552-85-2Relevant articles and documents
Smith et al.
, p. 978 (1977)
A NOVEL METHOD FOR SYNTHESIS OF OPTICALLY PURE BETA-AMINO ALCOHOLS
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, (2016/01/12)
A method for the preparation of β-amino alcohol of formula (III) in which R1 is Ph, (substituted) Ph, R2 is C1-8 alkyl or C4-6 cyclo alkyl, R3 = R4R5CHNH2 where, R4 = H, C1-8 alkyl, C4-6 cyclo alkyl, or - COOR6 (R6=C1-C8 alkyl); R5 = (subst) aryl], the method including subjecting an α-hydroxy ketone of formula (I) in which R1 and R2 are as defined above is reacted with a chiral amine of formula R3NH2 where R3 = R4R5CH- where, R4 = H, C1-8 alkyl, C4-6 cycloalkyl, or - COOR6 (R6=C1-8 alkyl), R5 = (subst) aryl] to produce a compound of formula (II) in which R1, R2 and R3 are as defined above, followed by reduction to form the compound of formula (III).
PROCESS FOR PRODUCING OPTICALLY ACTIVE s-AMINO ALCOHOL
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Page/Page column 22, (2008/06/13)
A process for easily producing an optically active β-amino alcohol useful as a pharmaceutical intermediate from an inexpensive, readily available starting material is provided. A readily available α-substituted ketone is reacted with an optically active amine to yield a diastereomer mixture of an optically active α-substituted aminoketone. One of the diastereomers is isolated optionally after the diastereomers are converted to salts with an acid. The optically active α-substituted aminoketone or a salt thereof thus isolated was stereoselectively reduced to yield an optically active β-substituted amino alcohol. The optically active β-substituted amino alcohol is subjected to hydrogenolysis to produce an optically active β-amino alcohol or a salt thereof.
