- Intracellular Generation of a Diterpene-Peptide Conjugate that Inhibits 14-3-3-Mediated Interactions
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Synthetic agents that disrupt intracellular protein-protein interactions (PPIs) are highly desirable for elucidating signaling networks and developing new therapeutics. However, designing cell-penetrating large molecules equipped with the many functional
- Parvatkar, Prakash,Kato, Nobuo,Uesugi, Motonari,Sato, Shin-Ichi,Ohkanda, Junko
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Read Online
- A Highly Fluorinated Chiral Aldehyde for Enantioselective Fluorescent Recognition in a Biphasic System
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A 1,1′-bi-2-naphthol (BINOL)-based aldehyde containing four perfluoroalkyl groups has been designed and synthesized. It shows enantioselective fluorescence enhancement at 420 nm when treated with the enantiomers of trans-1,2-diaminocyclohexane in an organ
- Wang, Chao,Wu, Xuedan,Pu, Lin
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Read Online
- Palladium-Catalyzed Tandem Carbonylative Diels-Alder Reaction for Construction of Bridged Polycyclic Skeletons
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A palladium-catalyzed tandem carbonylative lactonization and Diels-Alder cycloaddition reaction between aldehyde-tethered benzylhalides and alkenes has been developed. A range of alkenes and aldehyde-tethered benzylhalides bearing different substituents can be successfully transformed into the corresponding bridged polycyclic compounds in good yields. This strategy provides a unique approach to complex lactone-containing bridged polycyclic compounds.
- Wang, Siyuan,Zhou, Yangkun,Huang, Hanmin
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supporting information
p. 2125 - 2129
(2021/04/05)
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- Compound with PPAR delta agonistic activity, pharmaceutical composition and medical application
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The invention discloses a compound with PPAR delta agonistic activity, a pharmaceutical composition and medical application, wherein the structure of the compound is shown as a formula I in the specification. The compound shown in the formula I is a novel
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Paragraph 0061-0065
(2021/03/13)
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- An Intramolecular Cycloaddition Approach to the Kauranoid Family of Diterpene Metabolites
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Synthetic studies toward the ent-kauranoid family of diterpene natural products are reported. An intramolecular (4 + 3) cycloaddition allows the direct elaboration of diverse natural product frameworks, encompassing a challenging bicyclo[3.2.1]octane core. The established routes comprise only a few synthetic operations (3-5 steps), transforming a range of simple starting materials into the tetracyclic scaffolds that are commonly found in many ent-kaurene metabolites.
- Callebaut, Brenda,Hullaert, Jan,Van Hecke, Kristof,Winne, Johan M.
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supporting information
p. 310 - 314
(2019/01/10)
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- Fe(III)-Catalyzed Aerobic Intramolecular N-N Coupling of Aliphatic Azides with Amines
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An Fe(III)-catalyzed intramolecular N-N coupling of aliphatic azidoamines that forms diverse five- and six-membered semisaturated diazoheterocycles using air as an oxidant is reported, providing an alternative to hydrazine-based methods. Mechanistic studies suggest that a N-radical induced intramolecular homolytic substitution (SH2) is involved in ring closure. The power of this N-N bond-forming method is also demonstrated by using it as the final step in a total synthesis of (-)-newbouldine.
- Zhang, Yue,Duan, Dongyu,Zhong, Ying,Guo, Xin-Ai,Guo, Jiawei,Gou, Jing,Gao, Ziwei,Yu, Binxun
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supporting information
p. 4960 - 4965
(2019/09/03)
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- Synthesis of various cyclopropyl methyl bromide and its derivatives from ketones and/or aldehydes and some β-dicarbonyl compounds in the presence of BrCN and Et3N
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The ultimate goal in this paper has been developed for the synthesis of structurally various bromomethyl cyclopropane via an α-bromoketone and/or aldehydes with ethyl cyanoacetate or malononitrile and cyanogen bromide (BrCN) in the presence of Et3N to give products in excellent yields within about 3?s. All structures were characterized by IR, 1H-NMR, 13C-NMR, and Mass spectroscopy techniques. The reaction mechanism was discussed.
