Method for preparing (R)-(+)-N-acetyl-1-methyl-3-amphetamine at high temperature

The invention discloses a method for preparing (R)-(+)-N-acetyl-1-methyl-3-amphetamine at a high temperature. The method comprises the following steps: by taking 1-methyl-3-amphetamine as a substrateand immobilized lipase Novozym435 as a catalyst, adding an organic solvent and an acylation reagent,...

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Hauptverfasser: LIU BO, LU YUAN, TANG LAN, OU ZHIMIN, DAI HONGQIAN, DU LIHUA
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a method for preparing (R)-(+)-N-acetyl-1-methyl-3-amphetamine at a high temperature. The method comprises the following steps: by taking 1-methyl-3-amphetamine as a substrateand immobilized lipase Novozym435 as a catalyst, adding an organic solvent and an acylation reagent, and carrying out resolution reaction for 2-10 hours under the magnetic stirring conditions of 40-80DEG C and 1000rpm; and after the reaction is finished, separating and purifying a reaction solution to obtain (R)-(+)-N-acetyl-1-methyl-3-amphetamine. The substrate in the reaction provided by the invention achieves a conversion rate of 35.6% (the highest resolution reaction conversion rate is 50%) only in 4 hours, and the ee value of the R-configuration product achieves 98.3%. The used lipase isgranular immobilized lipase, and can be easily and quickly separated from the reaction solution. 本发明公开了一种高温下制备(R)-(+)-N-乙酰基-1-甲基-3-苯丙胺的方法,所述方法为:以1-甲基-3-苯丙胺为底物,以固定化脂肪酶Novozym435为催化剂,加入有机溶剂和酰化试剂,在40-80℃、1000rpm磁力搅拌条件下拆分反应2-10h,反