硝酸依柏康唑的合成新方法
發(fā)布時(shí)間:2019-06-03 09:52
【摘要】:標(biāo)題化合物是一種外用廣譜抗真菌感染藥物,以鄰苯二甲酸酐和3,5-二氯苯乙酸為原料,首先經(jīng)縮合、催化加氫、環(huán)合3步反應(yīng)制備得到關(guān)鍵中間體2,4-二氯-10,11-二氫-5H-二苯并[a,d]環(huán)庚烯-5-酮,然后經(jīng)還原、氯化、N-烴基化、成鹽等4步反應(yīng)制備得到。該合成方法縮短了標(biāo)題化合物的合成路線,提高了總收率,不產(chǎn)生有機(jī)磷廢棄物,更適于工業(yè)化生產(chǎn)。
[Abstract]:The title compound is a broad-spectrum antifungal drug for external use. Phthalic anhydride and 3,5-dichlorophenylacetic acid are used as raw materials. The key intermediate 2, 4-dichloro-10, 11-dihydro-5H-dibenzo [a, d] cycloheptene-5-one was prepared by three-step cyclization, and then prepared by reduction, chlorination, N-alkylation and salt formation. The synthesis method shortens the synthesis route of the title compound, improves the total yield, does not produce organophosphorus waste, and is more suitable for industrial production.
【作者單位】: 蘇州健雄職業(yè)技術(shù)學(xué)院生物與化學(xué)工程系;
【基金】:江蘇省高!扒嗨{(lán)工程”資助項(xiàng)目 太倉市科學(xué)技術(shù)局項(xiàng)目(TC2014GY19)
【分類號】:R914.5
,
本文編號:2491859
[Abstract]:The title compound is a broad-spectrum antifungal drug for external use. Phthalic anhydride and 3,5-dichlorophenylacetic acid are used as raw materials. The key intermediate 2, 4-dichloro-10, 11-dihydro-5H-dibenzo [a, d] cycloheptene-5-one was prepared by three-step cyclization, and then prepared by reduction, chlorination, N-alkylation and salt formation. The synthesis method shortens the synthesis route of the title compound, improves the total yield, does not produce organophosphorus waste, and is more suitable for industrial production.
【作者單位】: 蘇州健雄職業(yè)技術(shù)學(xué)院生物與化學(xué)工程系;
【基金】:江蘇省高!扒嗨{(lán)工程”資助項(xiàng)目 太倉市科學(xué)技術(shù)局項(xiàng)目(TC2014GY19)
【分類號】:R914.5
,
本文編號:2491859
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