- Highly Enantioselective Hydrogenation of Amides via Dynamic Kinetic Resolution Under Low Pressure and Room Temperature
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High-throughput screening and lab-scale optimization were combined to develop the catalytic system trans-RuCl2((S,S)-skewphos)((R,R)-dpen), 2-PrONa, and 2-PrOH. This system hydrogenates functionalized α-phenoxy and related amides at room temperature under 4 atm H2 pressure to give chiral alcohols with up to 99% yield and in greater than 99% enantiomeric excess via dynamic kinetic resolution.
- Rasu, Loorthuraja,John, Jeremy M.,Stephenson, Elanna,Endean, Riley,Kalapugama, Suneth,Clément, Roxanne,Bergens, Steven H.
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supporting information
p. 3065 - 3071
(2017/03/11)
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- 2-(4-R-Phenoxy/phenylthio)alkanoic esters of l-lupinine
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Considering the great pharmacological interest in phenoxy/phenylthioalkanoic esters of open-chain or cyclic aminoalcohols, a set of ten such esters of lupinine was prepared. Initially, their ability to displace [3H]QNB from rat brain preparation was investigated. With the exception of two, all the prepared esters exhibited good affinity to muscarinic receptors (on a non-selective basis), with pKi in the range 6.67-7.68.
- Sparatore, Anna,Sparatore, Fabio
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p. 169 - 174
(2007/10/03)
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- Direct resolution of α-monoalkyl-α-aryloxyacetic acids via ester or imide derivatives
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This paper describes a simple procedure for the resolution of racemic α-monoalkyl α-aryloxyacetic acids, using the chromatographic separation of their covalent derivatives. (R)-Ethyl mandelate, (R)-pantolactone and (S)-4-(1-methylethyl)-2-oxazolidinone are the resolving agents involved in the formation of equimolecular diastereomeric mixtures of esters or imides. Chromatographic resolutions were performed by means of gas chromatography (GC), thin-layer chromatography (TLC) and flash chromatography. Successive hydrolysis of separated diastereomers provided optically pure aryloxyacetic acids.
- Amoroso, Rosa,Bettoni, Giancarlo,Tricca, Maria Luisa,Loiodice, Fulvio,Ferorelli, Savina
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- Synthesis of N- 2-pyrrolidinone as antimicrobial agent
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Several N- 2-pyrrolidinones have been synthesised and screened for their antibacterial and antifungal activities. their structures have been elucidated on the basis of elemental analysis and spectral data.
- Bhatt, P.,Srivastava, S. D.,Mehta, P.
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p. 514 - 516
(2007/10/03)
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- Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 2. 2-Phenoxy-, 2-(phenylthio)-, and 2-(phenylamino)alkanoic acid esters
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Further modifications of the leads ((R)-(+)-hyoscyamine and (p- chlorophenyl)propionic acid α-tropanyl ester), which show analgesic and nootropic activities as a consequence of increased central presynaptic ACh release, are reported. 2-Phenoxy- and 2-(phenylthio)alkanoic acid esters showed the best results. Several members of these classes possess analgesic properties which are comparable to that of morphine and at the same time are able to reverse dicyclomine-induced amnesia. Confirmation was found that the mechanism of action is due to an increase in ACh release at central muscarinic synapses and that both auto- and heteroreceptors controlling ACh release are very likely involved. According to the results obtained with (R)- (+)-hyoscyamine, analgesic activity is stereochemistry dependent, since the R-(+)-enantiomers are always more efficacious than the corresponding S-(-)- ones. On the basis of their potency and acute toxicity, compounds (±)-28 (SM21) and (±)-42 (SM32) were selected for further study.
- Gualtieri,Bottalico,Calandrella,Dei,Giovannoni,Mealli,Romanelli,Scapecchi,Teodori,Galeotti,Ghelardini,Giotti,Bartolini
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p. 1712 - 1719
(2007/10/02)
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- N-substituted glutamic acid derivative and process for production and use thereof
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N-substituted glutamic acid derivative and salt thereof, a process for production thereof comprising acylation of glutanic acid or derivative thereof, a herbicidal composition comprising the compound, and a method for killing or controlling plants using the compound. The compounds have a selective herbicidal effect.
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