55984-17-3Relevant articles and documents
Chemoenzymatic synthesis of both enantiomers of 2-chloro-1-(2-furyl)ethanol
Gercek, Zuhal,Karakaya, Devrim,Demir, Ayhan S.
, p. 1743 - 1746 (2005)
Enzyme catalyzed transesterification of rac-2-chloro-1-(2-furyl)ethanol rac-1 using vinyl acetate afforded the enantiomers of 2-chloro-1-(2-furyl) ethanol 1 and 2-chloro-1-(2-furyl)ethyl acetate 2 in high enantiomeric excess. Several lipases were used for
Direct Synthesis of 3-Acylindoles through Rhodium(III)-Catalyzed Annulation of N-Phenylamidines with α-Cl Ketones
Zhou, Jianhui,Li, Jian,Li, Yazhou,Wu, Chenglin,He, Guoxue,Yang, Qiaolan,Zhou, Yu,Liu, Hong
supporting information, p. 7645 - 7649 (2018/12/11)
In the present study, a novel synthetic strategy to directly produce versatile 3-acylindoles through Rh(III)-catalyzed C-H activation and annulation cascade of N-phenylamidines with α-Cl ketones was developed, in which α-Cl ketones serve as unusual one-carbon (sp3) synthons. This strategy features high regioselectivity, efficiency, wide substrate tolerance, and mild reaction conditions, which further underscore its synthetic utility in drug molecule synthesis.
Enantioselective synthesis of heteroaromatic epoxyketones under phase-transfer catalysis using D-glucose- and D-mannose-based crown ethers
Rapi, Zsolt,Szabo, Tamas,Keglevich, Gyoergy,Szxoellosy, Aron,Drahos, Laszlo,Bako, Peter
body text, p. 1189 - 1196 (2011/10/19)
Heteroaromatic epoxyketones have been synthesized in an asymmetric Darzens condensation of 2-chloroacetylfuran or 2- and 3-chloroacetylthiophene with aromatic aldehydes and in the enantioselective epoxidation of α,β-enones with an N-methylpyrrole unit, in
Copper(I)-promoted synthesis of chloromethyl ketones from trichloromethyl carbinols
Ram, Ram N.,Manoj
, p. 5633 - 5635 (2008/12/21)
(Chemical Equation Presented) Reaction of several trichloromethyl carbinols with 2 equiv of CuCl/bpy in refluxing DCE for 3 h afforded chloromethyl ketones in excellent yield by 1,2-H shift in the copper-chlorocarbenoid intermediate.
Novel building blocks: 1-Aryl-2-chloro-1-ethoxyethenes - Preparations and transformations
Yoshimatsu, Mitsuhiro,Sakai, Miho,Moriura, Eri
, p. 498 - 507 (2008/02/06)
We described here a simple method for the preparation of 1-aryl-2-chloro-1-ethoxyethenes 2a-u, which are prodrugs for Alzheimer's disease, by the reaction of dichloroacetaldehyde diethyl acetal with various aryl and alkenyllithium compounds in high yields. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
Solvent and in situ catalyst preparation impacts upon Noyori reductions of aryl-chloromethyl ketones: application to syntheses of chiral 2-amino-1-aryl-ethanols
Tanis, Steven P.,Evans, Bruce R.,Nieman, James A.,Parker, Timothy T.,Taylor, Wendy D.,Heasley, Steven E.,Herrinton, Paul M.,Perrault, William R.,Hohler, Richard A.,Dolak, Lester A.,Hester, Matthew R.,Seest, Eric P.
, p. 2154 - 2182 (2007/10/03)
As part of medicinal chemistry efforts we found it necessary to develop general syntheses of highly enantiomerically enriched 1-aryl-2-chloroethanols and 1-aryl-2-methylaminoethanols. A survey of literature methods suggested that a truly general approach had not yet been reported, encouraging us to undertake the development of such a methodology. This study describes the design, development, and reduction to practice of a general synthesis of chiral 1-aryl-2-chloroethanols and the transformation of these entities to highly enantiomerically enriched 1-aryl-2-methylaminoethanols. Of particular importance were observations of the impact of solvent and the method of catalyst preparation on the yield and enantiomerical excess of chlorohydrins prepared via Noyori transfer hydrogenations of aryl-chloromethyl ketones.
PROCESS TO PRODUCE ENANTIOMERICALLY ENRICHED 1-ARYL- AND 1-HETEROARYL-2-AMINOETHANOLS
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Page 17, (2008/06/13)
The invention relates to a method of preparing enantiomerically enriched amino alcohols of Formula (I) wherein the variable R1, R2, and R3 are defined herein.
Pyridoquinoxaline antivirals
-
, (2008/06/13)
The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein R1, R2 and R3 are as defined in the specification. The compounds are useful for the treatment of viral infections.
Potent and subtype-selective CCK-B/gastrin receptor antagonists: 2,4-dioxo-1,5-benzodiazepines with a plane of symmetry
Hagishita, Sanji,Seno, Kaoru,Kamata, Susumu,Haga, Nobuhiro,Ishihara, Yasunobu,Ishikawa, Michio,Shimamura, Mayumi
, p. 1433 - 1446 (2007/10/03)
A series of CCK-B/gastrin receptor antagonists, 2,4-dioxo-1,5-benzodiazepine derivatives with a plane of symmetry, were designed, synthesized, and evaluated for antagonistic activity. Structure-activity relationship studies revealed that carbonylmethyl groups at both N-1 and N-5 positions and hydrophilic groups, such as the carboxyl group on the benzene ring attached to the ureido group at the C-3 position, brought about potent affinity and subtype selectivity for CCK-B/gastrin receptors. Several compounds showed excellent in vivo inhibition of gastric acid secretion induced by pentagastrin in anesthetized rats.
