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METHOD FOR ASYMMETRICALLY CATALYZED SYNTHESIS OF NITROPYRAZOLE AMIDE COMPOUND
METHOD FOR ASYMMETRICALLY CATALYZED SYNTHESIS OF NITROPYRAZOLE AMIDE COMPOUND
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机译:非对称催化合成硝基吡唑酰胺化合物的方法
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摘要
A paroxetine intermediate, a method for preparing the same, and uses thereof are provided. Specifically, the method includes: reacting a compound of formula I below with a compound of formula II in the presence of an organic base under the catalysis of a complex formed from a chiral amine oxide L and a rare-earth metal compound Ln(OTf) 3 to prepare a compound of formula III below: wherein R 1 is alkyl, phenyl or benzyl; R 2 , R 3 , R 4 are each independently C 1 -C 6 alkyl or C 6 -C 10 aryl; the chiral amine oxide L has the following structure: wherein n = 1,2; and R = Ph-, 2,6-Me 2 C 6 H 3 -, 2,6-Et 2 C 6 H 3 -, 2,6-iPr 2 C 6 H 3 -, Ph 2 CH-.
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机译:提供了帕罗西汀中间体,其制备方法及其用途。具体地,该方法包括:在有机碱的存在下,在由手性氧化胺L和稀土金属化合物Ln(OTf)形成的络合物的催化下,使下式I的化合物与式II的化合物反应。 3制备下式III的化合物:其中R 1为烷基,苯基或苄基; R 2,R 3,R 4各自独立地为C 1 -C 6烷基或C 6 -C 10芳基;手性氧化胺L具有以下结构:其中n = 1,2; R = Ph-,2,6-Me 2 C 6 H 3-,2,6-Et 2 C 6 H 3-,2,6-iPr 2 C 6 H 3-,Ph 2 CH-。
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