发明名称 PRODUCTION OF OPTICALLY ACTIVE ALPHA-SUBSTITUTED-BETA- AMINOKETONE DERIVATIVE
摘要 PROBLEM TO BE SOLVED: To directly produce an optically active α-substituted-β-aminoketone derivative from an optically inactive starting raw material by carrying out asymmetric Mannich reaction using a specific comples, a Lewis acid and a specific derivative. SOLUTION: (A) A synthetic zeolite, (B) a ketone and (C) an optically active aluminum-alkali metal-binaphthol complex of formula I, etc., are stirred and mixed in a solvent under an inert gas atmosphere and the mixture is reacted with (D) a Lewis acid of formula II (M is lanthanum, ytterbium or scandium; (m) is a positive number) and an α-aminoether derivative of formula III [R1 is a lower alkyl, phenyl or benzyl; R2 and R3 are each an (un)saturated lower alkyl or the like] to obtain the objective derivative of formula IV [R4 is a group of formula V (R7 is trifluoromethyl or a lower alkyl) or the like] having asymmetric structure induced at the α-position of the component B. The derivative has central muscle relaxing action.
申请公布号 JP2000072728(A) 申请公布日期 2000.03.07
申请号 JP19980238064 申请日期 1998.08.25
申请人 MITSUI CHEMICALS INC 发明人 YAMAZAKI SHINGO;IIDA TAKEHIKO;ARAI TAKAYOSHI;SHIBAZAKI MASAKATSU
分类号 C07D295/10;B01J31/22;C07B61/00;C07C221/00;C07C225/16;C07D261/08;C07D261/10;C07D275/02;C07D275/03 主分类号 C07D295/10
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