864416-19-3Relevant academic research and scientific papers
OPTICALLY ACTIVE 1-ARYL-2-FLUORO-SUBSTITUTED ETHYLAMINE AND METHOD FOR PRODUCING THE SAME
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Page/Page column 37-39, (2008/06/13)
PROBLEM TO BE SOLVED: To provide an optically active 1-aryl-2-fluoro-substituted ethylamine becoming an important intermediate of a candidate compound of a medicine and an agrochemical, and an industrial method for producing the same. SOLUTION: This method for producing optically active 1-aryl-2-fluoro-substituted ethylamine is provided by performing the dehydrating condensation of a fluoro-substituted methyl aryl ketone with an optically active 1-phenylethylamine in the presence of an acid catalyst to convert them to an optically active imine, further asymmetrically reducing the optically active imine to convert it to a mixture of optically active secondary amine diastereomers, inducing the diastereomer mixture of the optically active secondary amines to their salts and recrystallizing to obtain the optically active secondary amine having a high diastereomeric excess rate or its salt, and hydrolyzing the optically active secondary amine or its salt in the presence of a group VIII transition metal catalyst to obtain the optically active 1-aryl-2-fluoro-substituted ethylamine or its salt.
Asymmetric synthesis of α-monofluoromethyl- and α- difluoromethylbenzylamines through regioselective hydrogenolysis
Kanai, Masatomi,Ueda, Koji,Yasumoto, Manabu,Kuriyama, Yokusu,Inomiya, Kenjin,Ootsuka, Takashi,Katsuhara, Yutaka,Higashiyama, Kimio,Ishii, Akihiro
, p. 385 - 391 (2007/10/03)
Asymmetric synthesis of α-monofluoromethyl- and α- difluoromethylbenzylamines through regioselective hydrogenolysis is described. Hydrogenolysis of diastereomerically pure bis(α-methylbenzyl)amine derivatives having partially fluorinated methyl group at b
