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    PRODUCTION OF ALPHA-BROMOLACTAM DERIVATIVE
    1.
    发明专利
    PRODUCTION OF ALPHA-BROMOLACTAM DERIVATIVE 失效

    公开(公告)号：JPH10273481A

    公开(公告)日：1998-10-13

    申请号：JP5406298

    申请日：1998-03-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： ABRECHT STEFAN

    IPC: C07D463/00 ,  B01J27/08 ,  C07B61/00 ,  C07D207/26 ,  C07D207/273 ,  C07D498/04 ,  C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/56 ,  C07D505/00 ,  C07D507/08

    Abstract: PROBLEM TO BE SOLVED: To economically produce the objective compound by a method of a two step process comprising a reaction of 4-chloro-butyroyl chloride with N-bromosuccinimide and further the reaction of the product with an amine. SOLUTION: A reaction of 4-Chloro-butyroyl chloride with N- bromosuccinimide is carried out by adding thionyl chloride at first and immediately adding a catalytic amount of hydrogen bromide thereto to provide a compound of formula I. Further, the compound of formula I is reacted with an amine of the formula, R-NH2 (R is H, a lower alkyl, a lower alkoxy, a cycloalkyl, a lower alkenyl, an aryl, a heterocycle, etc.) in non-aqueous medium in the presence of sodium hydroxide or potassium hydroxide, and a phase transfer catalyst to provide a compound of formula II in the method for producing an α-bromolactam derivative. The compound of formula II is useful for production of cephalosporins, cephem, carbacephem or an iso-oxacephem derivative. The method can shorten the processes, and provide the objective compound at a low cost without requiring a reagent causing trouble such as bromine atom.

    PROCESS FOR THE PREPARATION OF PYRIDO[2,1-A]ISOQUINOLINE DERIVATIVES BY CATALYTIC ASYMMETRIC HYDROGENATION OF AN ENAMINE
    4.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRIDO[2,1-A]ISOQUINOLINE DERIVATIVES BY CATALYTIC ASYMMETRIC HYDROGENATION OF AN ENAMINE 审中-公开
    通过催化不对称氢化方法制备吡咯并[2,1-A]异喹啉衍生物的方法

    公开(公告)号：WO2008031750A3

    公开(公告)日：2008-06-19

    申请号：PCT/EP2007059265

    申请日：2007-09-05

    Applicant: HOFFMANN LA ROCHE ,  ABRECHT STEFAN ,  SCALONE MICHELANGELO ,  SCHMID RUDOLF

    Inventor： ABRECHT STEFAN ,  SCALONE MICHELANGELO ,  SCHMID RUDOLF

    IPC: C07D471/04

    CPC classification number: C07D455/06 ,  B01J31/2295 ,  B01J2231/641 ,  B01J2531/822 ,  C07D471/04 ,  Y02P20/55

    Abstract: The invention relates to a process for the preparation of pyrido[2, 1-a] isoquinoline derivatives of the formula (I), weherein R 2 , R 3 and R 4 are as defined in the specification, comprising the steps of: a) catalytic asymmetric hydrogenation of an enamine of the formula (II), wherein R 1 is lower alkyl, in the presence of a transition metal catalyst containing a chiral diphosphane ligand, b) introduction of an amino protecting group Prot and c) amidation of the ester to form an amide of formula (V), wherein R 2 , R 3 , R 4 and Prot are as defined in the specification.

    Abstract translation: 本发明涉及制备式（I）的吡啶并[2,1-a]异喹啉衍生物的方法，其中R 2，R 3，R 3和R 3， SUP 4+如说明书中所定义，包括以下步骤：a）在式（II）的烯胺的催化不对称氢化中，其中R 1是低级烷基，在 存在含有手性二膦配体的过渡金属催化剂，b）引入氨基保护基团Prot和c）酯的酰胺化以形成式（V）的酰胺，其中R 2，R R 4和R 4如说明书中所定义。

    PROCESS FOR THE PREPARATION OF PYRIDO [2,1-A] ISOQUINOLINE DERIVATIVES
    5.
    发明专利
    PROCESS FOR THE PREPARATION OF PYRIDO [2,1-A] ISOQUINOLINE DERIVATIVES 未知

    公开(公告)号：CA2708314C

    公开(公告)日：2015-06-23

    申请号：CA2708314

    申请日：2008-12-09

    Applicant: HOFFMANN LA ROCHE

    Inventor： ABRECHT STEFAN ,  ADAM JEAN-MICHEL ,  FETTES ALEC

    IPC: C07D401/06 ,  C07D207/26 ,  C07D471/04

    Abstract: The present invention relates to a novel process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the formula (I) wherein R2, R3 and R4 are each independently selected from the group consisting of hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy and lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by a group consisting of lower alkoxycarbonyl, aryl and heterocyclyl, and the pharmaceutically acceptable salts thereof. The pyrido[2,1-a] isoquinoline derivatives of the formula (I) are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

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