235112-66-0Relevant articles and documents
Synthesis method of micafungin side chain intermediate
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, (2020/09/12)
The invention discloses a synthesis method of a micafungin side chain intermediate. An important side chain intermediate for synthesizing micafungin can be obtained through only three steps, and the steps are simple. Firstly, 4-pentoxyl acetophenone and methyl p-formylbenzoate as initial raw materials are subjected to an aldol condensation reaction under the action of an alkali catalyst cesium carbonate to obtain an intermediate M1; then, the intermediate M1 and N-hydroxyl p-toluenesulfonamide are cyclized under the action of the alkali catalyst cesium carbonate to obtain an intermediate M2; and finally, transesterification reaction is carried out on the intermediate M2 and 1-hydroxybenzotriazole to obtain the high-purity micafungin side chain intermediate shown in the formula M (See the specification). A brand-new synthesis route is provided, and a foundation is laid for preparation of a final product micafungin.
Practical synthesis of FR195752, the side chain of Micafungin, utilizing a regioselective conversion of diaryl-β-diketone to 3,5-diarylisoxazole
Ohigashi, Atsushi,Kanda, Atsushi,Tsuboi, Hiroyuki,Hashimoto, Norio
, p. 179 - 184 (2012/12/24)
The practical synthesis of FR195752, the side chain of Micafungin, was established utilizing a highly regioselective conversion of diaryl-β- diketone to 3,5-diarylisoxazole via the corresponding β-keto enamine intermediate whose disfavored regioisomer could be recycled efficiently after its hydrolysis. In addition, the related substance of FR195752 could be strictly controlled by the purification of its intermediate.
FK463, a novel water-soluble echinocandin lipopeptide: Synthesis and antifungal activity [1]
Tomishima,Ohki,Yamada,Takasugi,Maki,Tawara,Tanaka
, p. 674 - 676 (2007/10/03)
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