6533b86ffe1ef96bd12ce7a8
RESEARCH PRODUCT
2-Sulfoximidoyl Acetic Acids from Multicomponent Petasis Reactions and Their Use as Building Blocks in Syntheses of Sulfoximine Benzodiazepine Analogues.
Carsten BolmKari RissanenHeliana Michaela Núñez PonceKhai-nghi TruongRenè Hommelsheimsubject
BenzodiazepinePetasis reaction010405 organic chemistrymedicine.drug_classChemistryOrganic ChemistrymedicinePhysical and Theoretical Chemistry010402 general chemistry01 natural sciencesBiochemistryCombinatorial chemistry0104 chemical sciencesdescription
Upon application of a multicomponent Petasis reaction, a broad range of NH-sulfoximines and boronic acids react with glyoxalic acid to afford the corresponding 2-substituted acetic acids with N-bound sulfoximidoyl groups. The protocol features excellent yields under ambient, metal-free conditions and short reaction times. Furthermore, the applicability of 2-sulfoximidoyl acetic acids as building blocks for synthesizing sulfoximine-based benzodiazepine analogues was demonstrated.
year | journal | country | edition | language |
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2021-04-09 | Organic letters |