- An oxidative approach to a hydroxypiperidinone utilizing a Rh-catalyzed C-H activation process
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C-H activation and isomerization using a Rh-catalyst provided quick access to dehydropiperidine derivatives that could be further oxidized to hydroxypiperidinone derivatives.
- Ayers, Timothy A.
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Read Online
- Total Synthesis of the Potent HIF-1 Inhibitory Antitumor Natural Product, (8R)-Mycothiazole, via Baldwin-Lee CsF/CuI sp3-sp2-Stille Cross-Coupling. Confirmation of the Crews Reassignment
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A convenient asymmetric total synthesis of the potent HIF-1 inhibitory antitumor natural product, (-)- or (+)-(8R)-mycothiazole (1), is described. Not only does our synthesis confirm the 2006 structural reassignment made by Crews (Crews, P., et al. J. Nat
- Wang, Liping,Hale, Karl J.
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Read Online
- Caesium fluoride-mediated hydrocarboxylation of alkenes and allenes: Scope and mechanistic insights
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A caesium fluoride-mediated hydrocarboxylation of olefins is disclosed that does not rely on precious transition metal catalysts and ligands. The reaction occurs at atmospheric pressures of CO2 in the presence of 9-BBN as a stoichiometric reductant. Stilbenes, β-substituted styrenes and allenes could be carboxylated in good yields. The developed methodology can be used for preparation of commercial drugs as well as for gram scale hydrocarboxylation. Computational studies indicate that the reaction occurs via formation of an organocaesium intermediate.
- Gevorgyan, Ashot,Obst, Marc F.,Guttormsen, Yngve,Maseras, Feliu,Hopmann, Kathrin H.,Bayer, Annette
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p. 10072 - 10078
(2019/11/14)
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- Preferential Photoreaction in a Porous Crystal, Metal-Macrocycle Framework: PdII-Mediated Olefin Migration over [2+2] Cycloaddition
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A nanosized confined space with well-defined functional surfaces has great potential to control the efficiency and selectivity of catalytic reactions. Herein we report that a 1,6-diene, which normally forms an intramolecular [2+2] cycloadduct under photoirradiation, preferentially undergoes a photoinduced olefin migration in a porous crystal, metal-macrocycle framework (MMF), and alternatively [2+2] cycloaddition is completely inhibited in the confined space. A plausible reaction mechanism for olefin migration triggered by the photoinduced dissociation of the Pd-Cl bond is suggested based on UV-vis diffuse reflectance spectroscopy, single-crystal XRD, and MS-CASPT2 calculation. The substrate scope of the photoinduced olefin migration in MMF was also examined using substituted allylbenzene derivatives.
- Yonezawa, Hirotaka,Tashiro, Shohei,Shiraogawa, Takafumi,Ehara, Masahiro,Shimada, Rintaro,Ozawa, Takeaki,Shionoya, Mitsuhiko
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supporting information
p. 16610 - 16614
(2018/12/11)
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- KINASE INHIBITORS AND USES THEREOF
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The present disclosure relates generally to compounds and compositions, intermediates, processes for their preparation, and their use as kinase inhibitors.
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Paragraph 0256; 0342
(2018/12/13)
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- MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES
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Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
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Paragraph 0269
(2017/08/01)
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- COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
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The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
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Page/Page column 722; 723
(2015/02/02)
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- Carboxylation of organoboronic esters with potassium methyl carbonate under copper catalysis
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In the presence of a copper catalyst, potassium methyl carbonate serves as a versatile carboxylating agent of allyl- and arylboronic esters for the preparation of carboxylic acids. Georg Thieme Verlag Stuttgart New York.
- Duong, Hung A.,Nguyen, Tuan Minh,Rosman, Nurul Zubaidah Binte,Tan, Lionel Jia Liang
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p. 1881 - 1885
(2014/07/22)
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- MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES
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Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
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Page/Page column 90
(2014/01/08)
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- Regioselective copper-catalyzed carboxylation of allylboronates with carbon dioxide
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In the presence of a Cu(I)/NHC catalyst, the reactions of allylboronic pinacol esters with CO2 (1 atm) are highly regioselective, giving exclusively the more substituted β,γ-unsaturated carboxylic acids in most cases. A diverse array of substituted carboxylic acids can be prepared via this method, including compounds featuring all-carbon quaternary centers.
- Duong, Hung A.,Huleatt, Paul B.,Tan, Qian-Wen,Shuying, Eileen Lau
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supporting information
p. 4034 - 4037
(2013/09/02)
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- ANALOGS OF DEHYDROPHENYLAHISTINS
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Analogs of dehydrophenylahistins are disclosed as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
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Page/Page column 32
(2011/08/03)
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- Studies toward the synthesis of maoecrystal v
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An approach toward the synthesis of maoecrystal V is described. The synthetic strategy for this approach was designed to address unique challenges posed by the strained tetrahydrofuran ring at the center of the target structure.(Figure Presented)
- Gu, Zhenhua,Zakarian, Armen
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supporting information; experimental part
p. 1080 - 1082
(2011/04/25)
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- Metal-free oxyaminations of alkenes using hydroxamic acids
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A radical-mediated approach to metal-free alkene oxyamination is described. This method capitalizes on the unique reactivity of the amidoxyl radical in alkene additions to furnish a general difunctionalization using simple diisopropyl azodicarboxylate (DIAD) as a radical trap. This protocol capitalizes on the intramolecular nature of the process, providing single regioisomers in all cases. Difunctionalizations of cyclic alkenes provide trans oxyamination products inaccessible using current methods with high levels of stereoselectivity, complementing cis-selective oxyamination processes.
