- A simple method for the preparation of aryl trifluoromethyl ketones
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4-Dimethylamino-1-trifluoroacetylpyridinium trifluoroacetate (2) is an effective, easy to handle and stable trifluoroacetylation agent. Aryl trifluormethyl ketones 4 are obtained in good yields by reaction of 2 with aromatic compounds 3 in the presence of aluminum chloride.
- Simchen, Gerhard,Schmidt, Andreas
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- MgCl2-catalyzed trifluoromethylation of carbonyl compounds using (trifluoromethyl)trimethylsilane as the trifluoromethylating agent
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Using (trifluoromethyl)trimethylsilane (TMSCF3) as the trifluoromethylating agent, MgCl2-catalyzed trifluoromethylation of carbonyl compounds proceeded readily at room temperature. In the presence of 10 mol% of MgCl2, a variety of carbonyl substrates such as aliphatic/aromatic aldehydes, acyclic/cyclic ketones and esters could be trifluoromethylated in DMF, giving the corresponding trimethylsilyl ethers (ketals) in up to 93% isolated yields. Trifluoromethylketones could be readily obtained after hydrolysis of the trimethylsilyl ketals. The reactions could tolerate air and moisture, and the use of oxygen and moisture-free conditions was not required.
- Cui, Bin,Sun, Hui,Xu, Yibo,Duan, Lili,Li, Yue-Ming
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p. 6754 - 6762
(2017/11/09)
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- M -Azipropofol (AziP m) a photoactive analogue of the intravenous general anesthetic propofol
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Propofol is the most commonly used sedative-hypnotic drug for noxious procedures, yet the molecular targets underlying either its beneficial or toxic effects remain uncertain. In order to determine targets and thereby mechanisms of propofol, we have synthesized a photoactivateable analogue by substituting an alkyldiazirinyl moiety for one of the isopropyl arms but in the meta position. m-Azipropofol retains the physical, biochemical, GABAA receptor modulatory, and in vivo activity of propofol and photoadducts to amino acid residues in known propofol binding sites in natural proteins. Using either mass spectrometry or radiolabeling, this reagent may be used to reveal sites and targets that underlie the mechanism of both the desirable and undesirable actions of this important clinical compound.
- Hall, Michael A.,Xi, Jin,Lor, Chong,Dai, Shuiping,Pearce, Robert,Dailey, William P.,Eckenhoff, Roderic G.
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experimental part
p. 5667 - 5675
(2010/11/04)
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- Reactions of 1-aryl-2,2,2-trifluoroethanone oximes with tetrasulfur tetranitride: Novel synthesis of 5-Aryl-5-trifluoromethyl-4H-1,3,2,4,6-dithiatriazines and 1-Aryl-2,2,2-trifluoroethanonylidenaminosulfenamides
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The reactions of 1-aryl-2,2,2-trifluoroethanone oximes with tetrasulfur tetranitride (S4N4) in toluene at reflux gave 5-aryl-5-trifluoromethyl-4H-1,3,2,4,6-dithiatriazines 2, 1-aryl-2,2,2-trifluoroethanonylidenaminosulfenamides 3 and sulfur in 0-37%, 7-53%, and 2-41% yields, respectively. Treatment of 2 with tributyltin hydride in the presence of azobisisobutyronitrile in benzene at 80° afforded 3 in excellent yields.
- Kim, Kil-Joong,Lee, Hyi-Seung,Kim, Kyongtae
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p. 295 - 302
(2007/10/03)
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- A Convenient Trifluoroacetylation of Arenes with 2-(Trifluoroacetoxy)pyridine
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2-(Trifluoroacetoxy)pyridine (TFAP) is useful for trifluoroacetylating arenes under Friedel-Crafts conditions.Benzene, alkylbenzenes, naphthalene, and dibenzofuran have reacted with TFAP in the presence of aluminum chloride in dichloromethane to give the corresponding trifluoromethyl aryl ketones in good isolated yields.
- Keumi, Takashi,Shimada, Masakazu,Takahashi, Masahiro,Kitajima, Hidehiko
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p. 783 - 786
(2007/10/02)
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