NN 阻转异构体的阻转选择性合成是一个新兴领域,但仍未得到充分探索;尤其是NN苯并咪唑阻转异构体的合成仍然是前所未有的。在此,首次通过钯催化苯并咪唑骨架的从头构建对映选择性合成 NN 苯并咪唑阻转异构体。利用现成的钯催化剂和双膦配体,可以方便地以高产率和优异的对映选择性获得多种非联芳基苯并咪唑和吲哚苯并咪唑阻转异构体。值得注意的是,这些 NN 苯并咪唑阻转异构体对乳腺癌 MCF-7 细胞表现出良好的抗肿瘤活性和选择性。简单的催化体系、广泛的底物范围、高对映选择性和良好的生物活性使该方法极具吸引力。
The invention relates to novel 3-heteorcycl-1-yluracils of formula (I) wherein R?1 and R2¿ together with the interjacent nitrogen atom form an optionally substituted, optionally benzo-condensed 5-membered heterocyclic ring and R3 through R5 have the meaning given in claim 1. The invention also relates to a method of the production of these substances and to herbicidal compositions containing such compounds as active ingredients.