Process for the preparation of ibodutant (MEN15596) and related intermediates
    7.
    发明授权
    Process for the preparation of ibodutant (MEN15596) and related intermediates 有权
    制备ibodutant(MEN15596)及相关中间体的方法

    公开(公告)号:US08431684B2

    公开(公告)日:2013-04-30

    申请号:US13321501

    申请日:2010-05-11

    IPC分类号: A61K38/06

    CPC分类号: C07D409/12

    摘要: This invention relates to a novel process for synthesizing the product ibodutant shown in the figure below, consisting of a small number of high-yield steps involving reagents and solvents with low environmental impact, characterized by the coupling of two portions, compounds (3) and (4), one of which (3) is synthesized by coupling of 6-methyl-2-benzo[b]thiophenecarboxylic acid (1) with 1-amino-alpha-alpha-cyclopentan carboxylic acid and subsequent cyclization with oxazolone, while the other, compound (4), is obtained from suitable highly selective functionalizations of 4-aminomethylpiperidine (2).

    摘要翻译: 本发明涉及一种合成下图所示产品的新颖方法,该方法由少量高产率步骤组成,包括试剂和低环境影响的溶剂,其特征在于两部分的化合物(3)和 (4),其中一个(3)通过6-甲基-2-苯并[b]噻吩甲酸(1)与1-氨基-α-α-环戊烷羧酸的偶合合成,随后与恶唑酮环化,而 其他化合物(4)由4-氨基甲基哌啶(2)的合适的高度选择性官能化得到。