会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 37. 发明授权
    • Process for preparation of fused pyrroles
    • 熔融吡咯的制备方法
    • US06872835B2
    • 2005-03-29
    • US10088276
    • 2001-07-02
    • Makoto TokunagaYasuo Wakatsuki
    • Makoto TokunagaYasuo Wakatsuki
    • C07B61/00C07D209/08C07D209/60C07D209/80C07D209/96C07D209/04
    • C07D209/80C07D209/08C07D209/96
    • The invention provides processes for the preparation of fused pyrroles, preferably indoles, which permit the use of inexpensive aromatic amines themselves as the raw material and attain high atomic efficiency and high regioselectivity. Specifically, a process for the preparation of fused pyrroles, e.g., indoles bearing methyl at the 3-position of pyrrole ring and R1 (or R2) of the general formula (4) at the 2-position thereof, or 3,3-disubstituted indoles bearing R1 and R2 at the 3-position of pyrrole ring and methyl at the 2-position thereof, characterized by reacting an alkynol of the general formula (4) with an aromatic primary amine in the presence of a ruthenium complex, more preferably with an acid or an ammonium salt thereof being made to coexist. [In the general formula (4), R1 and R2 are each independently hydrogen, optionally substituted alkyl, or optionally substituted aryl, or alternatively R1 and R2 may be united to form an alkylene chain.]
    • 本发明提供制备熔融吡咯,优选吲哚的方法,其允许使用廉价的芳族胺本身作为原料并获得高的原子效率和高的区域选择性。 具体地说,制备稠合吡咯的方法,例如在吡咯环的3-位含有甲基的吲哚和通式(4)的2-位的R 1(或R 2)的2-位, 或在吡咯环的3-位上带有R 1和R 2的3,3-二取代的吲哚,其2-位上的甲基,其特征在于使通式(4)的炔醇与芳族伯 在通式(4)中,R 1和R 2各自独立地为氢,任选取代的烷基(取代或未取代的烷基) ,或任选取代的芳基,或者R 1和R 2可以一起形成亚烷基链。