5445-25-0Relevant academic research and scientific papers
MCL1 INHIBITORS
-
Paragraph 0747, (2021/05/21)
The present disclosure generally relates to compounds of Formula (I) and pharmaceutical compositions that may be used in methods of treating cancer.
Bromination of α-Diazo Phenylacetate Derivatives Using Cobalt(II) Bromide
Wang, Haifeng,Sun, Xiangli,Hu, Manman,Zhang, Xiaoyi,Xie, Lele,Gu, Shuangxi
supporting information, p. 3347 - 3351 (2020/07/04)
A method for the bromination of α-diazo phenylacetate derivatives using cobalt(II) bromide is described. This bromination reaction features a short reaction time, broad substrate scope, operational simplicity, acid-free conditions, and gram-scalability. (Figure presented.).
Synthesis of α,α-disubstituted α-amino esters: Nucleophilic addition to iminium salts generated from amino ketene silyl acetals
Hata, Shingo,Koyama, Hiroshi,Shimizu, Makoto
experimental part, p. 9670 - 9677 (2012/01/04)
Alkoxycarbonyl iminium species are prepared easily by the oxidation of tetrasubstituted amino ketene silyl acetals, and subsequent nucleophilic addition of Grignard reagents to the iminium salts gives α,α- disubstituted α-amino ester derivatives in moderate to good yields, in which aryl and ethynyl substituents are readily introduced.
THE METHOD OF MAKING OPTICALLY ACTIVE 2-HALO-2-(N-SUBSTITUTED PHENYL)ACETIC ACID ESTERS AND 2-HALO-2-(N-SUBSTITUTED PHENYL)ACETIC ACIDS BY ENZYMATIC METHOD
-
Page/Page column 6, (2008/06/13)
The present invention relates to the process for the preparation of optically active 2-halo-2-(n-substituted phenyl)acetic acid esters and optically active 2-halo-2-(n-substituted phenyl)acetic acids, which are used intensively as important chiral intermediates, represented by general formula 2 and 3 respectively from racemic 2-halo-2-(n-substituted phenyl)acetic acid ester represented by general formula 1. In more detail, this invention relates to the process for preparing optically active 2-halo-2-(n-substituted phenyl)acetic acid esters and optically active 2-halo-2-(n-substituted phenyl)acetic acids by stereospecific hydrolysis of racemic 2-halo-2-(n-substituted phenyl)acetic acid esters using hydrolases or hydrolase-producing microorganisms in the aqueous phase or organic phase including aqueous solvent. This method is useful in the practical process because the production and separation of compounds with high optical purity is easier.
Potential GABAB Receptor Antagonists. X* the Synthesis of Further Analogues of Baclofen, Phaclbfen and Saclofen
Prager, Rolf H.,Schafer, Karl
, p. 813 - 823 (2007/10/03)
In an attempt to obtain new compounds with binding activity at the GABAB receptor site, we report the synthesis of 3-amino-2-arylpropanoic acids, and the sulfonic, phosphonic and hydroxamic acid analogues. In addition, we report the synthesis of the isomer of phaclofen, 3-amino-1-(4-chlorophenyl)-propylphosphonic acid, and the higher homologue of baclofen, 5-amino-2-(4-chlorophenyl)pentanoic acid.
SYNTHESES D'ESTERS OU D'ACIDES α-HALOGENES A PARTIR DES GEM DICYANO EPOXIDES.
Robert, A.,Jaguelin, S.,Guinamant, J. L.
, p. 2275 - 2282 (2007/10/02)
α-halogeno esters or α-halogenoacids were easily prepared by selective one pot reaction of gem-dicyano epoxides with halohydric acids in an alcoholic or aqueous media.
Nematicidal 3-substituted-4-phenyl-1,2,5-thiadiazoles
-
, (2008/06/13)
A method for controlling nematodes in agricultural crops utilizing selected 3-substituted-4-phenyl-1,2,5-thiadiazoles, nematicidal compositions thereof, and novel compounds useful therefor are disclosed and exemplified.
1-Aryl-3-azabicyclohexanes, a New Series of Nonnarcotic Analgesic Agents
Epstein, Joseph W.,Brabander, Herbert J.,Fanshawe, William J.,Hofmann, Corris M.,McKenzie, Thomas C.,et al.
, p. 481 - 490 (2007/10/02)
A series of 1-aryl-3-azabicyclohexanes was synthesized by hydride reduction of 1-arylcyclopropanedicarboximides.Hydroxyphenyl analogues 20, 22, and 24 were prepared by EtSNa-DMF ether cleavage of the corresponding methoxyphenyl analogues 2m, 2n, and 23, respectively, with the secondary amines 20 and 22 going through the N-formyl intermediates 19 and 21.The p-ethoxy analogue 26 was obtained by O-ethylation of 19, followed by base hydrolysis of the amide 25.The greatest analgesic potency in mouse writhing and rat paw-pain assays was observed for para-substituted compounds.Bicifadine, 1-(4-methylphenyl)-3-azabicyclohexane (2b), was the most potent member of the series and is presently undergoing clinical trials in man.Analgesic activity of 2b is limited to the (+) enantiomer 2v, which has the 1R,5S absolute configuration as determined by single-crystal X-ray analysis.The N-methyl analogue (27d) of 2b showed significant analgesic potency, whereas the N-allyl (27a), N-(cyclopropylmethyl) (27b), and N-(n-hexyl) (27c) analogues were inactive.Bicifadine (2b) showed a nonnarcotic profile different from analogous azabicycloalkane and 3-phenylpyrrolidine analgesics.
