Trifluoromethyl ketones can be prepared in good yield from primary carboxylic acid chlorides by reaction with pyridine and trifluoroacetin anhydride followed by aqueous work up.
Beginning with the weakly active lead structure 1, a new series of hPPAR agonists was developed. In vivo glucose and triglyceride lowering activity was obtained by homologation and oxamination to 3, then conversion to substituted benzisoxazoles 4 and 5. Further manipulation afforded benzofurans ...
At 340 °C, toluene gave five 1-trifluoromethyl-substituted compounds:- -2H,4H,5H-tetrafluorocyclohexa-1,4-diene (IX); -2H-4H/5H-hexafluorocyclohex-1-ene (X); -2H-octafluorocyclohex-1-ene (IV); -nonafluorocyclohex-1-ene (III); also perfluoromethylcyclohexane (II); traces of perfluorocyclohexane ...
This review divides the acidic deep eutectic solvents (ADES) into Brønsted and Lewis DES according to their diversity of acidic character. The hydrogen bond donors and halide salts for formulating an ADES are classified, the synthesis methods are described, and the physicochemical properties inc...
An efficient chemoenzymatic route was developed for synthesis of (S)-α-amino-4-fluorobenzeneacetic acid, a valuable chiral intermediate of Aprepitant, using immobilized penicillin amidase catalyzed kinetic resolution of racemic N-phenylacetyl-4-fluorophenylglycine. The optimum temperature, pH a...
The functionality of hydroxypropylsulfanyl units of metal-free and metallo-porphyrazines, which are new compounds (M = 2H, Mg, Co, Cu or Zn), has been produced by esterification with a carboxylate group such as 2-fluoro-5-(trifluoromethyl)phenylacetic acid. The symmetrically functionalized porph...
The first layered hydroxylammonium fluorometalates, (NH3OH)2CuF4 and (NH3OH)2CoF4, were prepared by the reaction of solid NH3OHF and the aqueous solution of copper or cobalt in HF. Both compounds crystallize in monoclinic, P21/c, unit cell with parameters: a = 7.9617(2) Å, b = 5.9527(2) Å, c = 5...
This paper presents the study of electrolytic decomposition of hydroxylammonium nitrate (HAN) ionic liquid in a transparent microreactor. The decomposition phenomena was captured using a high speed camera system. The captured images were post processed to study the effect of number of electrodes...
A new hydroxylammonium compound (NH3OH)2SiF6, has been synthesized by the addition of solid NH3OHF to an aqueous solution of H2SiF6. The compound was characterized by chemical analysis and X-ray powder diffraction, the thermal decomposition was studied by thermal analysis and mass spectrometry. ...
A new hydroxylammonium compound (NH3OH)2GeF6, has been synthesized by the addition of solid NH3OHF to a solution of GeO2 dissolved in 20% HF. The compound was characterized by chemical analysis and X-ray powder diffraction, the thermal decomposition was studied by thermal analysis and mass spect...
New hydroxylammonium fluorometallates of manganese and scandium, with the formulas (NH3OH)2MnF4 and (NH3OH)3ScF6, were prepared by the reactions of hydroxylammonium fluoride with solutions of manganese or scandium in aqueous HF. (NH3OH)2MnF4 crystallizes monoclinic, P21/c, the structure consisti...
2-Trifluoromethyl and 2-difluoromethyl substituted benzimidazole, benzoxazole and benzothiazole derivatives were efficiently prepared through a one-pot reaction of trifluoroacetic acid and difluoroacetic acid, respectively, with commercially available o-phenylenediamines, 2-aminophenols, and 2-a...
A review of difluoromethylene compounds as precursors to carbonyl compounds. Many ketones, carboxylic acids, esters, amides and carbonates, especially trifluoroalanine dipeptides, can be easily achieved due to the reactivity of difluoromethylene compounds or generated through the reactive difluo...
The first N-containing trifluorovinyl ether monomer (CF3)2NCF2OCFCF2 was synthesized. The starting perfluoroalkyl imine CF3–NCF2 was converted to the perfluoroalkyl amine (CF3)2NH by HF. The amine was converted into the carbamoyl fluoride (CF3)2NC(O)F via reaction with carbonyl fluoride COF2 in...
A new fluorine-containing synthon, R1COCF2SO2R2 (2, R1, R2=morpholino, piperidino, etc.), was developed for the introduction of difluoromethylene sulfonamide or difluoromethylene group. Under different conditions, 2 reacted readily with aromatic aldehydes to give the corresponding difluoromethyl...
An unprecedent transition-metal-free protocol for the synthesis of β-ketoamides from β-ketoesters is described. This method involves selective cleaving NP bond of an unusual aminating reagent, [tris(dimethylamino)phosphonio]difluoroacetate (ADFA), which is well known as the difluoromethylene y...
A comprehensive profile of prasugrel HCl is reported herein with 158 references. A full description including nomenclature, formulae, elemental analysis, and appearance is included. Methods of preparation for prasugrel HCl, its intermediates, and derivatives are fully discussed. In addition, the...
Epoxidation of 3-methoxy-16-methylene-estra-1,3,5(10)-trien-17-one in the presence of alkaline hydrogen peroxide gives rise to (16R)- and (16S)-spiro[3-methoxy-17-oxoestra-1,3,5(10)-triene-16,2′-oxirane] in similar proprotions. Epoxidation of the corresponding 16-methylene 17μ-alcohol and 16-m...
The synthesis of two novel radiolabelled estrogen derivatives, [125I](E)-3-methoxy-17α-iodovinylestra-1,3,5(10),6-tetraen-17β-ol (E[125I]IVDE) and [125I](Z)-3-methoxy-17α-iodovinylestra-1,3,5(10),6-tetraen-17β-ol (Z[125I]IVDE), was carried out aiming to study the influence of the introductio...
Three coordination complexes of Co(II)/Fe(II) with 4,4′-trimethylenedipyridine (bpp) and pseudohalides (SCN−, SeCN− and N3−) have been synthesized. The complexes have been characterized by X-ray single crystal structure determination. They are isomorphous having 2D layers in which two independe...
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