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Professor Michael Willis

Research in the Willis group is focused on the development of new catalysts and reactions for synthetic chemistry. The group is particularly interested in addressing synthetic challenges that are applicable to the pharmaceutical and agrochemical industries. The group has reported a series of reactions based on the incorporation of sulfur dioxide, using the reagent DABSO, to deliver a range of sulfonyl-derived products, including sulfones, sulfonamides, sulfoxides and sulfonyl fluorides. Related to this has been the development of powerful cross-coupling reactions based on the loss of sulfur dioxide from heterocyclic sulfinate coupling partners. This chemistry is particularly applicable where the corresponding boronic acids perform poorly, such as in the case of 2-pyridine examples.

Willis Group Website

CPalladium(II)-Catalyzed Synthesis of Sulfinates from Boronic Acids and DABSO: A Redox-Neutral, Phosphine-Free Transformation
One-pot palladium-catalyzed synthesis of sulfonyl fluorides from aryl bromides
Pyridine sulfinates as general nucleophilic coupling partners in palladium-catalyzed cross-coupling reactions with aryl halides

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Deeming AS1, Russell CJ2, Willis MC3.
Angew Chem Int Ed Engl. 2016 Jan 11;55(2):747-50. doi: 10.1002/anie.201508370. Epub 2015 Nov 24.
A redox-neutral palladium(II)-catalyzed conversion of aryl, heteroaryl, and alkenyl boronic acids into sulfinate intermediates, and onwards to sulfones and sulfonamides, has been realized. A simple Pd(OAc)2 catalyst, in combination with the sulfur dioxide surrogate 1,4-diazabicyclo[2.2.2]octane bis(sulfur dioxide) (DABSO), is suRead More
Davies AT1, Curto JM2, Bagley SW2, Willis MC1.
Chem Sci. 2017 Feb 1;8(2):1233-1237. doi: 10.1039/c6sc03924c. Epub 2016 Oct 11.
A mild, efficient synthesis of sulfonyl fluorides from aryl and heteroaryl bromides utilizing palladium catalysis is described. The process involves the initial palladium-catalyzed sulfonylation of aryl bromides using DABSO as an SO2 source, followed by in situ treatment of the resultant sulfinate with the electrophilic fluorineRead More
Markovic T1, Rocke BN2, Blakemore DC2, Mascitti V2, Willis MC1.
Chem Sci. 2017 Jun 1;8(6):4437-4442. doi: 10.1039/c7sc00675f. Epub 2017 Apr 28.
Pyridine rings are ubiquitous in drug molecules; however, the pre-eminent reaction used to form carbon-carbon bonds in the pharmaceutical industry, the Suzuki-Miyaura cross-coupling reaction, often fails when applied to these structures. This phenomenon is most pronounced in 2-substituted pyridines, and results from the difficulRead More