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1.发明授权Process for preparation of optically active .alpha.-bromo and .alpha.-chlorocarboxylic compounds 失效光学活性α-溴和α-氯代羧酸化合物的制备方法
公开(公告)号：US5852212A
公开(公告)日：1998-12-22
申请号：US662855
申请日：1996-06-12
IPC分类号： B01J31/24 , C07B61/00 , C07C51/36 , C07C53/19 , C07C55/32 , C07C59/135 , C07C59/147 , C07C227/14 , C07C229/20 , C07F15/00 , C07C53/15
摘要： Optically active .alpha.-bromo- or .alpha.-chlorocarboxylic compounds of the formula ##STR1## wherein X is bromine or chlorine; M is hydrogen, NR.sub.4.sup.+1 or a cation of an alkali or alkaline earth metal; R.sup.1 is hydrogen or lower alkyl; n is 0 or 1; R is hydrogen, C.sub.1 -C.sub.20 alkyl, or C.sub.1 -C.sub.20 alkyl substituted in the terminal position with --NR.sup.2.sub.2, --COOR.sup.2, --OR.sup.3, a free or protected --CHO group or a ring A; R.sup.2 is hydrogen or a lower alkyl; R.sup.3 is hydrogen or a protecting group; ring A is an unsubstituted or substituted ring; and * is a center of chirality, are prepared by enantioselectively hydrogenating, in the presence of a ruthenium complex of an optically active diphosphine ligand, a (Z)-.alpha.,.beta.-unsaturated compound of the general formula ##STR2## wherein R, n, X and M are as defined above.
摘要翻译： 式（I）的光学活性α-溴代或α-氯代羧酸化合物，其中X是溴或氯; M是氢，NR4 + 1或碱金属或碱土金属的阳离子; R1是氢或低级烷基; n为0或1; R是氢，C1-C20烷基或在具有-NR22，-COOR2，-OR3，游离或保护的-CHO基或环A的末端取代的C1-C20烷基; R2是氢或低级烷基; R3是氢或保护基; 环A是未取代或取代的环; 和*是手性中心，通过在光学活性二膦配体的钌络合物存在下，通过对映选择性氢化制备，通式为其中R，R 1，R 2， n，X和M如上所定义。
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2.发明授权
公开(公告)号：US5750690A
公开(公告)日：1998-05-12
申请号：US690215
申请日：1996-07-26
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07D231/04 , C07D231/06 , C07D237/04 , C07D243/02 , C07D243/04 , C07D487/04 , C07F9/50 , C07D237/26
CPC分类号： C07D231/06 , C07D231/04 , C07D237/04 , C07D243/02 , C07D487/04
摘要： A process for the asymmetric hydrogenation of a compound of the formula ##STR1## wherein each R, independently, is alkyl, arylmethyl, aryl, alkoxy, arylmethoxy or aryloxy or both R's, taken together, are methylene, ethylene or 1,2-phenylene and n is 1,2 or 3, or of a salt thereof to a compound of the formula ##STR2## in the form of an (S) or (R) enantiomer, wherein R and n have the significances given above, using an optically active ruthenium-diphosphine complex as catalyst, is described. The preparation of the compounds of formula II, as well as the compounds of formula II, which form a further object of the invention, are also described.
摘要翻译： 式II化合物的不对称氢化的方法，其中每个R独立地是烷基，芳基甲基，芳基，烷氧基，芳基甲氧基或芳氧基，或者两个R一起是亚甲基，亚乙基或1,2- 亚苯基，n为1,2或3，或其盐与式（I）或（R）对映异构体形式的式I化合物反应，其中R和n具有上述含义，使用 描述了一种光学活性的钌 - 二膦配合物作为催化剂。 还描述了形成本发明另一目的的式II化合物以及式II化合物的制备。
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公开(公告)号：US5880285A
公开(公告)日：1999-03-09
申请号：US993299
申请日：1997-12-18
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07D217/20
CPC分类号： C07D217/20
摘要： A process for the manufacture of optically active (R)- or (S)-1-(4-methoxy-benzyl)-1,2,3,4,5,6,7,8-octahydro-isoquinoline adducts of the formula ##STR1## wherein HX signifies a mineral acid from the group of HBF.sub.4, H.sub.2 SO.sub.4, HPF.sub.6, HBr, HI, HCl,HSbF.sub.6 or HClO.sub.4, or a strong organic acid from the group of C.sub.1-8 -alkylSO.sub.3 H, picric acid, formic acid, a lower alkylsulphonic acid or arylcarboxylic acid or a dicarboxylic acid,from a compound of the formula ##STR2## wherein HX has the significance given above, by asymmetric hydrogenation in the presence of a complex consisting of optically active diphosphine ligands with iridium, optionally in the presence of an additive.
