- Phase-transfer alkylation reactions using microreactors
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Phase-transfer alkylation in a microreactor proceeds smoothly, and the reaction has been found to be more efficient than that in a round-bottomed flask with vigorous stirring; we have observed by an optical microscope study that an interfacial area provid
- Ueno, Masaharu,Hisamoto, Hideaki,Kitamori, Takehiko,Kobayashi, Shu
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Read Online
- INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION
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Compounds of Formula (I) and methods of inhibiting the replication of viruses in a biological sample or patient, of reducing the amount of viruses in a biological sample or patient, and of treating a virus infection in a patient, comprising administering to said biological sample or patient an effective amount of a compound represented by Formula (I), a compound of Table A or B or a pharmaceutically acceptable salt thereof.
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Paragraph 00600-00602; 00684-00686
(2021/10/15)
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- Oxime-mediated oxychlorination and oxybromination of unactivated olefins
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An oxime-mediated oxychlorination and oxybromination of unactivated olefins relying on palladium catalysis has been developed. A wide range of chlorinated and brominated isoxazolines has been synthesized in moderate to good yields. To demonstrate the value of the method, the brominated isoxazoline has been further converted to other useful synthetic feedstock.
- Dong, Kui-Yong,Qin, Hai-Tao,Liu, Feng,Zhu, Chen
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supporting information
p. 1419 - 1422
(2015/03/04)
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- Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists
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Systematic SAR optimization of the GPR119 agonist lead 1, derived from an internal HTS campaign, led to compound 29. Compound 29 displays significantly improved in vitro activity and oral exposure, leading to GLP1 elevation in acutely dosed mice and reduc
- Azimioara, Mihai,Alper, Phil,Cow, Christopher,Mutnick, Daniel,Nikulin, Victor,Lelais, Gerald,Mecom, John,McNeill, Matthew,Michellys, Pierre-Yves,Wang, Zhiliang,Reding, Esther,Paliotti, Michael,Li, Jing,Bao, Dingjiu,Zoll, Jocelyn,Kim, Young,Zimmerman, Matthew,Groessl, Todd,Tuntland, Tove,Joseph, Sean B.,McNamara, Peter,Seidel, H. Martin,Epple, Robert
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supporting information
p. 5478 - 5483
(2015/01/09)
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- Construction of functionalized carbocycles having contiguous tertiary carbinol and all-carbon stereogenic centers
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A highly stereoselective protocol is reported for customizing functionalized carbocyclic building blocks (β-hydroxy esters) and bicyclic lactones with a stereoarray that contains contiguous tertiary carbinol and all-carbon stereocenters. The efficient asymmetric induction and diastereofacial selective addition of allyl and propargyl indiums to hindered α,α-disubstituted cycloalkanones is presented. The stereochemistry of representative products was unequivocally established from single-crystal X-ray crystal structure analyses, and a plausible reaction pathway was proposed to support the high diastereofacial selectivity.
- Reddy, Chennakesava,Babu, Srinivasarao Arulananda,Aslam, Nayyar Ahmad,Rajkumar, Vadla
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p. 2362 - 2380
(2013/05/22)
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- Synthesis of cationic dibenzosemibullvalene-based phase-transfer catalysts by di-π-methane rearrangements of pyrrolinium-annelated dibenzobarrelene derivatives
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Dibenzobarrelene derivatives, that are annelated with a pyrrolinium unit [N,N-dialkyl-3,4-(9′,10′-dihydro-9′,10′-anthraceno-3- pyrrolinium) derivatives], undergo a photo-induced di-π-methane rearrangement upon triplet sensitization to give the corresponding cationic dibenzosemibullvalene derivatives [N,N-dialkyl-3,4-{8c,8e-(4b,8b- dihydrodibenzo[a,f]cyclopropa[cd]pentaleno)}-pyrrolidinium derivatives]. Whereas the covalent attachment of a benzophenone functionality to the pyrrolinium nitrogen atom did not result in an internal triplet sensitization, the introduction of a benzophenone unit as part of the counter ion enables the di-π-methane rearrangement of the dibenzobarrelene derivative in the solid-state. Preliminary experiments indicate that a cationic pyrrolidinium-annelated dibenzosemibullvalene may act as phase-transfer catalyst in alkylation reactions.
