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    L-tartaric acid salt of a (1R) diastereomer of a 2-azadihydroxybicyclo�2.2.1!heptane compound and the preparation of 2-azabicyclo�2.2.1! heptane compounds
    1.
    发明授权
    L-tartaric acid salt of a (1R) diastereomer of a 2-azadihydroxybicyclo�2.2.1!heptane compound and the preparation of 2-azabicyclo�2.2.1! heptane compounds 失效
    2-氮杂双环[2.2.1]庚烷化合物的（1R）非对映异构体的L-酒石酸盐和2-氮杂双环[2.2.1]庚烷化合物的制备

    公开(公告)号：US5831096A

    公开(公告)日：1998-11-03

    申请号：US873284

    申请日：1997-06-10

    申请人： Patrick Leon ,  Michael O'Brien ,  Denis Largeau ,  Matthew Powers ,  Ching Tsuei

    发明人： Patrick Leon ,  Michael O'Brien ,  Denis Largeau ,  Matthew Powers ,  Ching Tsuei

    IPC分类号： C07D491/18 ,  C07D209/02 ,  C07D209/52 ,  C07D491/12

    CPC分类号： C07D209/52 ,  C07D209/02 ,  Y02P20/55

    摘要： A method for the preparation of a compound of formula ##STR1## wherein R is hydrogen or, respectively, a group of formula ##STR2## R.sub.1 is alkyl; Ar is optionally substituted aryl; and R.sub.3' and R.sub.3" are hydrogen, alkyl or phenyl, or R.sub.3' and R.sub.3" taken together with the carbon atom to which they are attached form cycloalkyl, or salt thereof, comprising acid facilitated acetalizing or ketalizing of a compound of formula ##STR3## wherein R.sub.3' and R.sub.3" are as defined above, and R.sub.4' and R.sub.4" are alkoxy, or taken together with the carbon atom to which they are attached form carbonyl, with a compound of formula ##STR4## wherein * represents an R chirality; R, R.sub.1 and Ar are as defined above, or salt thereof in isopropanol.

    摘要翻译： 其中R为氢或分别为式（II）或（II）的基团的式的化合物的方法R1为烷基; Ar是任选取代的芳基; 并且R 3'和R 3“是氢，烷基或苯基，或者R 3'和R 3”与它们所连接的碳原子一起形成环烷基，或其盐，其包含酸容易地使下式化合物进行缩醛化或缩酮化 其中R 3'和R 3“如上定义，并且R 4'和R 4”是烷氧基，或者与它们所连接的碳原子一起形成羰基的化合物与式 ）其中*表示R手性; R，R 1和Ar如上所定义，或其盐在异丙醇中。

    L-tartaric acid salt of a (1R) diastereomer of a 2-azadihydroxybicyclo�2.2.1!heptane compound and the preparation of 2-azabicyclo�2.2.1!heptane compounds
    3.
    发明授权
    L-tartaric acid salt of a (1R) diastereomer of a 2-azadihydroxybicyclo�2.2.1!heptane compound and the preparation of 2-azabicyclo�2.2.1!heptane compounds 失效
    2-氮杂双环[2.2.1]庚烷化合物的（1R）非对映异构体的L-酒石酸盐和2-氮杂双环[2.2.1]庚烷化合物的制备

    公开(公告)号：US5684159A

    公开(公告)日：1997-11-04

    申请号：US732024

    申请日：1996-10-16

    申请人： Michael O'Brien ,  Patrick Leon ,  Denis Largeau ,  Matthew Powers ,  Thierry Durand

    发明人： Michael O'Brien ,  Patrick Leon ,  Denis Largeau ,  Matthew Powers ,  Thierry Durand

    IPC分类号： C07D491/18 ,  C07D209/02 ,  C07D209/52

    CPC分类号： C07D209/52 ,  C07D209/02 ,  Y02P20/55

    摘要： A method according to the invention is directed to the preparation of a 2-azadihydroxybicyclo�2.2.1!heptane compound of formula ##STR1## wherein * represents an R chirality, *' represents an S chirality, R is hydrogen or, respectively, a group of formula ##STR2## wherein R.sub.1 is alkyl and Ar is optionally substituted aryl, comprising bishydroxylating a bicyclo�2.2.1!heptene compound of formula ##STR3## wherein *, *' and R are as previously defined, in the presence of about 0.1 mol to about 5 mol % of a metal osmate compound or about 0.06 mol % to about 0.07 mol % osmium tetroxide, and an oxidizing agent capable of regenerating osmium tetroxide. The invention is also directed to the treatment of the (1R) diastereomer of the 2-azadihydroxybicyclo�2.2.1!heptane compound (I) wherein R is a group of formula II with L-tartaric acid, and the L-tartaric acid salt product thereof. Furthermore, the invention is directed to using the (1R) diastereomer of the 2-azadihydroxybicyclo�2.2.1!heptane compound in an acid facilitated acetalizing or ketalizing reaction that results in the protection of the dihydroxy moieties thereof in isopropanol. In addition, the invention is directed to oxidizing a bis O-protected derivative of the (1R) diastereomer of the 2-azadihydroxybicyclo�2.2.1!heptane compound to a corresponding lactam compound in the presence of about 0.01 mol % to about 1 mol % of RuO.sub.2 with about 3 equivalents of an oxidant to form the lactam compound with in an enantiomeric excess ("ee") of greater than or equal to about 95%.

    摘要翻译： 根据本发明的方法涉及式（I）的化合物（I）的2-氮杂二羟基双环[2.2.1]庚烷化合物，其中*表示R手性，*'表示S 手性，R分别为氢或分别为式（II）的基团，其中R 1为烷基，Ar为任选取代的芳基，其包含双羟基化双酚[2.2.1]庚烯化合物 （III）其中*，*'和R如前所定义，在约0.1mol至约5mol％的金属锇酸盐化合物或约0.06mol％至约0.07的存在下 mol％的四氧化锇和能够再生四氧化锇的氧化剂。 本发明还涉及其中R是式II的基团与L-酒石酸的2-氮杂二羟基双环[2.2.1]庚烷化合物（I）的（1R）非对映异构体的处理，并且L-酒石酸盐 其产品。 此外，本发明涉及使用2-氮杂二羟基双环[2.2.1]庚烷化合物的（1R）非对映体在酸促进缩醛或缩酮反应中，其导致保护其在异丙醇中的二羟基部分。 此外，本发明涉及在约0.01mol％至约1mol的存在下将2-氮杂二羟基双环[2.2.1]庚烷化合物的（1R）非对映异构体的双O保护的衍生物氧化成相应的内酰胺化合物 ％的RuO 2与约3当量的氧化剂以形成具有大于或等于约95％的对映体过量（“ee”）的内酰胺化合物。