Patent ID: 6528686
Filing Date: 2003-03-04
Classification: C07C,C12P,Y02P,Y10S

Abstract:
A process for producing an (R,R)-1-phenyl-2-[(2-phenyl-1-alkylethyl)amino]ethanol derivative shown by the formula (XI) wherein R1, R2, R3, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom, an optionally substituted lower alkyl group, a hydroxyl group which may be protected with a protective group, an optionally substituted alkoxy group, an optionally substituted cycloalkyloxy group, an optionally substituted aralkyloxy group, an optionally substituted aryloxy group, an optionally substituted lower alkylthio group, an optionally substituted acyl group, a carboxyl group which may be protected with a protective group, an optionally substituted lower alkoxycarbonyl group, a nitro group or an optionally substituted amino group; and Z represents a hydrogen atom or a protective group for hydroxyl group; R7 and R8 represent, (A) respectively, a group selected from the group consisting of a hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aralkyl group, an optionally substituted aryl group, an optionally substituted acyl group, an optionally substituted lower alkoxycarbonyl group, an optionally substituted amino group, an optionally substituted alkylsulfonyl group, an optionally substituted arylsulfonyl group and a hydroxyl group which may be protected with a protective group, or (B) R7 represents a group shown by the formula (IX): â€”Oâ€”R7a, and R8 represents a group shown by the formula (X): â€”Oâ€”R8a, wherein R7a and R8a may form an optionally substituted ring with the adjacent oxygen atoms; R6, R9 and R10 independently represent a group selected from a group consisting of a hydrogen atom, a halogen atom, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aralkyl group, an optionally substituted aryl group, a hydroxyl group which may be substituted with a protective group, an optionally substituted alkoxy group, an optionally substituted cycloalkyloxy group, an optionally substituted aralkyloxy group, an optionally substituted aryloxy group, an optionally substituted lower alkylthio group, an optionally substituted aralkylthio group, an optionally substituted acyl group, an optionally substituted lower alkoxycarbonyl group, a nitro group and an optionally substituted amino group; and R11 represents a lower alkyl group, which comprises: a reaction of an (R)-2-amino-1-phenylethanol compound shown by the formula (II) â€ƒwherein R1, R2, R3, R4, R5 and Z have the same meanings as defined above, or a salt thereof, with a compound shown by the formula (VIII) â€ƒwherein R6, R7, R8, R9, R10 and R11 have the same meanings as defined above, and a reducing reaction of the reaction product of said reaction, wherein the reducing reaction is conducted in the presence of an acid catalyst selected from inorganic acids and aliphatic mono- or di-carboxylic acid.