- O2-Assisted Four-Component Reaction of Vinyl Magnesium Bromide with Chiral N-tert-Butanesulfinyl Imines To Form syn-1,3-Amino Alcohols
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An O2-assisted, four-component reaction has been developed to synthesize a wide range of syn-1,3-amino alcohols in one step. The reaction proceeds by oxygenation of vinyl magnesium bromide (component-I) with O2 (component-II) to give
- Gao, Lu,Luo, Jingfan,Song, Zhenlei,Wang, Runping,Zhang, Hongyun,Zheng, Chunmei
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supporting information
p. 24644 - 24649
(2021/10/12)
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- New IDO-1 INHIBITOR AND USE THEREOF
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The present invention refers to inhibit iDO-a 1 number and their use relates to search, more particularly by inhibiting the activity of the intracellular enzyme IDO (indoleamine-a 2,3 a-dioxygenase), which show excellent iDO-a 1 billion number number inhi
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Paragraph 0551; 0563; 0564; 0565
(2017/06/27)
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- Highly stereoselective syntheses of proline-derived vicinal amino alcohols through grignard addition onto N-tosylprolinal
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A highly diastereoselective Grignard addition to N-tosyl-l-prolinal has been developed to deliver a variety of proline-derived vicinal amino alcohols in good to excellent yields with high diastereoselectivities. A similar selectivity was also obtained by using N-tosyl-d-prolinal. The methodology has been applied to the synthesis of medicinally important 3-hydroxy-2-phenylpiperidines.
- Chaudhuri, Saikat,Parida, Amarchand,Ghosh, Santanu,Bisai, Alakesh
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supporting information
p. 215 - 220
(2016/01/20)
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- Oxidative desulfurization-fluorination of thioethers. Application for the synthesis of fluorinated nitrogen containing building blocks
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An oxidative desulfurization-fluorination protocol has been used to synthesize (2S)-2-(difluoromethyl)-N-tosylpyrrolidine (6a) and (2S)-2-(trifluoromethyl)-N-tosylpyrrolidine (7a) from the (2S)-prolinol-derived (2S)-2-(4-chlorophenylthiomethyl)-N-tosylpyr
- Hugenberg, Verena,Froehlich, Roland,Haufe, Guenter
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scheme or table
p. 5682 - 5691
(2011/02/18)
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- New aspects of catalytic intramolecular C-H amination: Unexpected formation of a seven-membered ring in nitrogen-containing systems
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The first example of the formation of a seven-membered ring by way of intramolecular-catalyzed amination of saturated C-H bonds is reported (Du Bois reaction). The influence of various structural parameters was studied, and it was shown that the unexpected regioselectivity observed in nitrogen-containing systems could be rationalized by conformational factors. These results open the way to innovative strategies for the general synthesis of polyfunctionalized piperidines.
- Toumieux, Sylvestre,Compain, Philippe,Martin, Olivier R.,Selkti, Mohamed
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p. 4493 - 4496
(2007/10/03)
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- Catalytic Asymmetric Intramolecular α-Alkylation of Aldehydes
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The development of a general catalytic asymmetric aldehyde α-alkylation reaction constitutes a major challenge in organic synthesis. Here, we report the first and successful approach toward its solution: (S)-α-methyl proline catalyzes the intramolecular a
- Vignola, Nicola,List, Benjamin
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p. 450 - 451
(2007/10/03)
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- Biphenyl derivatives and drug composition
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A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: [In the formula (1), A represents a single bond, —CH2—, —CO—, —CS— or —SO2—; B represents a single bond or —CH2—; R1represents a hydrogen atom, —OH, —NR11R12(wherein R11and R12each independently represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms), —OCOCH3, or a halogen atom; R2represents a hydrogen atom or R1and R2form a group ═O together; R3represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; provided that in the formula, the absolute configuration of the position a may be either R or S]. The compound of the present invention has considerably high safety and efficacy and is useful as, in particular, a vasopressin receptor antagonist.
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- Resolution and EPC Synthesis of Both Enantiomers of 2,5-Dimethylbicycloheptan-endo-2-ol, Key Intermediate in the Synthesis of Grandisol.
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The pure enantiomers of 2,5-dimethylbicycloheptan-endo-2-ol, key intermediate in the synthesis of grandisol, have been conveniently prepared by optical resolution with (2S)-(-)- and (2R)-(+)-1-(4-toluenesulphonyl)pyrrolidine-2-carboxylic acid chlor
- Rosini, Goffredo,Marotta, Emanuela,Raimondi, Andrea,Righi, Paolo
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p. 123 - 138
(2007/10/02)
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- Modified Di- and Tripeptides of the C-Terminal Portion of Oxytocin and Vasopressin as Possible Cognition Activation Agents
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A number of peptides and modified peptides were synthesized and studied for their ability to reverse electroconvulsive shock-induced amnesia in rodents.A few of these peptides were selected for secondary evaluation in tests of short-term memory in rats and aged rhesus monkeys.A number of the peptides and modified peptides were active in the amnesia reversal test.In selected secondary tests, however, the chosen compounds failed to show significant activity in enhancing memory.New methods for preparing methyleneamino and methyleneoxy isosters of peptides are reportrd.Other modified peptides also included methylenethio, methylenesulfonyl, and ethylene isosteres in place of the normal peptide amide bond.
- Nicolaides, E. D.,Tinney, F. J.,Kaltenbronn, J. S.,Repine, J. T.,DeJohn, D. A.,et al.
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p. 959 - 971
(2007/10/02)
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