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Room temperature Palladium-Catalyzed C─H Functionalization of Benzothiazole with Iodo(Hetero)Arenes

02 April 2020, Version 1
Working Paper
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

A versatile synthetic protocol involving the room temperature direct arylation of benzothiazole with a wide variety of iodo(hetero)arenes under palladium-catalyzed conditions and promoted by HFIP as the reaction solvent has been presented herewith. An in-situ one-pot sequential HFIP promoted selective iodination of (hetero)arenes followed by Pd-catalyzed direct arylation of benzothiazole has also been disclosed. Synthesis of PMX 610 (antitumor agent) analog has been disclosed and also CJM 126 (antitumor agent) has been synthesized.

Keywords

C-H bond functionalization
Benzothiazole
HFIP
Palladium-catalyzed
Room temperature

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Version History

Apr 02, 2020 Version 1

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The content is available under CC BY NC ND 4.0 [opens in a new tab]

DOI

10.26434/chemrxiv.12055305.v1
D O I: 10.26434/chemrxiv.12055305.v1 [opens in a new tab]

Author’s competing interest statement

No conflict of interest

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