Process for the direct and regioselective functionalization in position
2 of phenothiazine
    2.
    发明授权
    Process for the direct and regioselective functionalization in position 2 of phenothiazine 失效
    苯并噻嗪位置2中的直接和选择性功能化过程

    公开(公告)号:US5089613A

    公开(公告)日:1992-02-18

    申请号:US680942

    申请日:1991-04-05

    申请人: Mariano Meneghin

    发明人: Mariano Meneghin

    IPC分类号: C07D279/18 C07D279/20

    CPC分类号: C07D279/20

    摘要: Preparation of 2-alkylthio-phenothiazines by direct functionalization of phenothiazine by reaction of the phenothiazine, N-protected by an acryl group, with a sulfonating agent such as sulfuric acid, sulfuric anhydride, chlorosulfonic acid, or oleum, in order to obtain, after work-up of the reaction mixture, phenothiazine-2-sulfonic acid, followed by the reduction of this or, optionally, of its acyl chloride derivative, to obtain 2-mercapto-phenothiazine which subsequently is subjected to S-alkylation to thereby obtain the desired target compound.

    Process for the preparation of
cis-5-fluoro-2-methyl-1-(4-methyl-thiobenzylidene)-indene-3-acetic acid
    4.
    发明授权
    Process for the preparation of cis-5-fluoro-2-methyl-1-(4-methyl-thiobenzylidene)-indene-3-acetic acid 失效
    顺式-5-氟-2-甲基-1-(4-甲基 - 硫代亚苄基) - 茚-3-乙酸的制备方法

    公开(公告)号:US4748271A

    公开(公告)日:1988-05-31

    申请号:US875405

    申请日:1986-06-17

    申请人: Mariano Meneghin

    发明人: Mariano Meneghin

    CPC分类号: C07C323/00

    摘要: A process is described for the preparation of cis-5-fluoro-2-methyl-1-(4-methylthiobenzylidene)-indene-3-acetic acid that consists in reacting a lower alkyl ester of 5-fluoro-2-methylindene-3-acetic acid with a substantially equimolecular amount of 4-methylthio-benzaldehyde in a solid-liquid two-phase system in which the solid phase is a potassium alcoholate or hydroxide and the liquid phase is a solution of the reagents in an organic solvent inert in the reaction conditions, in the presence of a phase transfer catalyst and at a temperature comprised between -20.degree. and +20.degree. C.

    摘要翻译: 描述了制备顺式-5-氟-2-甲基-1-(4-甲硫基亚苄基) - 茚-3-乙酸的方法,该方法包括使5-氟-2-甲基茚-3-酮 - 乙酸与基本上等摩尔量的4-甲硫基 - 苯甲醛在固 - 液两相体系中固相是醇钾或氢氧化钾,液相是试剂在有机溶剂中的溶液为惰性的 在相转移催化剂存在下,在-20℃〜+ 20℃的温度下进行反应。

    Process for the direct and regioselective functionalization in position
2 of phenothiazine
    5.
    发明授权
    Process for the direct and regioselective functionalization in position 2 of phenothiazine 失效
    吩噻嗪2位直接和区域选择性官能化方法

    公开(公告)号:US5191078A

    公开(公告)日:1993-03-02

    申请号:US844434

    申请日:1992-03-02

    申请人: Mariano Meneghin

    发明人: Mariano Meneghin

    IPC分类号: C07D279/20

    CPC分类号: C07D279/20

    摘要: A process for the direct and regioselective functionalization of phenothiazine which allows one to introduce an SH group in position 2 is described. The thus-obtained 2-mercapto-phenothiazine is easily transformed into 2-methylthio-phenothiazine, an important intermediate for the preparation of pharmacological active compounds. One of the reaction routes (described in detail in the specification) involves the production of an N-aryl-phenothiazine-2-sulfinic acid [compound (III)] which can be isolated as a salt (e.g., an alkaline salt) by treatment with an aqueous alkaline solution. Thus compound (III-A) is produced.

    摘要翻译: 描述了允许在位置2引入SH基团的吩噻嗪的直接和区域选择性官能化的方法。 由此得到的2-巯基吩噻嗪易于转化为2-甲硫基吩噻嗪,2-甲硫基吩噻嗪是制备药物活性化合物的重要中间体。 反应路线之一(在说明书中详细描述)涉及可以通过处理分离作为盐(例如,碱性盐)的N-芳基吩噻嗪-2-亚磺酸[化合物(III)]的制备 用碱性水溶液。 因此,生成化合物(III-A)。