Method for catalytically synthesizing chiral quaternary carbon-containing 2,5-dihydrothiophene compound

• Main Authors: XIAO LINJIU, ZHAO YANAN, LAN LIYAN, ZHU XIAOYU, LI WENZE
• Format: Patent
• Language: Chinese; English
• Published: 18.05.2018
• Subjects: APPARATUS THEREFOR; CHEMISTRY; GENERAL METHODS OF ORGANIC CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention belongs to an organic chemical synthesis method and discloses a method for catalytically synthesizing a chiral quaternary carbon-containing 2,5-dihydrothiophene compound. The method comprises the following steps of taking mercaptoacetaldehyde and alpha-aryl-beta-nitro-tert-butyl acrylate as raw materials, tetragonal amide containing quinine and 3,5-dimethylphenyl structure as a catalyst and 5-molecular sieve as an additive, performing sulfa-Michael/Aldol tandem reaction in chloroform serving as a solvent until reaction is finished, and directly adding trifluoroacetic anhydride and triethylamine for dehydration reaction without separating an intermediate to obtain a target product. Based on a mode of hydrogen bond catalysis, the method provided by the invention adopts simple,rapid and efficient one-pot method tandem reaction, the raw materials and the catalyst are simple and easy to obtain, the reaction condition is mild, the operation is simple and the atom economy is good; the method is capable