One-Pot, Atom and Step Economy (PASE) Assembly of Trifluoromethylated Pyrimidines from CF3 -Ynonesстатья
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Дата последнего поиска статьи во внешних источниках: 5 октября 2017 г.
Аннотация:A highly efficient synthetic method for the preparation of of 6-trifluoromethylated pyrimidines was developed. The reaction of CF3-substituted ynones and nitrogen 1,3-bis(nucleophile)s was employed for the one-pot assembly of the pyrimidine core. The cascade route proceeded through an aza-Michael addition, intramolecular cyclization, and dehydration reaction sequence to give the target heterocycles in excellent yields (up to 97 %). When acetamidine was used as the bis(nucleophile), the unexpected addition of two equivalents of the CF3-substituted ynone to the acetamidine was observed.