Synthesis 2022; 54(24): 5451-5460
DOI: 10.1055/a-1929-2650
paper

One-Pot Synthesis of 2-Sulfonamidobenzo[b]thiophenes Enabled by a Mild Protonative Activation of Ynamides

Solbin Kim
a   Eco-Friendly New Materials Research Center, Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology (KRICT), 141 Gajeong-ro, Yuseong-gu, Daejeon, 34114, Republic of Korea
b   Department of Chemistry, Hanyang University, 222 Wangsimni-ro, Seongdong-gu, Seoul, 04763, Republic of Korea
,
So Yeun Lim
a   Eco-Friendly New Materials Research Center, Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology (KRICT), 141 Gajeong-ro, Yuseong-gu, Daejeon, 34114, Republic of Korea
b   Department of Chemistry, Hanyang University, 222 Wangsimni-ro, Seongdong-gu, Seoul, 04763, Republic of Korea
,
Kihun Kwak
a   Eco-Friendly New Materials Research Center, Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology (KRICT), 141 Gajeong-ro, Yuseong-gu, Daejeon, 34114, Republic of Korea
b   Department of Chemistry, Hanyang University, 222 Wangsimni-ro, Seongdong-gu, Seoul, 04763, Republic of Korea
,
Hee Nam Lim
c   Department of Chemistry and Biochemistry, Yeungnam University, 280 Daehak-Ro, Gyeongsan, Gyeongbuk, 38541, Republic of Korea
,
Hyun-Suk Yeom
a   Eco-Friendly New Materials Research Center, Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology (KRICT), 141 Gajeong-ro, Yuseong-gu, Daejeon, 34114, Republic of Korea
› Author Affiliations
H.-S.Y. acknowledges the grant (project PJ016028) from the Rural Development Administration (RDA). H.N.L. thanks Yeungnam University for financial support (2021 Yeungnam University Research Grant).


Abstract

The silica gel promoted or solvent-promoted protonative intramolecular cyclization of ynamides containing an o-(methylthio)aryl group resulted in the one-pot formation of biologically important ­benzo[b]thiophenes. Compared with ynamide activation methods that use strong Brønsted acids or expensive transition metals, this protocol is mild and economical. Due to these merits, various functionalized 2-amidobenzo[b]thiophenes were furnished in a convenient way.

Supporting Information



Publication History

Received: 28 June 2022

Accepted after revision: 23 August 2022

Accepted Manuscript online:
23 August 2022

Article published online:
23 September 2022

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