- Gholizadeh, Saeed,Safa, Kazem D.,Noroozi Pesyan, Nader
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p. 1239 - 1253
(2019/04/27)
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- Highly selective construction of medium-sized lactams by palladium-catalyzed intramolecular hydroaminocarbonylation of aminoalkynes
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A novel palladium-catalyzed intramolecular hydroaminocarbonylation of aminoalkynes has been developed. This direct and operationally simple protocol provides a rapid and reliable approach to a diverse array of valuable seven-and eight-membered lactams with high chemoselectivity and regioselectivity. The high selectivity might be attributed to rational tuning the electronic nature of the amine moiety and the palladium catalyst which enabled this transformation to proceed in the absence of acidic or any other additives under fairly mild reaction conditions. This method paves the way for the synthesis of medium-sized lactams.
- Hu, Yue,Huang, Hanmin
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supporting information
p. 5070 - 5073
(2017/11/07)
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- Annulation of o-Quinodimethanes through N-Heterocyclic Carbene Catalysis for the Synthesis of 1-Isochromanones
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The activation of 2-(bromomethyl)benzaldehydes using N-heterocyclic carbenes represents a novel approach to the generation of o-quinodimethane (o-QDM) intermediates. Coupling with ketones such as phenylglyoxylates, isatins, or trifluoromethyl ketones via [4 + 2] annulation gives access to functionalized 1-isochromanones.
- Janssen-Müller, Daniel,Singha, Santanu,Olyschl?ger, Theresa,Daniliuc, Constantin G.,Glorius, Frank
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supporting information
p. 4444 - 4447
(2016/09/09)
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- 1:1 adducts of sickle hemoglobin
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Provide herein are 1:1 adducts of sickle hemoglobin (HbS) and a compound of formula (I), as defined herein, suitable as modulators of HbS, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
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Page/Page column 44; 45
(2016/02/29)
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- One-pot synthesis of 1H-isochromenes and 1,2-dihydroisoquinolines by a sequential isocyanide-based multicomponent/Wittig reaction
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A one-pot synthesis of 1H-isochromenes and 1,2-dihydroisoquinolines by a I-MCR/Wittig sequence was developed. The reaction of phosphonium salt 5, an acid, an amine (or without), and an isocyanide gave the 1H-isochromenes 7 or 1,2-dihydroisoquinolines 9 in
- Wang, Long,Guan, Zhi-Rong,Ding, Ming-Wu
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p. 2413 - 2420
(2016/03/01)
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- 1:1 ADDUCTS OF SICKLE HEMOGLOBIN
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Provide herein are 1:1 adducts of sickle hemoglobin (HbS) and a compound of formula (I), as defined herein, suitable as modulators of HbS, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
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Paragraph 0239; 0240
(2015/08/04)
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- 1:1 ADDUCTS OF SICKLE HEMOGLOBIN
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Provide herein are 1:1 adducts of sickle hemoglobin (HbS) and a compound of formula (I), as defined herein, suitable as modulators of HbS, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
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Paragraph 0128; 0129
(2015/09/23)
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- NOVEL COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.
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Paragraph 1946; 1947
(2015/10/05)
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- Asymmetric synthesis of carbocycles: Use of intramolecular conjugate displacement
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Intramolecular conjugate displacement (ICD), the process illustrated in eqn (1), has been applied to the Morita-Baylis-Hillman adducts formed from (5S)-5-(l-menthyloxy)-2(5H)-furanone and aldehydes that are substituted in the γ- or δ-position by geminal phenylthio groups. When the initial Morita-Baylis-Hillman alcohols are acetylated and oxidized to geminal sulfones, deprotonation causes ring closure by ICD (2.5→2.6). Hydrogenation, DIBAL-H reduction and desulfonylation releases an optically pure carbocycle. The Royal Society of Chemistry 2013.
- Sreedharan, Dinesh T.,Clive, Derrick L. J.
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p. 3128 - 3144
(2013/06/04)
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- Synthesis of 2-aryl-1,2-dihydrophthalazines via reaction of 2-(bromomethyl)benzaldehydes with arylhydrazines
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The reaction of 2-(bromomethyl)benzaldehydes with arylhydrazines employing K2CO3 as a base and FeCl3 as a catalyst in CH3CN at 100 C delivers 2-aryl-1,2-dihydrophthalazines with yields ranging from 60 to 91%. The transformation is considered to proceed as an intermolecular condensation/intramolecular nucleophilic substitution.
