Copper-promoted dehydrosulfurative carbon-nitrogen cross-coupling with concomitant aromatization for synthesis of 2-aminopyrimidines

Ngoc Son Le Pham; Yujeong Kwon; Hyunik Shin; Jeong-Hun Sohn

doi:10.1039/d2ra05180j

Copper-promoted dehydrosulfurative carbon-nitrogen cross-coupling with concomitant aromatization for synthesis of 2-aminopyrimidines

RSC Adv. 2022 Dec 20;13(1):172-177. doi: 10.1039/d2ra05180j. eCollection 2022 Dec 19.

Authors

Ngoc Son Le Pham¹, Yujeong Kwon¹, Hyunik Shin², Jeong-Hun Sohn¹

Affiliations

¹ Department of Chemistry, Chungnam National University Daejeon 34134 Republic of Korea sohnjh@cnu.ac.kr.
² Yonsung Fine Chemicals R&D Center Suwon 16675 Republic of Korea.

Abstract

Copper-promoted dehydrosulfurative C-N cross-coupling of 3,4-dihydropyrimidin-1H-2-thione with amine accompanied by concomitant aromatization to generate 2-aryl(alkyl)aminopyrimidine derivatives is described. The reaction proceeded well with a wide range of thiono substrates and aryl/aliphatic amines as the coupling partners, offering efficient access to biologically and pharmacologically valuable 2-aryl(alkyl)aminopyrimidines with rapid diversification.