- Schmidt, Valerie A.,Alexanian, Erik J.
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supporting information; experimental part
p. 11402 - 11405
(2011/09/16)
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- NEW CYCLOHEXYLAMINE DERIVATIVES HAVING β2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES
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The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
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Page/Page column 81
(2011/12/02)
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- ANALOGS OF DEHYDROPHENYLAHISTINS AND THEIR THEAPEUTIC USE
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Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
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Page/Page column 22-23
(2008/12/08)
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- Hydrocarboxylation of allenes with CO2 catalyzed by silyl pincer-type palladium complex
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Tridentate PSiP pincer-type palladium complex-catalyzed hydrocarboxylation of allenes under carbon dioxide to give synthetically useful β,γ-unsaturated carboxylic acids was developed. This novel CO2-fixation reaction is thought to proceed through the catalytic generation of σ-allyl palladium species via hydropalladation of allenes, followed by its regioselective nucleophilic addition to CO2 in the presence of an appropriate reducing agent. The reaction is successfully applied to various allenes bearing functional groups such as ester, carbamate, ketone, and alkene, showing high synthetic utility of this protocol. Copyright
- Takaya, Jun,Iwasawa, Nobuharu
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supporting information; experimental part
p. 15254 - 15255
(2009/03/12)
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- Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
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Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1′, R1″, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.
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- New synthesis of 2-alkyl-4,4-dimethyl-5-halomethylisoxazolidin-3-ones via intramolecular halocyclization of N-alkyl-2,2-dimethyl-3-butenohydroxamic acids
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N-Alkyl-2,2-dimethyl-3-butenohydroxamic acids and their cyclic derivatives were halocyclized by iodine monochloride, N-bromosuccinimide, or N-chlorosuccinimide to afford the corresponding 2-alkyl-4,4-dimethyl-5-halomethylisoxazolidinones and 5-membered ring fused isoxazolidinones in excellent yields.
- Kim, Hyoung Rae,Shin, Seung Il,Park, Hyun Ju,Jeon, Dong Ju,Ryu, Eung K.
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p. 789 - 791
(2007/10/03)
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- Alkylation of lithium dienediolates of butenoic acids. Regioselectivity effects of structure and leaving group of the alkylating agent
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Regioselectivity of alkylation of but-2-enoic acids I and 2 by alkyl halides strongly depends on the reactivity of the electrophile. High α selectivity results for saturated alkyl halides, whereas poor α-selectivity is obtained for highly reactive allyl and benzyl halides. For reactive alkylating halides selectivity is partly governed by the ion pairing aggregates of the dienediolates. Lithium bromide and the carboxylate generated in the ongoing reaction cause opposite effects on regioselectivity.
- Aurell, Maria J.,Gil, Salvador,Mestres, Ramon,Parra, Margarita,Parra, Lilian
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p. 4357 - 4366
(2007/10/03)
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- Hydromagnesation of Isoprene by Isopropylmagnesium Chloride in the Presence of Nickel(II) Compounds
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The reaction of isoprene with alkylmagnesium halides in the presence of nickel complexes with phosphine oxides and nitrobgen-containing ligands gives dimeric hydromagnesation products along with monomeric magnesium-containing allyl-type products.
- Viktorov, N. B.,Zubritskii, L. M.
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p. 267 - 270
(2007/10/03)
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- SELECTIVE HYDROMAGNESATION OF ISOPRENE UNDER THE ACTION OF ALKYLMAGNESIUM HALIDES IN THE PRESENCE OF Ni(II) COMPLEXES
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The reaction of isoprene and alkyl Grignard reagent in the presence of phosphine complexes of nickel was shown to result in the selective formation of a telodimer H(C5H8)2MgX, which can be subjected to further transformations.The influence of the nature of Grignard reagent on the reaction yield was observed.
- Viktorov, N. B.,Zubritskii, L. M.,Petrov, A. A.
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p. 1121 - 1124
(2007/10/02)
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- Acetoxy lactonization of alkenyl acetic acids promoted by ammonium persulfate and trifluoromethanesulfonic acid in acetic acid
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The reactions of substituted 4-pentenoic and 3-butenoic acids with ammonium persulfate in acetic acid, in the presence of trifluoromethanesulfonic acid, gave the products of acetoxy lactonization in good yield.
- Tiecco, Marcello,Testaferri, Lorenzo,Tingoli, Marco
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p. 5351 - 5358
(2007/10/02)
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- α-Oxo Sulfones. 4. Correction of a Pretended α-Oxo Sulfone by an Unambiguous Synthesis of the Revised Structure
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By an independent synthesis the oxidation product of 1,1-dichloro-2,2-dimethyl-1-(phenylthio)-3-butene (1) was shown not to be α-oxo sulfone "2" as published earlier but a phenylsulfonyl γ-butyrolactone, 3.This synthesis involves the intramolecular reaction of a sulfenic carboxylic mixed anhydride with an olefinic bond.A rationale for the formation of 3 from 1 is presented.
- Schank, K.,Frisch, A.,Zwanenburg, B.
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p. 4580 - 4582
(2007/10/02)
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