- Aljaar, Nayyef,Conrad, Jürgen,Beifuss, Uwe
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p. 1045 - 1053
(2013/03/29)
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- Asymmetric Synthesis of Functionalized Tetrahydronaphthalenes via an Organocatalytic Nitroalkane-Michael/Henry Domino Reaction
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An organocatalytic nitroalkane-Michael/Henry reaction sequence to functionalized 1,2,3,4-tetrahydronaphthalen-1-ols is described. Starting from 2-(nitromethyl)benzaldehyde and nitroalkenes a bifunctional quinine-based squaramide organocatalyst is used to afford the title compounds in moderate to very good yields (25-84%), high diastereomeric ratios (dr>95:5) after crystallization and good to excellent enantioselectivities of 63-99% ee. Starting from γ-nitro aldehydes and ketones secondary and tertiary cyclohexanols bearing four stereogenic centers can also be prepared with this Michael/Henry domino reaction. Copyright
- Enders, Dieter,Hahn, Robert,Atodiresei, Iuliana
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p. 1126 - 1136
(2013/05/21)
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- New CRTH2 Antagonists
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The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
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Page/Page column 43
(2012/12/13)
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- New heterocyclic inputs for the povarov multicomponent reaction
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Oxa-, thia- and imidazolones are reactive inputs as electron-rich olefin components in Povarov reactions. On interaction with anilines and aldehydes, these substrates afford the corresponding multicomponent adducts in a regioselective manner. Intramolecular processes are also explored. Post-condensation oxidation provides convenient access to a variety of fused quinoline derivatives. Georg Thieme Verlag Stuttgart ? New York.
- Vicente-Garcia, Esther,Ramon, Rosario,Lavilla, Rodolfo
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supporting information; scheme or table
p. 2237 - 2246
(2011/09/15)
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- 9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites
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Synthesis, radioligand binding and molecular modeling studies of several 9-aminomethyl-9,10-dihydroanthracene (AMDA) analogs were carried out to determine the extent of the steric tolerance associated with expansion of the tricyclic ring system and amine
- Shah, Jitesh R.,Mosier, Philip D.,Peddi, Srinivas,Roth, Bryan L.,Westkaemper, Richard B.
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supporting information; experimental part
p. 935 - 938
(2010/06/20)
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- INHIBITORS OF CYTOSOLIC PHOSPHOLIPASE A2
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This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLAα). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.
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Page/Page column 45
(2008/06/13)
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- Processes for the preparation of aryl-and heteroaryl-alkylsulfonyl halides
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The present invention provides processes for the preparation of arylalkylsulfonyl halides and heteroarylalkylsufonyl halides of Formula I: Ar—R—SO2—X, that are useful as intermediates in the preparation of pharmaceuticals.
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Page/Page column 11
(2008/06/13)
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- Synthesis of PDK, a Novel Porphyrin-Linked Dicarboxylate Ligand
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A novel trinucleating ligand system H4(PDK), for porphyrin-based diamine bis(Kemp's triacid)-imide, was constructed by using two molecules of Kemp's triacid and one molecule of porphyrin as building blocks. The dimeso-substituted octaalkylporphyrin unit, carrying bromomethyl groups at the ortho positions of two trans-positioned meso-phenyl groups, was synthesized from (3,3′-diethyl-4,4′-dimethyl-2,2′-dipyrrolyl)methane and α-bromo-o-tolualdehyde. The structures of both of the two atropisomers (α,α- and α,β-) of bromoporphyrin, H2(α,α-BP) and H2(α,β-BP), were determined by X-ray crystallography, with the α,β-isomer as the free base form and the α,α-isomer as the zinc complex. Both the α,α- and α,β-isomers of the bromomethyl porphyrins were converted to their aminomethyl derivatives, H2(α,α-AP) and H2(α,β-AP), through the corresponding imidoporphyrin intermediates, H2(α,α-IP) and H2(α,β-IP), by the Gabriel synthesis. The α,α- and α,β- aminoporphyrins were coupled with Kemp's triacid anhydride-chloride to form H4(α,α-PDK) and H4(α,β-PDK), respectively. Unlike the α,β-isomer, the structure of which was determined by X-ray crystallography for the zinc complex, H4(α,α-PDK) has a remarkable and complicated solvent-dependent 1H NMR spectrum that suggests the existence of hydrogen bonding interactions between two convergent, tethered Kemp's triacid units, as predicted in a modeling study. The convergent feature is essential for the target ligand H4(α,α-PDK) to form trinuclear metal complexes with a bis(carboxylato) dimetallic unit sitting above a metalloporphyrin ring.
- Zhang, Xiao-Xiang,Lippard, Stephen J.
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p. 5298 - 5305
(2007/10/03)
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