Establishment of a modular, sequential synthesis method based on switchable active linkers, products and uses thereof

Abstract

The application belongs to the field of organic synthesis, and relates to a bifunctional compound containing an alkenyl group and a sulfonyl fluoride which can be used as a switchable active linker, and a novel method for orderly linking of different nucleophiles. The method constructs intramolecular non-covalent interaction through Michael addition reaction of N-nucleophiles and the alkenyl end of the switchable active linker, thereby changing the reaction activity of the sulfonyl fluoride end of the linker, so that it can further react with various O- / N-nucleophiles to realize orderly linking between different nucleophiles. Compared with the traditional method of ensuring the orderly reaction by introducing and removing a protecting group, the method for orderly linking of the compound disclosed by the application reduces the operation and time cost of the synthesis process, and the reaction condition is mild and simple, and the reaction reagent is cheap and easy to obtain. In addition, the application also discloses a class of alkyl sulfonate and / or sulfonamide compounds synthesized by the method and the application of the alkyl sulfonate and / or sulfonamide compounds in medicine, materials and the like.

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