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出 处:《药学学报》1989年第1期22-26,共5页Acta Pharmaceutica Sinica
摘 要:化合物Ⅰ和Ⅱ是制备醋酸肤轻松的中间体。用我们实验室选得的Arthrobactor simplex No.A-1可将Ⅰ脱氢生成Ⅱ,收率一般为62~63%,最高可超过70%。当底物Ⅰ的浓度为0.1%时,转化速度很快,没有任何产物累积。当浓度增加到0.2%时,除了得到少量Ⅱ外还可测出四种转化中间体Ⅳ,Ⅴ,Ⅵ,Ⅶ。而当底物Ⅰ浓度增加到0.5%时,并加入B-CS缓冲液及4%乙醇(95%,Ⅴ/Ⅴ),化合物Ⅱ以长方体结晶形式生成。在此条件下,其收率最稳定,熔点在250℃以上。Both compound Ⅰ and Ⅱ are intermediates in fluocinanide acetate synthesis. Ⅰ could be dehydrogenated to Ⅱ in 62%~63% yields by Arthrobactor simplex No. A-l, which was selected in our laboratory. When concentration of Ⅰ was 0.1%, it was transformed so fast that Ⅱ could not be accumulated. When concentraction was increased to 0.2%,four intermediates Ⅳ,Ⅴ,Ⅵ and Ⅶ were formed in addition to a little amount of product Ⅱ.When concentration of substrate Ⅰ was increased to 0.5% and B-CS buffer solution and 4% alcohol (95%, Ⅴ/Ⅴ) were added, compound Ⅱ in cuboidal microcrystalline form was obtained. Under this condition, the yield was steady and melting point was above 250℃.
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