofuran solvent, sodium borohydride reduction at 0 ° to give two epimers of alcohol