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    CHIRAL REDUCTIONS OF IMINES LEADING TO THE SYNTHESES OF OPTICALLY ACTIVE AMINES
    4.
    发明公开
    CHIRAL REDUCTIONS OF IMINES LEADING TO THE SYNTHESES OF OPTICALLY ACTIVE AMINES 失效
    手性削减了亚胺SYTHESE光学活性胺的LEAD

    公开(公告)号：EP0873298A4

    公开(公告)日：2000-05-17

    申请号：EP96933160

    申请日：1996-09-27

    申请人： NPS PHARMA INC

    发明人： VAN WAGENEN BRADFORD C ,  BARMORE ROBERT M

    IPC分类号： C07C209/44 ,  C07C209/52 ,  C07C211/27 ,  C07C211/29 ,  C07C211/30 ,  C07C213/02 ,  C07C215/46 ,  C07C217/54 ,  C07C227/04 ,  C07C229/38 ,  C07C231/18 ,  C07C237/30 ,  C07C253/30 ,  C07C255/58

    CPC分类号： C07C209/52

    摘要： A process for preparing an R enantiomer of a compound of formula (I) wherein Me is methyl, Ar is 3-methoxyphenyl, 3-chlorophenyl, or 1-naphthyl, and X is independently selected from the group consisting of H, F, Cl, Br, I, phenyl, CF3, CF2H, CFH2, lower alkyl (e.g., Me), O-lower alkyl (e.g., OMe), OCH2CF3, OH, CN, NO2, C(O)-lower alkyl (e.g., C(O)Me), C(O)O-lower alkyl (e.g., C(O)OMe), C(O)NH-lower alkyl (e.g., C(O)NH-Me), C(O)N-lower alkyl2 (e.g., C(O)NMe2), OC(O)-lower alkyl (e.g., OC(O)Me), and NH-C(O)-lower alkyl (e.g., NH-C(O)Me), where "lower alkyl" is selected from a group consisting of 1 to 6 carbon atoms, and m is an integer between 1 and 5, by asymmetrically and enantioselectively reducing an imine with a reducing agent/chiral auxiliary agent complex so as to produce an enantiomeric excess of R enantiomer of the compound of formula (I) over the S enantiomer of the compound of formula (I). The process is especially useful to produce compounds (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(2-chlorophenyl)propanamine and (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(phenyl)propanamine. Enantiomeric excess of the R enantiomer over S enantiomer of greater than 65 % have been achieved.

    3-Aminomethyl derivatives of indane, indoline and dihydrobenzofurane and dihydrobenzothiophene
    7.
    发明公开
    3-Aminomethyl derivatives of indane, indoline and dihydrobenzofurane and dihydrobenzothiophene 失效
    茚满，二氢吲哚，二氢苯并呋喃和二氢苯并噻吩-3-氨基甲基衍生物。

    公开(公告)号：EP0281261A2

    公开(公告)日：1988-09-07

    申请号：EP88301073.8

    申请日：1988-02-09

    申请人： H. LUNDBECK A/S

    发明人： Boegesoe, Klaus Peter ,  Perregaard, Jens Kristian

    IPC分类号： C07C215/46 ,  C07C217/54 ,  C07C219/26 ,  C07C271/00 ,  C07D307/81 ,  C07D333/58 ,  C07D209/14 ,  A61K31/13 ,  A61K31/22 ,  A61K31/325 ,  A61K31/34

    CPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58

    摘要： Indane-, dihydrobenzofurane-, dihydrobenzothiophene-, and indoline- derivatives of the following formula:
    wherein X, R¹, R², R³ and R⁴ are as defined in Claim 1,
    are effective at presynaptic DA receptors, or both at pre- and postsynaptic DA receptors, indicating usefulness in the treatment of disorders of the central nervous system (CNS) such as schizophrenia or Parkinson's disease.
    The 1-aminomethyl derivatives of Formula I exist as optical isomers, and the useful effects are often found in the single enantiomers to a different degree.
    A method for the preparation of compounds of Formula I is described.

    摘要翻译： 茚，二氢苯并呋喃 - ，二氢苯并噻吩 - 和下式的二氢吲哚衍生物：其中X，R 1，R 2，R 3和R 4如权利要求1中所定义， 在突触前DA受体或前突触后DA受体上均有效，表明在治疗中枢神经系统疾病（CNS）如精神分裂症或帕金森病中有用。 式I的1-氨基甲基衍生物作为光学异构体存在，并且在单一对映异构体中经常发现有用的效果达到不同程度。 描述了制备式I化合物的方法。