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    Procedure for the preparation of racemic and enantiomerically pure derivatives of 1,5 diaryl-3-trifluorromethyl-Δ2-pyrazolines
    37.
    发明授权
    Procedure for the preparation of racemic and enantiomerically pure derivatives of 1,5 diaryl-3-trifluorromethyl-Δ2-pyrazolines 失效

    公开(公告)号：US06958403B2

    公开(公告)日：2005-10-25

    申请号：US11007449

    申请日：2004-12-08

    申请人： Montserrat Alcon-Marrugat ,  Miguel Angel Pericas-Brondo ,  Maria Rosa Cuberes-Altisen ,  Jordi Frigola-Constansa

    发明人： Montserrat Alcon-Marrugat ,  Miguel Angel Pericas-Brondo ,  Maria Rosa Cuberes-Altisen ,  Jordi Frigola-Constansa

    IPC分类号： C07D231/06 ,  C07D231/12

    CPC分类号： C07D231/06

    摘要： Procedure for preparation of compounds with the general formula 1, which include the racemic mixtures (±)-1, and the enantiomerically pure compounds (−)-1 and (+)-1, wherein R1 and R3, like or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, with the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group; which involves obtaining the racemic mixture with the general formula (±)-1 by reacting an (E)-1,1,1-trifluoro-4-aryl-3-buten-2-one with a phenylhydrazine, followed by a treatment with chlorosulphonic acid, or by reacting with chlorosulphonic acid followed by a reaction with sodium hydroxide and, finally, with thionyl chloride. The product obtained by either of these methods is made to react with ammonium carbonate or ammonia, or with sodium sulphite and methyl iodide or methyl sulphate. In addition, to obtain the enantiomerically pure compounds with the general formula 1 by resolving the racemic mixture with the general formula (±)-1, a reaction is effected with optically active ephedrine, followed by formation of the sodium salt of each enantiomer, reaction with thionyl chloride and ammonium carbonate or ammonia, or instead with thionyl chloride followed by sodium sulphite and methyl iodide or methyl sulphate to thereby obtain separately the enantiomerically pure compounds with the general formulae (−)-1 and (±)-1.

    Resolution of amines
    38.
    发明授权
    Resolution of amines 失效
    分解胺

    公开(公告)号：US06187930B1

    公开(公告)日：2001-02-13

    申请号：US09462326

    申请日：2000-04-10

    申请人： Antoni Torrens-Jover ,  Jordi Frigola-Constansa

    发明人： Antoni Torrens-Jover ,  Jordi Frigola-Constansa

    IPC分类号： C07D23112

    CPC分类号： C07D231/12

    摘要： The procedure comprises reacting the mixture that comprises 2-[phenyl(1-methyl-1 H-pyrazole-5-yl)methoxy]-N,N-dimethylethanamine (I) with an enantiomer of an optically active acid to form a diastereoisomeric salt, separating said salt and liberating the enantiomer of said compound (I). The dextrorotatory enantiomer of (I) can be obtained by reacting a racemic mixture or non-racemic mixture of (I) with (+)-ditoluyl-L-tartaric acid, optionally mixed with p-toluensulphonic acid. Compound (I) has analgesic properties and its most active enantiomer is dextrorotatory.

    摘要翻译： 该方法包括将包含2- [苯基（1-甲基-1H-吡唑-5-基）甲氧基] -N，N-二甲基乙胺（I）的混合物与光学活性酸的对映异构体反应，形成非对映异构体盐 ，分离所述盐并释放所述化合物（I）的对映异构体。 （I）的右旋对映异构体可以通过将（I）与（+） - 二甲氧基-L-酒石酸的外消旋混合物或非外消旋混合物任选与对甲苯磺酸混合而获得。 化合物（I）具有镇痛特性，其最活泼的对映异构体是右旋的。

    Process for obtaining enantiomers of cis-olirtine
    39.
    发明授权
    Process for obtaining enantiomers of cis-olirtine 失效
    获得顺式 - 奥利汀对映异构体的方法

    公开(公告)号：US6118009A

    公开(公告)日：2000-09-12

    申请号：US485023

    申请日：2000-02-01

    申请人： Antoni Torrens-Jover ,  Jordi Frigola-Constansa

    发明人： Antoni Torrens-Jover ,  Jordi Frigola-Constansa

    IPC分类号： C07D231/12

    CPC分类号： C07D231/12

    摘要： The procedure comprises (a) the enantioselective reduction of a pro-chiral ketone (III) by using a reducing and agent and chiral catalyst, both boron derivatives, in an anhydrous solvent or mixture of anhydrous solvents to form an enantiomer of an alcohol (II), and (b), the alkylation of (II), in phase transfer conditions, with optionally prior isolation and purification thereof, with 2-chloro-N,N-dimethylethylamine, to form an enantiomer of (I). Cyzolirtine exhibits analgesic properties.

    摘要翻译： PCT No.PCT / ES98 / 00223 Sec。 371日期2000年2月1日 102（e）日期2000年2月1日PCT提交1998年7月31日PCT公布。 公开号WO99 /​​ 07684 日期1999年2月18日该方法包括（a）通过使用还原剂和试剂和手性催化剂（硼衍生物）在无水溶剂或无水溶剂混合物中形成对映异构体（a）对映异构选择性还原前手性酮 的醇（II）和（b）中，（II）在相转移条件下的烷基化，任选地先前用2-氯-N，N-二甲基乙胺分离和纯化，形成（I ）。 Cyzolirtine具有镇痛作用。