14944-23-1Relevant articles and documents
Lewis Acid Promoted Dearomatization of Naphthols
Boldrini, Cosimo,Casti?eira Reis, Marta,Harutyunyan, Syuzanna R.,Kulish, Kirill,Pérez, Juana M.
, p. 15843 - 15846 (2020)
Two-step dearomative functionalization of naphthols promoted by Lewis acids and copper(I) catalysis was developed. Initially, Lewis acid complexation inverted the electronic properties of the ring and established an equilibrium with the dearomatized counterpart. Subsequent trapping of the dearomatized intermediate with organometallics as well as organophosphines was demonstrated and provided the corresponding dearomatized products.
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)
Taylor, Alexander M.,C?té, Alexandre,Hewitt, Michael C.,Pastor, Richard,Leblanc, Yves,Nasveschuk, Christopher G.,Romero, F. Anthony,Crawford, Terry D.,Cantone, Nico,Jayaram, Hariharan,Setser, Jeremy,Murray, Jeremy,Beresini, Maureen H.,De Leon Boenig, Gladys,Chen, Zhongguo,Conery, Andrew R.,Cummings, Richard T.,Dakin, Leslie A.,Flynn, E. Megan,Huang, Oscar W.,Kaufman, Susan,Keller, Patricia J.,Kiefer, James R.,Lai, Tommy,Li, Yingjie,Liao, Jiangpeng,Liu, Wenfeng,Lu, Henry,Pardo, Eneida,Tsui, Vickie,Wang, Jian,Wang, Yongyun,Xu, Zhaowu,Yan, Fen,Yu, Dong,Zawadzke, Laura,Zhu, Xiaoqin,Zhu, Xiaoyu,Sims, Robert J.,Cochran, Andrea G.,Bellon, Steve,Audia, James E.,Magnuson, Steven,Albrecht, Brian K.
, p. 531 - 536 (2016)
CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology. As part of our effort to explore the potential therapeutic implications of selectively targeting bromodomains, we set out to identify a CBP/EP300 bromodomain inhibitor that was potent both in vitro and in cellular target engagement assays and was selective over the other members of the bromodomain family. Reported here is a series of cell-potent and selective probes of the CBP/EP300 bromodomains, derived from the fragment screening hit 4-methyl-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one.
THERAPEUTIC COMPOUNDS AND USES THEREOF
-
Page/Page column 232, (2016/05/02)
The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
4H-THIENO[3,2-C]CHROMENE-BASED INHIBITORS OF NOTUM PECTINACETYLESTERASE AND METHODS OF THEIR USE
-
Page/Page column 16, (2012/12/13)
Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.
NAPHT- 2 -YLACETIC ACID DERIVATIVES TO TREAT AIDS
-
Page/Page column 328, (2012/01/15)
The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).
Cooperative catalysis approach to intramolecular hydroacylation
Beletskiy, Evgeny V.,Sudheer,Douglas, Christopher J.
experimental part, p. 5884 - 5893 (2012/09/21)
Prior examples of hydroacylation to form six- and seven-membered ring ketones require either embedded chelating groups or other substrate design strategies to circumvent competitive aldehyde decarbonylation. A cooperative catalysis strategy enabled intram
Design, synthesis, structure, and dehydrogenation reactivity of a water soluble o-iodoxybenzoic acid derivative bearing a trimethylammonium group
Cui, Li-Qian,Dong, Zhi-Lei,Liu, Kai,Zhang, Chi
supporting information; experimental part, p. 6488 - 6491 (2012/02/02)
5-Trimethylammonio-1, 3-dioxo-1, 3-dihydro-1λ5-benzo[d][1, 2]iodoxol-1-ol anion (AIBX 1a), an o-iodoxybenzoic acid (IBX) derivative having the trimethylammonium moiety on its phenyl ring, possesses very good solubility in water and distinct oxidative properties from IBX, which is demonstrated in the oxidation of various β-keto esters to the corresponding dehydrogenated products using water as cosolvent. The regeneration of AIBX 1a can be easily realized from the reaction mixture due to its good water solubility.2011 American Chemical Society.
Regiospecific synthesis of carboxylated and simple α-tetralones with homophthalates and various acrylates by a simple condensation method
Roy,Rahman,Islam
, p. 594 - 596 (2007/10/03)
Various carboxylated enols (3) have been prepared by taking advantage of simple condensation reactions of various homophthalates (1) with different acrylates (2), and these enols under heating with two different solvents (DMF and DMSO), afforded ten specific α-tetralones in good to moderate yields using NaCl as a catalyst.
SCHWEFELVERBINDUNGEN DES ERDOELS XV. METHYL-5,6,7,8-TETRAHYDRODINAPHTHOTHIOPHENE UND METHYLDINAPHTHOTHIOPHENE
Boberg, Friedrich,Jachiewicz, Adam,Garming, Alfons
, p. 1 - 12 (2007/10/02)
A one pot synthesis gives methyl-5,6,7,8-tetrahydrodinaphthothiophenes (7) from methyl-1,2,3,4-tetrahydronaphthalen-1-ones (1) by bromination and sulfurization.Tetrahydro compounds 7 have been dehydrogenated to corresponding dinaphthothiophenes 8.Proofs for the constitutions are nmr data of 7, 8 and the independent synthesis of one compound 8.A reaction mechanism with 1,4-dithiine intermediates is discussed. Key words: Alkyl-1,2,3,4-tetrahydronaphthalen-1-ones; alkyl-5,6,7,8-tetrahydrodinaphthothiophenes; alkyldinaphthothiophenes; dehydrogenation with o-chlorobenzoquinone.
Directed ortho metalation reactions. Convergent synthesis of "angular" anthracyclinones ochromycinone and X-14881 C
Katsuura, K.,Snieckus, V.
, p. 124 - 130 (2007/10/02)
Convergent syntheses of the benzanthraquinone natural products X-14881 C (2c) and ochromycinone (2d) have been achieved using aromatic directed metalation strategies.Key steps involve (a) the condensations of dilithiated cis-tetralol (13a) with the ald