- Heterogeneous magnetic catalyst for S-arylation reactions
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A convenient method for the synthesis of monodisperse, superparamagnetic copper ferrite (CuFe2O4) nanoparticles with high surface area has been described. The synthesized material was characterized by various techniques. XRD showed the nanocrystalline nature of CuFe2O 4 with a crystallite size of 6 nm. TEM analysis showed that uniform spherical CuFe2O4 particles are formed with a size of 55 ± 5 nm. N2 adsorption/desorption measurements confirmed the mesoporous nature of the sample with surface area >216 m2 g -1. The field dependent magnetization, illustrated by VSM and saturation magnetization was found to be 44 emu g-1. The catalytic applications of the synthesized CuFe2O4 nanoparticles were explored for the cross-coupling of thiols with diverse range of aryl halides. Aryl iodides and bromides result in biarylsulfides in good to excellent yields (62-98%) whereas aryl chlorides gave significant amount of diaryldisulfide. Scope of this catalytic protocol further extended to one-pot synthesis of biologically important tricyclic dibenzothiazepines. The superparamagnetic nature of CuFe2O4 nanoparticles was found to be advantageous for their easy, quick and quantitative separation from the reaction mixture. Negligible leaching of Cu and Fe in consecutive cycles makes the catalyst economical and environmentally benign.
- Panda, Niranjan,Jena, Ashis Kumar,Mohapatra, Sasmita
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- Coupling of thiols and aromatic halides promoted by diboron derived super electron donors
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We have proven that pyridine-boryl complexes can be used as superelectron donors to promote the coupling of thiols and aromatic halides through a SRN1 mechanism. The reaction is efficient for a broad substrate scope, tolerating heterocycles including pyridines, enolizable or reducible functional groups. The method has been applied to intermediates in drug synthesis as well as interesting functionalized polythioethers through a controlled and consecutive intramolecular electron transfer process.
- Franco, Mario,Vargas, Emily L.,Tortosa, Mariola,Cid
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supporting information
p. 11653 - 11656
(2021/11/12)
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- A process for the preparation of intermediates quetiapine (by machine translation)
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The invention discloses a preparation method for a quetiapine intermediate. The preparation method comprises: taking thiosalicylic acid as an initial raw material to prepare 2-nitro-2'-carboxyldiphenyl sulfide, esterifying and reducing, and then performing intramolecular amino-ester exchange reaction for cyclization, so as to obtain the quetiapine intermediate 10,11-dihydro-11-oxodibenzo[b,f][1,4]thiazepine. The preparation method is simple, the target product is high in purity, the reaction yield is relatively high, the production cost is effectively reduced, and industrialized production of the high-purity quetiapine intermediate is facilitated to be realized.
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Paragraph 0021
(2017/02/24)
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- Syntheses of the tricyclic cores of clozapine, dibenzo[b,f][1,4]thiazepin- 11(10H)-one, and dibenzo[b,f][1,4]oxazepin-11(10H)-one in C-14 labeled form by [14C]carbonylation
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Clozapine has been demonstrated to bind covalently to proteins as a result of metabolic activation that has been proposed to be a precursor to the serious side effects including death that occur in a small percentage of the population. The covalent modifi
- Elmore, Charles S.,Dorff, Peter N.,Richard Heys
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p. 787 - 792
(2013/01/09)
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