通过钯（II）-SPRIX催化的C-H活化对含有手性季碳中心的四氢环戊并[b]吲哚进行对映选择性合成。
Enantioselective synthesis of tetrahydrocyclopenta[b]indole bearing a chiral quaternary carbon center via Pd(ii)-SPRIX-catalyzed C-H activation.
作者信息
Abozeid Mohamed Ahmed, Sairenji Shiho, Takizawa Shinobu, Fujita Makoto, Sasai Hiroaki
机构信息
The Institute of Scientific and Industrial Research (ISIR), Osaka University, Mihogaoka, Ibaraki-shi, Osaka 567-0047, Japan.
出版信息
Chem Commun (Camb). 2017 Jun 22;53(51):6887-6890. doi: 10.1039/c7cc03199h.
The highly enantioselective cyclization of 3-alkenylindole via C-H activation has been established using Pd(OCOCF) in conjunction with the chiral spiro bis(isoxazoline) ligand (SPRIX). The presence of an N-allyl substituent on the substrate has a strong impact on both reactivity and selectivity, leading to tricyclic indole products (up to 96% ee) with a chiral quaternary carbon center.
通过C-H活化实现的3-烯基吲哚的高度对映选择性环化反应已通过使用Pd(OCOCF)与手性螺双（异恶唑啉）配体（SPRIX）相结合得以实现。底物上N-烯丙基取代基的存在对反应活性和选择性都有很大影响，从而得到具有手性季碳中心的三环吲哚产物（对映体过量高达96%）。
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