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METHODS FOR THE SYNTHESIS OF AMINES SUCH AS EPHEDRINE AND INTERMEDIATES

机译:合成如苯丙氨酸和中间体的胺的方法

摘要

A method for the preparation of a compound of formula (VI): in which RSUB2 /SUBis an optionally substituted C1-C6 alkyl; RSUB4 /SUBis H, OH, an optionally substituted C1-C6 alkyl or an optionally substituted C1-C6 alkoxy; RSUB5 /SUBis an optionally substituted aryl, an optionally substituted aralkyl, or an optionally substituted alkyl; and RSUB6 /SUBis H or an optionally substituted C1-C6 alkyl; the method including the step of subjecting a ketone of formula (V) in which RSUB2/SUB, RSUB4 /SUBand RSUB5 /SUBare as defined above, to reductive amination with an amine of formula RSUB3/SUBNHSUB2 /SUBin which RSUB3 /SUBis an optionally substituted alkyl, and a reductant to form the compound of formula (VI), wherein the reaction is conducted in the presence of a supercritical fluid or a liquefied gas.
机译:制备式(VI)化合物的方法:其中R 2 是任选取代的C1-C6烷基; R 4 为H,OH,任选取代的C1-C6烷基或任选取代的C1-C6烷氧基; R 5 是任选取代的芳基,任选取代的芳烷基或任选取代的烷基; R 6 为H或任选取代的C1-C6烷基;该方法包括使其中R 2 ,R 4 和R 5 如上定义的式(V)的酮的步骤,还原为式R 3 NH 2 的胺的还原胺化反应,其中R 3 是任选取代的烷基,并形成还原剂式(VI)的化合物,其中反应在超临界流体或液化气的存在下进行。

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