A Simple Key For indazole alkylation Unveiled
A Simple Key For indazole alkylation Unveiled
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The scope of boronic acid substitution was investigated while in the response of a range of formylboronic acids 1b–file with DIAD (2b) followed by cyclization (Scheme two).
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The starting up material 12 was synthesized by making use of our common technique which on subjection to Pd-catalyzed immediate biaryl coupling using the reported procedure16 afforded a new course of bio-azaheterocycles, i.e.
The mechanism for that C–N bond formation during the copper catalysed response of arylboronic acids with diazadicarboxylates has been proposed by Uemura and Chatani.
The indazole core is an interesting pharmacophore as a result of its purposes in medicinal chemistry. In past times number of years, this moiety is useful for the synthesis of kinase inhibitors.
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-aryl section labored properly to provide the corresponding solution in a very good generate. The products 48a and 48b may be fashioned with moderate selectivity (1:1). The products 48c and 48d were being also obtained under common conditions. The goal compounds 48e–m ended up also accomplished through this [4 + 1] cyclization in very good yields. The substrate scope of several different allenes 47 substituted by a number of electron-donating or electron-deficient groups at diverse positions gave the corresponding products in appropriate to large yields.
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