Fluoroform (CHF3) can be considered as an ideal reagent for difluoromethylation reactions. However, due to the low reactivity of fluoroform, only very few applications have been reported so far. Herein we report a continuous flow difluoromethylation protocol on sp(3) carbons employing fluoroform as a reagent. The protocol is applicable for the direct C-alpha-difluoromethylation of protected alpha-amino acids, and enables a highly atom efficient synthesis of the active pharmaceutical ingredient eflornithine.
Utilization of fluoroform for difluoromethylation in continuous flow: a concise synthesis of α-difluoromethyl-amino acids
Ciaglia, Tania;
2018-01-01
Abstract
Fluoroform (CHF3) can be considered as an ideal reagent for difluoromethylation reactions. However, due to the low reactivity of fluoroform, only very few applications have been reported so far. Herein we report a continuous flow difluoromethylation protocol on sp(3) carbons employing fluoroform as a reagent. The protocol is applicable for the direct C-alpha-difluoromethylation of protected alpha-amino acids, and enables a highly atom efficient synthesis of the active pharmaceutical ingredient eflornithine.File in questo prodotto:
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