- COMPOUNDS AS GLP-1R AGONISTS
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The present application provides compounds that may be used as a glucagon-like peptide-1 receptors (GLP-1R) agonist, or stereoisomers, tautomers, or pharmaceutically acceptable salts of any of the foregoing. Also provided are pharmaceutical compositions containing such compounds, or stereoisomers, tautomers, or pharmaceutically acceptable salts of any of the foregoing. Methods of prepare these compounds and compositions and method of using them to treat or present a disease or a condition mediated by GLP-1R.
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Paragraph 0747
(2022/03/07)
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- Alkenylation and Arylation of Peptides via Ni-Catalyzed Reductive Coupling of α- C-Tosyl Peptides with Csp2Triflates/Halides
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A Ni-catalyzed reductive cross-coupling between α-C-tosyl peptides and Csp2 triflates/halides has been developed. This protocol enables the formation of various unnatural di- and tripeptides containing vinyl and aryl side chains, and it expands the applications of Ni-catalyzed reductive cross-coupling in late-stage diversification of peptides.
- Chen, Yunrong,Gong, Hegui,Ma, Guobin,Qian, Qun,Song, Yanhong,Sun, Deli,Tao, Xianghua
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supporting information
p. 7418 - 7422
(2021/10/12)
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- Iron-Catalyzed Tertiary Alkylation of Terminal Alkynes with 1,3-Diesters via a Functionalized Alkyl Radical
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Direct oxidative C(sp)?H/C(sp3)?H cross-coupling offers an ideal and environmentally benign protocol for C(sp)?C(sp3) bond formations. As such, reactivity and site-selectivity with respect to C(sp3)?H bond cleavage have remained a persistent challenge. Herein is reported a simple method for iron-catalyzed/silver-mediated tertiary alkylation of terminal alkynes with readily available and versatile 1,3-dicarbonyl compounds. The reaction is suitable for an array of substrates and proceeds in a highly selective manner even employing alkanes containing other tertiary, benzylic, and C(sp3)?H bonds alpha to heteroatoms. Elaboration of the products enables the synthesis of a series of versatile building blocks. Control experiments implicate the in situ generation of a tertiary carbon-centered radical species.
- Tian, Ming-Qing,Shen, Zhen-Yao,Zhao, Xuefei,Walsh, Patrick J.,Hu, Xu-Hong
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supporting information
p. 9706 - 9711
(2021/03/19)
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- GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
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Paragraph 00971; 00972
(2021/01/22)
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- A Stepwise Annulation for the Transformation of Cyclic Ketones to Fused 6 and 7-Membered Cyclic Enimines and Enones
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The efficient construction of functionalized polycyclic structures is an important objective in organic synthesis. Herein, we disclose a three-step “[2 + n]” annulation method for the transformation of cyclic ketones to fused enimines and enones. The method relies on the Suzuki coupling reaction and the amide reductive alkenylation reaction. A series of fused bicyclic (6/6, 6/7, 8/7) and tricyclic (6/6/6; 6/6/7, 6/5/7) ring systems bearing an α,β-enimine or an α,β-enone functionality have been synthetized in good overall yields.
- Wu, Dong-Ping,He, Qian,Chen, Dong-Huang,Ye, Jian-Liang,Huang, Pei-Qiang
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supporting information
p. 315 - 322
(2019/02/16)
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- Cyclic Alkenylsulfonyl Fluorides: Palladium-Catalyzed Synthesis and Functionalization of Compact Multifunctional Reagents
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A series of low-molecular-weight, compact, and multifunctional cyclic alkenylsulfonyl fluorides were efficiently prepared from the corresponding alkenyl triflates. Palladium-catalyzed sulfur dioxide insertion using the surrogate reagent DABSO effects sulfinate formation, before trapping with an F electrophile delivers the sulfonyl fluorides. A broad range of functional groups are tolerated, and a correspondingly large collection of derivatization reactions are possible on the products, including substitution at sulfur, conjugate addition, and N-functionalization. Together, these attributes suggest that this method could find new applications in chemical biology.
- Lou, Terry Shing-Bong,Bagley, Scott W.,Willis, Michael C.
