- HCl·DMPU-assisted one-pot and metal-free conversion of aldehydes to nitriles
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We report an efficient HCl·DMPU assisted one-pot conversion of aldehydes into nitriles. The use of HCl·DMPU as both an acidic source as well as a non-nucleophilic base constitutes an environmentally mild alternative for the preparation of nitriles. Our protocol proceeds smoothly without the use of toxic reagents and metal catalysts. Diverse functionalized aromatic, aliphatic and allylic aldehydes incorporating various functional groups were successfully converted to nitriles in excellent to quantitative yields. This protocol is characterized by a broad substrate scope, mild reaction conditions, and high scalability. This journal is
- Hammond, Gerald B.,Mudshinge, Sagar R.,Potnis, Chinmay S.,Xu, Bo
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supporting information
p. 4161 - 4164
(2020/07/14)
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- Mechanism of bromoxynil phototransformation: Effect of medium and surfactant
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Bromoxynil (BXN, 3,5-dibromo-4-hydroxybenzonitrile) is a herbicide that is classified as a highly hazardous chemical, toxic for the reproduction. The processes and mechanisms regarding the fate of this compound in the environmental compartments subject to
- Bououden, Zelikha,Halladja, Sabrina,Sleiman, Mohamad,Leremboure, Martin,Richard, Claire
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p. 151 - 156
(2018/08/10)
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- Photoinduced Synthesis of Dibenzofurans: Intramolecular and Intermolecular Comparative Methodologies
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The SRN1 reaction has been used as a powerful tool for the synthesis of heterocycles, and only a few studies about photoinduced intramolecular cyclization to generate a new C-O bond by a radical pathway have been reported. This work introduces two strategies for the synthesis of substituted dibenzofurans by electron transfer (eT) reactions. The first one is a three-step process that comprises bromination of o-arylphenols, Suzuki-Miyaura cross-coupling and photoinduced cyclization in order to obtain the above-mentioned products. The second one is a metal-free procedure and does not require any photocatalyst. Different solvents were tested, and the yields ranged from low to moderate. A comparison was established between both methodologies, showing that the second one is the most suitable for the synthesis of dibenzofurans.
- Camargo Solórzano, Patricia,Brigante, Federico,Pierini, Adriana B.,Jimenez, Liliana B.
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supporting information
p. 7867 - 7877
(2018/06/11)
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- 2 - (3-cyano-4-alkoxy) phenyl-4-substituted thiazole-5- formic acid class compound, composition and its preparation and use
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The invention relates to a 2-(3-cyano-4-alkoxy) phenyl-4-substituted thiazole-5-formic acid compound which has xanthine oxidase inhibitory activity and is shown in a general formula I, a composition and preparation methods thereof. The invention also relates to applications of the compound and the composition thereof to preparation of medicaments for treating and/or preventing hyperuricemia and gout diseases. In the formula I, R2 is substituted or unsubstituted phenyl or a substituted or unsubstituted heteroaromatic radical, R1 is a substitutive aliphatic group of a straight chain or a branched chain, substituted or unsubstituted alicyclic hydrocarbonyl or substituted or unsubstituted aryl alkyl and A is an oxygen atom, a sulfur atom or a nitrogen atom.
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Paragraph 0101; 0102
(2016/10/07)
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- Intermediates for macrocyclic compounds
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The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
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Page/Page column 33; Sheet 8
(2015/11/30)
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- Hexamethonium bis(tribromide) (HMBTB) a recyclable and high bromine containing reagent
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A recyclable and high bromine containing di-(tribromide) reagent, hexamethonium bis(tribromide) (HMBTB) has been synthesized and utilized for the bromination of various organic substrates. The spent reagent hexamethonium bromide (HMB) can be effectively recycled by regenerating and reusing it without significant loss of activity. The crystalline and stable bis(tribromide) is an effective storehouse of very high percentage of active bromine requiring just half an equivalent of it for complete bromination. Both the Br3- moieties in HMBTB are nearly linear with Br-Br-Br angle of 179.55°.
- Paul, Bappi,Bhuyan, Bishal,Purkayastha, Debraj D.,Dhar, Siddhartha S.,Patel, Bhisma K.
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p. 5646 - 5650
(2015/09/21)
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- 4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS
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The present invention provides substituted 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly NAMPT inhibitors and in which R1 R2, Y, X, "Het" and "p" have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salts or stereoisomers or N-oxide thereof.
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Page/Page column 151
(2014/08/06)
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- A new recyclable 1,4-bis(3-methylimidazolium-1-yl)butane ditribromide [bMImB]·(Br3)2 ionic liquid reagent for selective bromination of anilines or phenols and α-bromination of alkanones under mild conditions
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1,4-Bis(3-methylimidazolium-1-yl)butane ditribromide [bMImB] ·(Br3)2 has been synthesized and explored as a new efficient brominating agent. The crystalline ditribromide reagent is stable for months and acts as a safe source of bromine requiring just 0.5 equiv. for complete bromination. It has a high active bromine content per molecule and shows a remarkable reactivity toward various substrates in acetonitrile at room temperature. The prepared reagents were used as a green recyclable reaction media for the selective bromination of anilines, phenols and α-bromination of alkanones in excellent yields. The product can easily be isolated by just washing the highly water soluble 1,4-bis(3-methylimidazolium-1-yl)butane ditribromide [bMImB]·(Br3)2 from the brominated product. The spent reagent can be recovered, regenerated, and reused without any significant loss. the Partner Organisations 2014.