- Ihmels, Heiko,Luo, Jia
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supporting information; experimental part
p. 119 - 126
(2011/05/15)
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- Photoinduced radical reactions of α-alkylated ethyl 2-oxo-1-cyclopentanecarboxylate derivatives: α-cleavage and cyclization to the skeleton of linear cyclohexano diquinanes
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The tricyclic core of linear cyclohexano diquinanes was synthesized using photoinduced electron transfer (PET) as a key step. The reaction proceeded in high regioselective manner via ketyl radical anions leading to distonic δ-keto radical anion as reactive intermediates. The irradiation was carried out at a wavelength of 254 nm with triethylamine (TEA) as a strong reducing reagent in acetonitrile. We also showed that the photolysis of the α-alkylated 2-oxocyclopentanecarboxylate derivatives does not lead to any cyclization products via a δ-hydrogen abstraction process. In this case α-C-C bond cleavage as a predominant process was observed.
- Tzvetkov, Nikolay T.,Waske, Prashant A.,Neumann, Beate,Stammler, Hans-Georg,Mattay, Jochen
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p. 1710 - 1713
(2008/09/19)
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- Cyclopentane carboxylate compounds, process and intermediates for preparing the same and use thereof
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The present invention discloses cyclopentane carboxylate compounds. The 1-hydrocarbyl-2-acyloxy-cyclopentane carboxylates according to the invention have a general formula (I): wherein groups R1, R2 and R3, which are ident
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Page/Page column 9
(2010/11/08)
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- CYCLOPENTANE CARBOXYLATE COMPOUNDS, PROCESS AND INTERMEDIATES FOR PREPARING THE SAME AND USE THEREOF
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The present invention discloses cyclopentane carboxylate compounds. The I-hydrocarbyl-2-acyloxy-cyclopentane carboxylates according to the invention have a general formula (I): wherein groups R1, R2 and R3, which are ident
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Page/Page column 17
(2010/11/08)
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- Synthesis of alkylated iridolactone analogs
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Bicyclic δ-lactones, iridolactones analogs with an alkyl group at the bicyclic junction, are obtained from α-alkyl-α-hydroxymethylcyclopentanones via an intramolecular Horner-Wadsworth-Emmons reaction.
- Guerrab, Zineb,Daou, Boujemaa,Fkih-Tetouani, Souad,Ahmar, Mohammed,Cazes, Bernard
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p. 5727 - 5730
(2007/10/03)
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- The synthesis of 5-substituted 6-oxo-2-piperidinecarboxylic acid derivatives from cyclopentanone-β-ketoesters
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Ethyl 2-oxocyclopentanonecarboxylate was converted to 5-substituted 6-oxopiperidinecarboxylic derivatives via a synthetic sequence consisting of a) C-1-alkylation of the cyclopentanone-β-ketoester b) introduction of a protected amino group at the α'-position (C-3) of the cyclopentanone carbonyl group via bromination and substitution with phthalimide c) base promoted ring opening of the disubstuted cyclopentanone-β-ketoester to form the corresponding diester or ester-acid derivatives and d) final deprotection of the amino group with concomitant ring closure to produce the title compounds.
- Compernolle, Frans,Baens, Nicole,Hoornaert, Georges J.
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p. 433 - 438
(2007/10/03)
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- Utilization of Me3SiSnBu3 in organic synthesis I. Generation of stannyl anion from Me3SiSnBu3 and R4NX
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A metal free stannyl anion generated from Me3SiSBu3 and R4NX in DMF reacted with an aryl halide bearing carbonyl group to produce an aryl anion via the so-called halogen-metal exchange process, which reacted with a carbonyl group to afford a cyclized product in good yield.
- Mori, Miwako,Kaneta, Naotake,Isono, Naohiro,Shibasaki, Masakatsu
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p. 255 - 260
(2007/10/02)
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