72181-95-4Relevant academic research and scientific papers
Catalytic Asymmetric Homologation of Ketones with α-Alkyl α-Diazo Esters
Tan, Fei,Pu, Maoping,He, Jun,Li, Jinzhao,Yang, Jian,Dong, Shunxi,Liu, Xiaohua,Wu, Yun-Dong,Feng, Xiaoming
, p. 2394 - 2402 (2021/02/16)
The homologation of ketones with diazo compounds is a useful strategy to synthesize one-carbon chain-extended acyclic ketones or ring-expanded cyclic ketones. However, the asymmetric homologation of acyclic ketones with α-diazo esters remains a challenge due to the lower reactivity and complicated selectivity. Herein, we report the enantioselective catalytic homologation of acetophenone and related derivatives with α-alkyl α-diazo esters utilizing a chiral scandium(III) N,N′-dioxide as the Lewis acid catalyst. This reaction supplies a highly chemo-, regio-, and enantioselective pathway for the synthesis of optically active β-keto esters with an all-carbon quaternary center through highly selective alkyl-group migration of the ketones. Moreover, the ring expansion of cyclic ketones was accomplished under slightly modified conditions, affording a series of enantioenriched cyclic β-keto esters. Density functional theory calculations have been carried out to elucidate the reaction pathway and possible working models that can explain the observed regio- and enantioselectivity.
Radical-Polar Crossover Annulation: A Platform for Accessing Polycyclic Cyclopropanes
Milligan, John A.,Burns, Kevin L.,Le, Anthony V.,Polites, Viktor C.,Wang, Zheng-Jun,Molander, Gary A.,Kelly, Christopher B.
, p. 242 - 247 (2019/12/11)
Photoredox-mediated radical/polar crossover (RPC) processes provide unique solutions to challenging annulations. Herein, we describe an approach to the cyclopropanation of olefins that are embedded within bicyclic scaffolds. Whereas these systems are noto
As opioid receptor antagonists or inverse agonists of the novel compounds
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Paragraph 0323; 0324, (2016/10/08)
Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
A new mild method for the C-acylation of ketone enolates. a convenient synthesis of β-keto-esters,-thionoesters, and-thioesters
Hale, Karl J.,Grabski, Milosz,Flasz, Jakub T.
supporting information, p. 370 - 373 (2013/03/13)
A new method for ketone enolate C-acylation is described which utilizes alkyl pentafluorophenylcarbonates, thiocarbonates, and thionocarbonates as the reactive acylating agents, and MgBr2·Et2O, DMAP, and i-Pr2NEt as the reagents for enolization. A wide range of ketones have been observed to undergo clean C-acylation via this protocol.
NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS
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, (2011/06/19)
Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
N- INDEN- 2 -YL- ISOPROPYLSULFONAMIDES AS AMPA RECEPTOR POTENTIATORS
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Page/Page column 24, (2010/07/10)
A compound of formula (I) and salts thereof are provided: Wherein n and R1 are defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or
METHOD OF TREATMENT USING NOVEL ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS
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, (2010/05/13)
A method of treatment using pharmaceutical compositions containing novel antagonists or inverse agonists at opioid receptors for the treatment of binge eating disorder, anorexia nervosa, bulimia nervosa, excess drug or alcohol use, or eating disorder not otherwise specified.
NOVEL HETEROCYCLE COMPOUNDS
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Page/Page column 44-45, (2009/04/24)
The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.
Synthesis of benzocyclic ketones via palladium-catalyzed cyclization of ω-(2-iodoaryl)alkanenitriles
Pletnev, Alexandre A.,Larock, Richard C.
, p. 2133 - 2136 (2007/10/03)
An efficient procedure for the synthesis of 2,2-disubstituted benzocyclic ketones by intramolecular carbopalladation of nitriles has been developed. The cyclization of substituted 3-(2-iodoaryl)propanenitriles affords indanones in high yields. The reactio
Carbopalladation of nitriles: Synthesis of benzocyclic ketones and cyclopentenones via Pd-catalyzed cyclization of ω-(2-iodoaryl)alkanenitriles and related compounds
Pletnev, Alexandre A.,Larock, Richard C.
, p. 9428 - 9438 (2007/10/03)
An efficient procedure for the synthesis of 2,2-disubstituted benzocyclic ketones by intramolecular carbopalladation of nitriles has been developed. The cyclization of substituted 3-(2-iodoaryl)-propanenitriles affords indanones in high yields. The reaction is compatible with a wide variety of functional groups. This methodology has been extended to the synthesis of tetralones and cyclopentenones.