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supporting information
p. 18859 - 18863
(2019/11/19)
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- GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme glycolate oxidase (GO). Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
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Paragraph 001013; 001014; 001015
(2019/07/17)
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- One-Pot Relay Gold(I) and Br?nsted Acid Catalysis: Cyclopenta[b]annulation of Indoles via Hydroamination/Nazarov-Type Cyclization Cascade of Enynols
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An expedient relay gold(I) and Br?nsted acid catalyzed hydroamination/Nazarov cyclization of 1-(2-aminophenyl)pent-4-en-2-ynols for the synthesis of various polyfunctionalized cyclopenta[b]indoles is described. The synthetic utility of this method has bee
- Dhiman, Seema,Ramasastry
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supporting information
p. 5116 - 5119
(2015/11/03)
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- Achieving vinylic selectivity in Mizoroki-heck reaction of cyclic olefins
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In Heck reactions of cyclic olefins, the products usually have aryl groups that end up at the allylic and/or homoallylic position. We herein report new selectivity that adds aryl groups to the vinylic position. Cyclic olefins of various ring size worked well. The desired isomers were produced by palladium-hydride-catalyzed isomerization of the initial products. Thus, a specific catalyst must be used so that it can perform two jobs under one set of reaction conditions. Copyright
- Wu, Xiaojin,Lu, Yunpeng,Hirao, Hajime,Zhou, Jianrong
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supporting information
p. 6014 - 6020
(2013/06/26)
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- INHIBITORS OF VIRAL REPLICATION, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES
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The present invention relates to compounds of formula (1) as claimed in claim 1, their use in the treatment or the prevention of viral disorders, including HIV. (Formula I)
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Page/Page column 144
(2012/10/18)
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- Trichlorophenyl formate: Highly reactive and easily accessible crystalline CO surrogate for palladium-catalyzed carbonylation of aryl/alkenyl halides and triflates
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The high utility of 2,4,6-trichlorophenyl formate, a highly reactive and easily accessible crystalline CO surrogate, is demonstrated. The decarbonylation with NEt3 to generate CO proceeded rapidly at rt, thereby allowing external-CO-free Pd-catalyzed carbonylation of aryl/alkenyl halides and triflates. The high reactivity of the CO surrogate enabled carbonylation at rt and significantly reduced the quantities of formate to near-stoichiometric levels. The obtained trichlorophenyl esters can be readily converted to a variety of carboxylic acid derivatives in high yields.
- Ueda, Tsuyoshi,Konishi, Hideyuki,Manabe, Kei
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supporting information
p. 5370 - 5373,4
(2012/12/12)
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- The palladium-catalyzed trifluoromethylation of vinyl sulfonates
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A method for the palladium-catalyzed trifluoromethylation of cyclohexenyl sulfonates has been developed. Various cyclohexenyl triflates and nonaflates underwent trifluoromethylation under mild reaction conditions using a catalyst system composed of Pd(dba
- Cho, Eun Jin,Buchwald, Stephen L.
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supporting information; experimental part
p. 6552 - 6555
(2012/01/15)
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- Caesium fluoride-promoted Stille coupling reaction: An efficient synthesis of 9Z-retinoic acid and its analogues using a practical building block
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A highly efficient and rapid total synthesis of 9Z-retinoic acid was accomplished by caesium fluoride-promoted Stille coupling reaction; using a common building block, 9Z-retinoic acid analogues were also prepared by the same method without isomerisation of the Z-double bond. The Royal Society of Chemistry 2008.
- Okitsu, Takashi,Iwatsuka, Kinya,Wada, Akimori
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supporting information; experimental part
p. 6330 - 6332
(2009/04/13)
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- The reaction of tetralones with nitriles: A simple approach to the synthesis of new substituted benzo[h]quinazolines, benzo[f]quinazolines and dibenzo[a,i]phenanthridines
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The one-pot reaction of 1-tetralone with nitriles in the presence of triflic anhydride affords in good yields 2,4-disubstituted 5,6-dihydrobenzo[h] quinazolines, which oxidation with DDQ leads to the corresponding benzo[h]quinazolines. 2-Tetralone undergo
- Herrera, Antonio,Martínez-Alvarez, Roberto,Chioua, Mourad,Chatt, Rachid,Chioua, Rachid,Sánchez, Angel,Almy, John
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p. 2799 - 2811
(2007/10/03)
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- Selective iron-catalyzed cross-coupling reactions of Grignard reagents with enol triflates, acid chlorides, and dichloroarenes
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Cheap, readily available, air stable, nontoxic, and environmentally benign iron salts such as Fe(acac)3 are excellent precatalysts for the cross-coupling of Grignard reagents with alkenyl triflates and acid chlorides. Moreover, it is shown that dichloroarene and -heteroarene derivatives as the substrates can be selectively monoalkylated by this method. All cross-coupling reactions proceed very rapidly under notably mild conditions and turned out to be compatible with a variety of functional groups in both reaction partners. A detailed analysis of the preparative results suggests that iron-catalyzed C-C bond formations can occur via different pathways. Thus, it is likely that reactions of methylmagnesium halides involve iron-ate complexes as the active components, whereas reactions of Grignard reagents with two or more carbon atoms are effected by highly reduced iron-clusters of the formal composition [Fe(MgX)2]n generated in situ. Control experiments using the ate-complex [Me4Fe]Li2 corroborate this interpretation.
- Scheiper, Bodo,Bonnekessel, Melanie,Krause, Helga,Fuerstner, Alois
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p. 3943 - 3949
(2007/10/03)
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- New electrochemical carboxylation of vinyl triflates. Synthesis of β-keto carboxylic acids
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Electrochemical reduction of alicyclic vinyl triflates (1a-1e) in a DMF solution containing 0.1 M Bu4NBF4 under an atmospheric pressure of carbon dioxide with a platinum cathode and a magnesium anode resulted in the cleavage of an ox
- Kamekawa, Hisato,Senboku, Hisanori,Tokuda, Masao
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p. 1591 - 1594
(2007/10/03)
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