- Magnesium catalyzed dephenylsulfonylation: Synthesis of 5-ethyl-1H-indole
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A novel magnesium metal catalyzed synthesis of 5-ethyl-1H-indole from 5-[2-(phenyl sulfonyl)ethyl]-1H-indole by dephenylsulfonylation mechanism providing an alternative and attractive approach to 5-ethyl-1H-indole with high yields. This approach is for both the protected and unprotected indoles.
- Rao, S. Venkat,Shrikant, H. Havale,Kumar, B. Sanjith,Krishna, G. Siva
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- A Low Rhodium Content Smart Catalyst for Hydrogenation and Hydroformylation Reactions
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Abstract: This paper describes the preparation, broad characterization and study of activity in hydrogenation and hydroformylation reactions of an easily produced 0.18% Rh/Al2O3. Analytical studies on fresh and recycled samples shed light on the smart properties of such catalyst. Results showed high activity as well as fine/excellent chemoselectivity or regioselectivity, characteristics that may suggest a wide range of applicability. Graphic Abstract: The low metal content catalyst 0.18% Rh/Al2O3 was very active in both hydrogenation and hydroformylation reactions so providing intermediates for valuable APIs, as Nabumetone and Eletriptan, and a fragrance with a fresh, green-floral smell, that recalls scent of lily of the valley.[Figure not available: see fulltext.]
- Paganelli, Stefano,Tassini, Riccardo,Rathod, Vikas D.,Onida, Barbara,Fiorilli, Sonia,Piccolo, Oreste
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p. 1508 - 1521
(2020/10/15)
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- Synthesis of (Z)-5-[(5-(2-(Phenylsulfonyl-ethyl)-1H-indol-3-yl)methelene]- thiozolidine-2,4-dione of potential pharmacological interest
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Formylation of 5-bromoindole (1) under Vilsmeier-Hack formylation conditions using POCl3 and DMF as a reagents under cooling conditions (0-5 °C) followed by simple processing gave a 5-bromoindole-3- carboxyaldehyde (2) and condensation of (2) with thiazolidine-2,4-dione (3) in toluene as a solvent in the presence of PTSA and TBAB as a phase transfer catalyst under stirring at room temperature for 10-30 min, then slowly raise the temperature to 105 °C and maintained for 12-15 h, obtained a product(Z)-5-((5-bromo-1-alkyl-1H-indol-3-yl)methylene)thiazolidine-2,4-dione (4) later on condensation of (4) with phenylvinylsulfone (5) in the presence of palladium acetate as a catalyst in DMF as a solvent heating at 100-105 °C for 16 h gave (5Z)-5-((1-alkyl-5-((E)-2(-(phenylsulfonyl)vinyl)-1H-indol-3-yl) methelene)thiozolidine-2,4-dione (8) and on reduction of (8) in the presence of hydrogen gas, palladium-carbon by using catalytic amount acetic acid medium in methanol as a solvent heating at 45-50 °C for 8 h gave (Z)-5-((1-alkyl-5-(2- (-(phenylsulfonyl)ethyl)-1Hindol-3yl)methelene)thiozolidine-2,4-dione (11) and 11 could also be prepared by alternate methods structure of 11 has been established on the basis of its spectral and analytical data. Copyright
- Laxminarayana, Keetha,Rajendiran, Chinnapillai,Mukkanti, Khagga
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p. 1661 - 1665
(2013/05/09)
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- A NOVEL PROCESS FOR THE PREPARATION OF ELETRIPTAN
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The present invention relates to a novel process for the preparation of (R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole and its intermediates thereof.
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Paragraph 0030
(2013/07/25)
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- One-pot three-component sulfone synthesis exploiting palladium-catalysed aryl halide aminosulfonylation
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A palladium-catalysed aminosulfonylation process is used as the key-step in a one-pot, three-component sulfone synthesis. The process combines aryl-, heteroaryl- and alkenyl iodides with a sulfonyl unit and an electrophilic coupling fragment. The sulfonyl unit is delivered in the form of an aminosulfonamide, which then serves as a masked sulfinate. The sulfinate is combined, in situ, with an electrophilic coupling partner, such as a benzylic, allylic or alkyl halide, an electron-poor arene, or a cyclic epoxide, to provide the corresponding sulfone products in good to excellent yields. The mild reaction conditions and use of commercially available reaction components allows the easy preparation of a broad range of sulfones featuring a variety of functional groups. The process obviates the need to employ thiol starting materials, and oxidative operations.
- Richards-Taylor, Charlotte S.,Blakemore, David C.,Willis, Michael C.
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p. 222 - 228
(2014/01/06)
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- NOVEL PROCESS FOR THE PREPARATION OF ELETRIPTAN
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The present invention relates to a novel process for the preparation of (R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole and its intermediates thereof.
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Page/Page column 3
(2011/09/16)
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- SYNTHESIS OF NOVEL 5-(2-(PHENYLSULFONYL)ETHYL)-1H-INDOLE DERIVATIVES
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An objective of the present invention is to develop commercially viable methods for the synthesis of 5-[2-phenylsulfony)ethyl]-1H-indole of Formule (II), where R1 and R2 are same or different and each independently represent a hydrog
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