摘要翻译： 制备式（I）的光学活性（R） - 或（S）-1-（4-甲氧基 - 苄基）-1,2,3,4,5,6,7,8-八氢 - 异喹啉加成物的方法 其中HX表示来自HBF4，H2SO4，HPF6，HBr，HI，HCl，HSbF6或HClO4的无机酸，或来自C1-8烷基SO3H，苦味酸，甲酸的强有机酸 ，由下式化合物的低级烷基磺酸或芳基羧酸或二羧酸，其中HX具有上述含义，通过不对称氢化在由光学活性二膦配体与铱组成的络合物存在下，任选地 在存在添加剂的情况下。
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公开(公告)号：US5710322A
公开(公告)日：1998-01-20
申请号：US808297
申请日：1997-02-28
申请人： Emil Albin Broger , Rudolf Schmid
发明人： Emil Albin Broger , Rudolf Schmid
IPC分类号： B01J23/42 , B01J23/44 , C07B61/00 , C07C227/32 , C07C249/02 , C07C251/08 , C07C251/12 , C07C249/00
CPC分类号： C07C251/12 , C07C227/32
摘要： The compounds of the formula ##STR1## wherein R is OH, NH.sub.2, lower-alkyl-NH or phenyl-lower alkyl-NH are presented. These compounds can be catalytically hydrogenated to the corresponding .alpha.-aminocarboxylic acid derivatives which are intermediates in the synthesis of therapeutic pseudopeptides.
摘要翻译： 提供了其中R是OH，NH 2，低级烷基-NH或苯基 - 低级烷基-NH的式的化合物。 这些化合物可以催化氢化成相应的α-氨基羧酸衍生物，它们是合成治疗性假肽的中间体。
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公开(公告)号：US6037479A
公开(公告)日：2000-03-14
申请号：US105592
申请日：1998-06-26
CPC分类号： C07D405/04 , C07B53/00 , C07F15/004 , C07F15/0053 , C07F15/008 , C07F9/743 , C07F9/803
摘要： Novel, chiral diarsine compounds, which are present in the (R)- or (S)- or (rac)-form, of the formula ##STR1## wherein R signifies an optionally substituted aryl from the group of phenyI, naphthyl, furyl and thienyl; C.sub.3-8 -cycloalkyl or C.sub.1-8 -alkyl;R.sup.1, R.sup.2, R.sup.3 each independently signify C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy, aryloxy, F or Cl,R.sup.2 and R.sup.3 each independently also signify hydrogen orR.sup.1 and R.sup.2 together signify tetramethylene or a benzo or benzofuro system or dioxymethylene on the respective benzene ring; orR.sup.2 and R.sup.3 together signify dioxymethylene,and the manufacture of the diarsine compounds of formula I, as well as complexes of the compounds of formula I with Group VIII metal and their use for enantioselective reactions.
摘要翻译： 存在于下式的（R） - 或（S） - 或（外消旋） - 形式中的新型手性胂系化合物，其中R表示苯基，萘基，呋喃基和噻吩基中任选取代的芳基; C 3-8 - 环烷基或C 1-8 - 烷基; R 1，R 2，R 3各自独立地表示C 1-8烷基，C 1-8 - 烷氧基，芳氧基，F或Cl，R 2和R 3各自独立地表示氢或R 1和R 2一起表示四氢呋喃或苯并或苯并呋喃体系或二氧亚甲基 各苯环; 或R 2和R 3一起表示二甲亚甲基，并且制备式I的胂化合物，以及式I化合物与Ⅷ族金属的络合物及其用于对映选择性反应。
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