肤轻松中间体的微生物脱氢

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。

MICROBIOLOGICAL DEHYDROGENATION OF INTERMEDIATE OF FLUOCINANIDE ACETATE

Both compound I and II are intermediates in fluocinanide acetate synthesis. I could be dehydrogenated to II in 62% approximately 63% yields by Arthrobactor simplex No. A-1, 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 concentration 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 degrees C.