| 摘要 |
A process for preparing enantiomer-pure cis1-amino-2-hydroxyindane is characterised in that: (a) racemic trans1-aminoindan-2-ol is reacted according to known processes with acids or acid derivatives having the general formula RCOX, yielding type (A) amides, in which the substituents have the following meanings: R stands for hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl and phenyl, groups that may carry one to three halogen atoms and/or one to three among the following residues: cyano, C1-C6 alkoxy, C1-C6 alkylthio phenyl, phenylthio and phenoxy, the phenyl residues in turn carrying one to three among the following groups: C1-C4 alkyl, C1-C4 alkoxy, halogen, cyano and nitro; X stands for OH, halogen, OR1 and SR1, in which R1 stands for alkyl C1-C6, phenyl and COR. In a second step (b), a supersaturated solution or melt of racemic amide (A) is blended with seed crystals of an enantiomer, then (c) the precipitated crystals are isolated and the remaining mother liquor or melt is again supersaturated, after separation of racemic amide (A), and blended with seed crystals of the other enantiomer in order to selectively crystallise said enantiomer. Finally (d), the thus obtained enantiomer-pure transamide is reacted according to known methods to yield enantiomer-pure cis1-amino-2-hydroxyindane.
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