83112-50-9Relevant academic research and scientific papers
Synthesis of α-hydroxyacetophenones
McLaughlin, Mark,Belyk, Kevin M.,Qian, Gang,Reamer, Robert A.,Chen, Cheng-Yi
experimental part, p. 5144 - 5148 (2012/07/03)
A general method for the preparation of α-hydroxyacetophenones is presented. Functionalized arylmagnesium species are transmetalated to the corresponding arylzinc intermediates, which undergo Cu(I)-catalyzed reaction with acetoxyacetyl chloride. Acidic hy
Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator
Nique, Francois,Hebbe, Severine,Triballeau, Nicolas,Peixoto, Christophe,Lefrancois, Jean-Michel,Jary, Helene,Alvey, Luke,Manioc, Murielle,Housseman, Christopher,Klaassen, Hugo,Van Beeck, Kris,Guedin, Denis,Namour, Florence,Minet, Dominque,Van Der Aar, Ellen,Feyen, Jean,Fletcher, Stephen,Blanque, Roland,Robin-Jagerschmidt, Catherine,Deprez, Pierre
supporting information, p. 8236 - 8247,12 (2020/09/15)
Structural modification performed on a 4-methyl-4-(4-hydroxyphenyl) hydantoin series is described which resulted in the development of a new series of 4-(hydroxymethyl)diarylhydantoin analogues as potent, partial agonists of the human androgen receptor. T
NOVEL IMIDAZOLIDINE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS
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Page/Page column 55, (2010/04/06)
Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3a R3b, R4a, R4b, R4c, and ml are as describe
OXIME COMPOUNDS AND THE USE THEREOF
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Page/Page column 359, (2008/06/13)
The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO2, CRsu
Synthesis of 3-substituted benzamides and 5-substituted isoquinolin-1(2H)-ones and preliminary evaluation as inhibitors of poly(ADP-ribose)polymerase (PARP)
Watson, Corrine Y.,Whish, William J. D.,Threadgill, Michael D.
, p. 721 - 734 (2007/10/03)
Inhibitors of poly(ADP-ribose)polymerase (PARP) inhibit repair of damaged DNA and thus potentiate radiotherapy and chemotherapy of cancer. 3-Substituted benzamides and 5-substituted isoquinolin-1-ones have been synthesised and evaluated for inhibition of PARP. Reduction of 3-(bromoacetyl)benzamide, followed by treatment with base, gave RS-3-oxiranylbenzamide. Reduction of 3-(hydroxyacetyl)benzonitrile with bakers' yeast gave the R-diol which was converted to R-3-(1,2-dihydroxyethyl)benzamide. Similar reduction of 3-(acetoxyacetyl)benzonitrile led towards the S-diol which was converted to its cyclic acetonide. E-2-(2,6-Dicyanophenyl)-N,N-dimethylethenamine was formed by condensation of 2,6-dicyanotoluene with dimethylformamide dimethyl acetal (DMFDMA); cyclisation under acidic conditions afforded 5-cyanoisoquinolin-1-one. Heck coupling of 5-iodoisoquinolin-1-one with propenoic acid formed E-3-(1-oxoisoquinolin-5-yl)propenoic acid. 3-Oxiranylbenzamide, 5-bromoisoquinolin-1-one and 5-iodoisoquinolin-1-one were among the most potent inhibitors of PARP activity in a preliminary screen in vitro. Copyright (C) 1998 Elsevier Science Ltd.
