2. Academic Validation
  3. Synthesis of C3-Alkylated Indoles on DNA via Indolyl Alcohol Formation Followed by Metal-Free Transfer Hydrogenation

Synthesis of C3-Alkylated Indoles on DNA via Indolyl Alcohol Formation Followed by Metal-Free Transfer Hydrogenation

  • Org Lett. 2019 Sep 6;21(17):6633-6637. doi: 10.1021/acs.orglett.9b02132.
Pinwen Cai 1,  Guanyu Yang 1,  Lanzhou Zhao 1,  Jinqiao Wan 1,  Jin Li 1,  Guansai Liu 1
Affiliations

Affiliation

  • 1 Discovery Chemistry Unit, HitGen Inc., Building 6, No. 8 Huigu 1st East Road, Tianfu International Bio-Town, Shuangliu District, Chengdu 610200, Sichuan, P. R. China.
PMID: 31411480 DOI: 10.1021/acs.orglett.9b02132
Abstract

3-Alkylated indole cores have been found in countless Natural Products and many biologically active compounds, including pharmaceuticals. In this report, a highly efficient approach to C3-alkylated indole derivatives on DNA via indolyl alcohol formation followed by metal-free transfer hydrogenation is developed. This on-DNA C3 alkylation approach is attractive because library compounds can be constructed from simple aldehydes or acid functionalized aldehydes, which are widely commercially available.

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