Hydroxytrifluoromethylation of Alkenes Using Fluoroform-Derived CuCF3
Hydroxytrifluoromethylation of alkenes using the fluoroform (CF3H)-derived [CuCF3] reagent is described. In the presence of additive B2Pin2 and air, this reagent effectively facilitates the addition of hydroxy and trifluoromethyl groups across an alkene double bond, a formal hydroxytrifluoromethylation process. Various β-trifluoromethyl alcohols can be synthesized from simple alkenes where the ultimate CF3 source is the industrial byproduct fluoroform.
A facile method for hydroxytrifluoromethylation of alkenes with Langlois reagent and DMSO
A practical hydroxytrifluoromethylation of alkenes using the Langlois reagent as the trifluoromethyl source and DMSO as the oxidant is described. This reaction is mild and operationally simple, without exclusion of either moisture or oxygen, allowing access to a wide range of β-trifluoromethyl alcohols in useful yields. This transformation is environmentally friendly and can be easily scaled up to gram level.
NMP and O2 as Radical Initiator: Trifluoromethylation of Alkenes to Tertiary β-Trifluoromethyl Alcohols at Room Temperature
A novel strategy was developed to trigger ·CF3 by using in situ generated peroxide in NMP under O2 or air as the radical initiator. Radical trifluoromethylation of alkenes was achieved toward tertiary β-trifluoromethyl alcohols. Various tertiary β-trifluoromethyl alcohols can be synthesized in good yields without extra oxidants or transition metal catalysts. Preliminary mechanistic investigation revealed that O2 diffusion can influence the reaction rate.
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is i
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(2010/11/08)
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