Preparation method of posaconazole important intermediate

The invention provides a preparation method of a posaconazole important intermediate. A synthesis route is as follows: a formula is shown in the description. The preparation method comprises the specific preparation steps: (1) adding a compound III into an aprotic solvent; in the presence of an acid...

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Hauptverfasser: YANG HANXIN, SHA WEI, LIANG JIANHUA, MA ZONGPU, LI TING
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides a preparation method of a posaconazole important intermediate. A synthesis route is as follows: a formula is shown in the description. The preparation method comprises the specific preparation steps: (1) adding a compound III into an aprotic solvent; in the presence of an acid binding agent, dropwise adding benzyl chloroformate at 0 to 5 DEG C; reacting at 20 DEG C to 25 DEGC for 1h to 8h; after reacting, adding 1 to 5 times of purified water into a reaction system; crystallizing in an ice water bath for 3h to 5h; filtering and drying to obtain a compound II; (2) underthe protection of nitrogen gas, adding the compound II into toluene or ethylene glycol dimethyl ether; then adding the acid binding agent and a compound IV in sequence; carrying out reflowing reactionfor 12h to 48h; after reacting, filtering while the product is hot; crystallizing at 0 to 10 DEG C for 1h to 5h; filtering and drying to obtain the intermediate I. 种泊沙康唑重要中间体的制备方法,合成路线如下:具体制备步骤如下:(1)将化合物III加入到非质子溶剂中,在缚酸剂的存在下,在