Process for preparing optically active threonine
    62.
    发明授权
    Process for preparing optically active threonine 失效
    光学活性苏氨酸制备方法

    公开(公告)号:US4906773A

    公开(公告)日:1990-03-06

    申请号:US287434

    申请日:1988-12-21

    摘要: A process for preparing optically active threonine is disclosed, which comprises asymmetrically hydrogenating a 2-N-acylaminoacetoacetic ester represented by formula (I): ##STR1## wherein R.sup.1 represents a lower alkyl group, a phenyl group, a phenyl group substituted with a lower alkyl group or a lower alkoxy group, a benzyl group, or a benzyl group substituted with a lower alkyl group or a lower alkoxy group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a phenyl group, a phenyl group substituted with a lower alkyl group or a lower alkoxy group, a benzyloxy group, or a benzyloxy group substituted with a lower alkyl group or a lower alkoxy group, in the presence of a ruthenium-optically active phosphine complex as a catalyst to obtain an optically active threonine derivative represented by formula (II): ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, and then hydrolyzing the compound of formula (II). The 2-N-acylaminoacetoacetic ester intermediate can be selectively prepared in a high yield. Either natural type threonine or non-natural type threonine can be prepared selectively by selecting the absolute configuration of the ligand of the ruthenium-optically active phosphine complex.

    Process for preparing N-acyltetrahydroisoquinoline
    63.
    发明授权
    Process for preparing N-acyltetrahydroisoquinoline 失效
    制备N-酰基四氢异喹啉的方法

    公开(公告)号:US4851537A

    公开(公告)日:1989-07-25

    申请号:US38571

    申请日:1987-04-15

    CPC分类号: C07D217/06 C07D217/20

    摘要: A process for preparing an N-acyltetrahydroisoquinoline represented by formula (II) ##STR1## wherein A represents a phenylene ring substituted with a hydroxyl group, a lower alkoxy group, an acetoxy group, or a benzyloxy group; R represents a hydrogen atom, a lower alkyl group, or a phenyl group; and X represents a hydrogen atoms, a phenyl group, or a phenyl group substituted with a hydroxyl group, a lower alkoxy group, or an acetoxy group, which comprises asymmetrically hydrogenating an N-acyl-1-methylenetetrahydroisoquinoline or N-acyl-1-benzylidenetetrahydroisoquinoline represented by formula (I) ##STR2## wherein A, R, and X are as defined above, in the presence of an optically active ruthenium-phosphine complex as a catalyst. The process exclusively and efficiently provides a useful isomer of the N-acyltetrahydroisoquinoline of high purity which is useful as an intermediate for synthesizing isoquinoline type alkaloids as pharmaceuticals without involving optical resolution of a racemate.

    摘要翻译: 制备由式(II)表示的N-酰基四氢异喹啉的方法其中A表示被羟基,低级烷氧基,乙酰氧基或苄氧基取代的亚苯基环; R表示氢原子,低级烷基或苯基; X表示氢原子,苯基或被羟基,低级烷氧基或乙酰氧基取代的苯基,其包括不对称地氢化N-酰基-1-亚甲基四氢异喹啉或N-酰基-1- 由式(I)表示的亚苄基四氢异喹啉,其中A,R和X如上所定义,在光学活性钌 - 膦配合物作为催化剂存在下进行。 该方法专门有效地提供了高纯度的N-酰基四氢异喹啉的有用异构体,其可用作合成异喹啉类生物碱作为药物而不涉及外消旋物的光学拆分的中间体。

    Ruthenium-phosphine complex
    65.
    发明授权
    Ruthenium-phosphine complex 失效
    钌膦络合物

    公开(公告)号:US4766225A

    公开(公告)日:1988-08-23

    申请号:US130577

    申请日:1987-12-09

    CPC分类号: C07F15/0053 C07C51/36

    摘要: A ruthenium-phosphine complex represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a methyl group, or a methoxy group; and R.sup.2 represents a lower alkyl group, a halogenated lower alkyl group, a phenyl group, or a phenyl group substituted with a lower alkyl group. The complex is inexpensive and exhibits excellent performance as a catalyst for various organic syntheses, particularly for asymmetric hydrogenation.

    摘要翻译: 由式(I)表示的钌膦络合物:其中R 1表示氢原子,甲基或甲氧基; R 2表示低级烷基,卤代低级烷基,苯基或被低级烷基取代的苯基。 该复合物是便宜的,并且作为各种有机合成的催化剂表现出优异的性能,特别是用于不对称氢化。

    Rhodium-phosphine complex
    68.
    发明授权
    Rhodium-phosphine complex 失效
    铑膦络合物

    公开(公告)号:US4604474A

    公开(公告)日:1986-08-05

    申请号:US714281

    申请日:1985-03-21

    摘要: A novel rhodium-phosphine complex represented by the formula[Rh(p-Tolyl BINAP).sub.2 ].sup.+ Y.sup.-wherein p-Tolyl BINAP represents 2,2'-bis(di-p-tolylphosphino)-1,1'-binaphthyl, and Y represents ClO.sub.4, PF.sub.6, BF.sub.4 or PCl.sub.6 is described. This complex can be used as a catalyst for various organic syntheses and also for asymmetric syntheses such as an asymmetric isomerization reaction and an asymmetric hydrogenation reaction. Due to its high activity, the complex is very useful as a catalyst.

    摘要翻译: 由式[Rh(对甲苯基BINAP)2] + Y-表示的新型铑 - 膦配合物,其中对甲苯基BINAP表示2,2'-双(二对甲苯基膦基)-1,1'-联萘, 并描述Y表示ClO 4,PF 6,BF 4或PCl 6。 该络合物可用作各种有机合成的催化剂,也可用作不对称异构化反应和不对称氢化反应的不对称合成。 由于其活性高,络合物作为催化剂是非常有用的。