- Veisi, Hojat,Sedrpoushan, Alireza,Mohammadi, Pourya,Faraji, Ali Reza,Sajjadifar, Sami
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p. 25898 - 25903
(2014/07/07)
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- Ruthenium-catalyzed intramolecular selective halogenation of O-methylbenzohydroximoyl halides: A new route to halogenated aromatic nitriles
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The intramolecular halogenation of O-methylbenzohydroximoyl halides in the presence of a Ru catalyst and the ligand diphenylacetylene afforded halo substituted aromatic nitriles in a highly regioselective manner. Further, substituted nitriles were converted into substituted tetrazole derivatives in the presence of NaN3 and I2.
- Chinnagolla, Ravi Kiran,Pimparkar, Sandeep,Jeganmohan, Masilamani
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supporting information
p. 3146 - 3148
(2013/06/04)
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- PROCESS TO PREPARE ETHYL 4-METHYL-2-(4-(2-METHYLPROPYLOXY)-3-CYANOPHENYL)-5-THIAZOLECARBOXYLATE
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Disclosed is a process for the preparation of Ethyl 4-methyl-2-(4-(2-methylpropyloxy)-3-cyanophenyl)-5-thiazolecarboxylate (I) the key intermediate for the preparation of [2-[3-cyano-4-(2-Methyl-propoxy)phenyl]-4-methyl-5-thiazole carboxylic acid (Febuxostat, I(A)) is approved under the trademark Uloric? by the US Food and Drug Administration for the treatment of hyperuricemia and gouty arthritis.
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Paragraph 0085; 0086; 0087; 0088
(2013/07/19)
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- IMPROVED PROCESS TO PREPARE ETHYL 4-METHYL-2-(4-(2-METHYLPROPYLOXY)-3-CYANOPHENYL)-5-THIAZOLECARBOXYLATE
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Disclosed is a process for the preparation of Ethyl 4-methyl-2-(4-(2-methylpropyloxy)-3-cyanophenyl)-5-thiazolecarboxylate (I) the key intermediate for the preparation of [2-[3-cyano-4-(2-Methyl-propoxy)phenyl]-4-methyl-5-thiazole carboxylic acid (Febuxostat, I(A)) is approved under the trademark Uloric ? by the US Food and Drug Administration for the treatment of hyperuricemia and gouty arthritis.
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Page/Page column 10
(2012/03/27)
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- Phosphonium salt-catalysed synthesis of nitriles from in situ activated oximes
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A metal-free catalytic method for the conversion of aromatic and aliphatic aldoximes to nitriles at room temperature using oxalyl chloride (1.2 equiv) in combination with 5 mol % of triphenylphosphine oxide is reported. Of the many potential pathways leading from oxime to nitrile a manifold involving chlorophosphonium salt-catalysed decomposition of oxime chlorooxalates formed in situ is shown to be operative.
- Denton, Ross M.,An, Jie,Lindovska, Petra,Lewis, William
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supporting information; experimental part
p. 2899 - 2905
(2012/05/05)
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- A practical and cost-efficient, one-pot conversion of aldehydes into nitriles mediated by 'activated DMSO'
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Participation of activated DMSO in the one-pot transformation of aldehydes to nitriles has been described by reacting aldehydes with NHHHCl in DMSO in the absence of any added base or catalyst. The method is applicable to access a wide range of aromatic, heterocyclic, and aliphatic nitriles, in which only water is a byproduct. A straightforward and practical procedure is demonstrated on a multigram scale. Georg Thieme Verlag Stuttgart - New York.
- Augustine, John Kallikat,Bombrun, Agnes,Atta, Rajendra Nath
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p. 2223 - 2227
(2011/10/31)
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- Synthesis and reactivity studies of a new reagent, ethyltriphenylphosphonium tribromide
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A new reagent, ethyltriphenyl phosphonium tribromide (ETPPTB), has been synthesized and studied. Results show that the reagent is quite efficient for various reactions such as organic bominations, acylations, and isothiocyanate preparation. Copyright
- Jamir, Latonglila,Alimenla,Kumar, Anil,Sinha, Dipak,Sinha, Upasana B.
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experimental part
p. 147 - 155
(2011/03/17)
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- PROCESS FOR THE PREPARATION OF 2-[3-CYANO-4-(2-METHYLPROPOXY)PHENYL]-4-METHYLTHIAZOLE-5-CARBOXYLIC ACID AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
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The present invention relates to novel and improved processes for the preparation of 2-[3-cyano-4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid compound of formula-1 and its pharmaceutically acceptable salts thereof. the present invention also provides the novel process for the preparation of crystalline forms of 2-[3-cyano-4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid compound of formula-1 and its intermediates.
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Page/Page column 44
(2011/12/02)
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- A PROCESS FOR THE PREPARATION OF FEBUXOSTAT
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The present invention relates to a process for the preparation of Febuxostat, useful in the pharmaceutical field for the treatment of the hyperuricemia.
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Page/Page column 14
(2010/12/29)
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- PHENOXY ACETIC ACID DERIVATIVES
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The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
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Page/Page column 78-79
(2010/09/03)
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- A new recyclable ditribromide reagent for efficient bromination under solvent free condition
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1,2-Dipyridiniumditribromide-ethane (DPTBE) has been synthesized and explored as a new efficient brominating agent. The crystalline ditribromide reagent is stable for months and acts as a safe source of bromine requiring just 0.5 equiv for complete bromination. It has high active bromine content per molecule and shows a remarkable reactivity compared to other tribromide reagents toward various substrates by just grinding the reagent and substrates in a porcelain mortar at room temperature. No organic solvent has been used during any stage of the reaction for substrates giving product as solid. Product can easily be isolated by just washing the highly water soluble 1,2- dipyridiniumdibromide-ethane (DPDBE) from the brominated product. The spent reagent can be recovered, regenerated, and reused without any significant loss.
- Kavala, Veerababurao,Naik, Sarala,Patel, Bhisma K.
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p. 4267 - 4271
(2007/10/03)
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