【摘要】 <正> 我们曾报道从全合成前列腺素(PG)F2α的中间体(Ⅰα)出发,合成了(15S)-15-甲基PGF2α甲酯(Ⅱ2)及其15-差向异构体(Ⅱb)。(Ⅱ2)与(Ⅱb)混合物经宫腔给予患持久黄体不育症奶牛,0.5～3毫克即有显著治疗作用;从阴道给予中期妊娠孕妇,5毫克左右即有相当满意的流产作用,且用法简便,其终止早期妊娠试验正在进行中。更多还原

【Abstract】 A convenient synthetic method for d,1-4β-[3’-oxo-transocten-(l’)]- 5α benzoyloxy-3,3aβ,4,5,6, 6aβ-hexahydro-2H-cycloponta [b]furan- 2-one (Ⅰb),an important intermediate for 15-methyl-PGF2α,was reported. Methanolysis of product (Ⅳ) in the presence of anhydrous potassium carbonate led to lactone diol (Ⅴ) in 80% yield. Both products (Ⅳ) and (Ⅴ) were identified with spectroscopy and compared with authentic samples of (Ⅷ).Selective blocking of the primary hydroxy group of (Ⅴ) was carried out by treating with trimethylsilyldi- ethylamine at - l0°in anhydrous acetone or pyridine.Benzoylation and subsequent removal of the prim-blocking group yielded (Ⅶa). The structure of (Ⅶa) was compared with spectroscopy to that of (Ⅷ). The overall yield of (Ⅶa) from (Ⅴ) was about 40%.Oxidation of (Ⅶa) under mild acidic condition furnished an aldehyde,which was subjected to Horner-Emmous-Wittig reaction with sodium salt of diethyl 2-oxoheptylphosphonate to give the tit1e compound (Ⅰb).更多还原