[EN] AZAINDOLE DERIVATIVES, PREPARATIONS THEREOF, USES THEREOF AND COMPOSITIONS CONTAINING THEM<br/>[FR] DERIVES AZAINDOLE, PREPARATIONS DE CES DERIVES AZAINDOLE ET COMPOSITIONS CONTENANT CES DERNIERS
申请人:ASTRAZENECA AB
公开号:WO2004087704A1
公开(公告)日:2004-10-14
Compounds of formula I or pharmaceutically acceptable salts thereof Formula (I) wherein Ar, R1, R2, R3, Ra, Rb and X are as defined in the specificationas well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Catalytic asymmetric dipolar cycloadditions of indolyl delocalized metal-allyl species for the enantioselective synthesis of cyclopenta [b]indoles and pyrrolo[1,2-a]indoles
作者:Fei Tian、Wu-Lin Yang、Tao Ni、Jian Zhang、Wei-Ping Deng
DOI:10.1007/s11426-020-9854-3
日期:2021.1
synthons and efficient methods to synthesize chiral polycyclic indoles has been a hot topic in organic synthesis and medicinal chemistry owing to their broad applications in medicines, pesticides, and other functional molecules. Here, we disclosed novel indolyl substituted metal-allyl zwitterionic intermediates through the decarboxylation of conveniently available vinyl indoloxazolidones, which could be
由于其在药物,农药和其他功能分子中的广泛应用,新型合成子和合成手性多环吲哚的有效方法的开发一直是有机合成和药物化学领域的热门话题。在这里,我们公开了通过方便地获得的乙烯基吲哚恶唑烷酮的脱羧作用而得到的新颖的吲哚基取代的金属-烯丙基两性离子中间体,通过阴离子离域化可以将其视为两种偶极种类。钯-π-烯丙基物种倾向于在不对称的[3 + 2]与缺电子的烯烃的加成中用作全碳的1,3-偶极子,从而提供了多取代的环戊烯[ b具有高区域选择性和立体选择性的吲哚。同时,在原位生成的C1烯醇铵不对称[3 + 2]环加成反应中,铱-π-烯丙基物种被认为是aza-1,3-偶极子,提供了具有高非对映异构体的吡咯并[1,2- a ]吲哚。和对映选择性。另外,偶极环加成可以容易地按比例放大,并且环加合物的几种合成转化被证明用于快速合成各种手性多环吲哚。
Azaindole derivatives, preparations thereof, uses thereof and compositions containing them
申请人:Wei Zhongyong
公开号:US20070027179A1
公开(公告)日:2007-02-01
Compounds of formula I or pharmaceutically acceptable salts thereof Formula (I) wherein Ar, R
1
, R
2
, R
3
, R
a
, R
b
and X are as defined in the specificationas well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
公式 I 的化合物或其药学上可接受的盐,公式(I)中的Ar、R1、R2、R3、Ra、Rb和X定义如说明书中所述,以及包括该化合物的盐和药物组合物的制备方法。它们在治疗中有用,特别是在疼痛管理方面。