申请人:Ichikawa Gosei Chemical Co., Ltd.
公开号:US05648534A1
公开(公告)日:1997-07-15
1,2-di-substituted indan expressed by general formula (I) wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, Y is a halogen atom, and X and Y can be in either cis- or trans-configuration forming either a racemic body or an optically active substance; or 1,2-di-substituted indan expressed by general formula (I') wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, and X and OH group can be in either cis- or trans-configuration forming either a racemic body or an optically-active substance; or cis-1,2-epoxyindan expressed by general formula (VI) wherein R is phenyl or a lower alkyl group, oxazoline ring is in cis-configuration forming either a racemic body or an optically active substance is reacted, under an acidic condition, with a nitrile expressed by general formula (II) wherein R is phenyl or a lower alkyl group to produce cis-1-aminoindan-2-ol expressed by general formula (V) wherein NH.sub.2 and OH groups are in cis-configuration forming either a racemic body or an optically-active substance. ##STR1##
通式(I)表示的1,2-二取代茚烷,其中X是一个取代基,在酸性条件下可以被提取出来形成茚烷骨架的1-位置上的碳正离子,Y是一个卤素原子,X和Y可以是顺式或反式构型,形成外消旋体或光学活性物质;或通式(I')表示的1,2-二取代茚烷,其中X是一个取代基,在酸性条件下可以被提取出来形成茚烷骨架的1-位置上的碳正离子,X和OH基团可以是顺式或反式构型,形成外消旋体或光学活性物质;或通式(VI)表示的顺-1,2-环氧茚烷,其中R是苯基或较低的烷基,噁唑环处于顺式构型,形成外消旋体或光学活性物质,在酸性条件下,与通式(II)表示的腈反应,其中R是苯基或较低的烷基,产生顺-1-氨基茚烷-2-醇,通式(V)表示,其中NH2和OH基团处于顺式构型,形成外消旋体或光学活性物质。