Trifluoromethoxyarenes were identified as halide surrogates in Ni-catalyzed couplings with arylboronic acids, potassium aryl trifluoroborates and aryl trialkoxysilanes, under mechanochemical conditions. Unusual reactivity of potassium benz...
Artikel
The Asymmetric Construction α‐CF2H Pyrrolidine via 1,3‐Dipolar Cycloaddition of N‐2,2‐Difluoroethylthioisatin Ketoimines with Meldrum's Acid Derived Electron‐Deficient Olefins
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An efficient organocatalytic 1,3-dipolar cycloaddition of N-2,2-difluoroethylthioisatin ketoimines with Meldrum's acid derived electron-deficient olefins was described. The fused ring compound with certain anti-tumor activity was easily achieved through a convenient transformation.
Abstract
We report here a directly catalytic asymmetric method in the construction of CF2H-containing pyrrolidines. A variety of enantioenriched difluoromethylated pyrrolidine (34 examples, up to 97% ee) were obtained on a 1, 3-dipole cycloaddition model. The subsequent hydrolysis reaction provides a new difluoromethyl substituted fused ring compound which has certain anticancer activity.
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