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Assessing the Bioisosterism of the Trifluoromethyl Group with a Protease Probe

✍ Scribed by Monika Jagodzinska; Florent Huguenot; Gabriele Candiani; Matteo Zanda


Publisher
John Wiley and Sons
Year
2009
Tongue
English
Weight
184 KB
Volume
4
Category
Article
ISSN
1860-7179

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✦ Synopsis


Scheme 1. Synthesis of the key fluorinated intermediate 8. Reagents and conditions: a) BnBr, NaH; b) 1. Mg, 2. CF 3 CO 2 Et; c) NaH, CS 2 , CH 3 I, THF; d) H 3 PO 2 , TEA, AIBN, dioxane, reflux; e) H 2 /Pd(OH) 2 , EtOAc; f) PPh 3 , CBr 4 , CH 2 Cl 2 .


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Iridium-Catalyzed Reactions of Trifluoro
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## Abstract **Catalytic convenience**: The use of iridium or ruthenium catalysts for Cο£ΏH bond activation has led to the addition reaction of trifluoromethylated compounds to alkenes (see scheme). This atom‐economical reaction occurs under neutral reaction conditions and without the formation of und