科研之友
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摘要
Aryl- and amino-substituted pyrimidine C-nucleoside analogs have been synthesized in good to excellent yields by one-pot coupling of terminal sugar alkynes, substituted benzoyl chlorides, and amidine salts. The reaction conditions are tolerant of various structurally complex sugars having sterically bulky groups, unprotected hydroxyl groups, and sensitive substituents. The sugar alkynes include structurally diverse pyranosides, acyclic glycosides, and furanosides. The substituted benzoyl chlorides bear electron-withdrawing and -donating substituents with different steric hindrance. The amidine salts include acetamidine hydrochloride, benzamidine hydrochloride, and guanidine hydrochloride.
