PURPOSE: To effectively obtain an optically active deriv., for a synthesizing raw material of biotin, etc., by asymmetrically hydrogenating the specified furoimidazole derivs. with hydrogen in the presence of a homogeneous catalyst comprising Rh complex and the specified chiral phosphine ligands.
CONSTITUTION: The objective diastereomeric dihydrofuroimidazole deriv., for a synthesizing raw material of (+)-biotin(vitamin H) represented by formula VI, is obtained by an asymmetric hydrogenation of furoimidazole deriv. of formula I (wherein R1 is protective group leavable by a known method; R2 is H or a protective group leavable by a known method) with hydrogen in the presence of a homogeneous catalyst comprising Rh complex and chiral phosphine ligands such as a compd. of formula II (R3a, R3b, R4a and R4b are 1-12C alkyl, 5-7C cycloalkyl or 6-12C aryl), formula III (R5 and R7 are the same as R3a; R6 is 1-4C alkoxy or 1-4C dialkylamino), formula IV (R8a, R8b, R9a and R9b are the same as R3a; R10 is H or NH2 protective group) or formula V (R11a, R11b, R12a and R12b are the same as R3a) or the like.
FUERITSUKUSU SHIYUPINDORAA
RUDORUFU FUTSUKUSU
MARUTEIN AIAA
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