Ruthenium(II)-Catalyzed Site-Selective Hydroxymethylation of Indolines with Paraformaldehyde

• DOI: 10.1021/acs.joc.8b02873
• Publication Date: 2018-12-07T13:46:13Z
• Authors: Suk Hun Lee; Taejoo Jeong; Kunyoung Kim; Na Yeon Kwon; Ashok Kumar Pandey; Hyung Sik Kim; Jin-Mo Ku; Neeraj Kumar Mishra; In Su Kim
• Keywords: Paraformaldehyde; Scope (computer science)

The facile synthesis of hydroxymethylated indole derivatives is crucial for their further development as pharmaceutical compounds and other synthetic purposes. Herein, we describe the ruthenium(II)-catalyzed hydroxymethylation indolines N-heterocycles using paraformaldehyde an abundant C1 feedstock. A wide substrate scope range high levels site selectivity well functional group tolerance were observed.