Patent · US Active

1,4-sulfur-bridged polycyclic compounds containing dihydrobenzofuran structure, its preparation method and application thereof

US12162897B2 · kind B2 · utility

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8Claims
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Inventors

Key dates

Filing dateMar 18, 2022
Grant dateDec 10, 2024
Priority date
Expiry dateMar 18, 2042

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61K31/429
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

The present invention discloses a 1,4-sulfur-bridged polycyclic compound containing dihydrobenzofuran structure which has a structural formula (I). A preparation method is also disclosed which includes the steps of: dissolving 2-nitrobenzofuran (II) and 5H-thiazolone (III) in an organic solvent; then adding molecular sieve and chiral catalyst, stirring and allowing reaction at room temperature under argon protection until the reaction is completed; and carrying out separation and purification to obtain a 1,4-sulfur-bridged polycyclic compound (I) containing dihydrobenzofuran structure. The polycyclic compounds of the present invention have a substructure of dihydrobenzofuran and 1,4-thiopiperidinone. The application of the compound for the preparation of antitumor drugs is also disclosed, which has a good potential value in antitumor drug research. The preparation method has the advantages of novelty, simplicity, simple operation, mild reaction conditions, high yield and high stereoselectivity, and etc.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.