16217-22-4Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors
Yu, Jianjun,Xu, Lei,Hong, Duidui,Zhang, Xiaotuan,Liu, Jieyu,Li, Daqiang,Li, Jia,Zhou, Yubo,Liu, Tao
, p. 543 - 558 (2019)
A series of novel phenol ether derivatives were designed, synthesized, and evaluated as non-covalent proteasome inhibitors. Most compounds exhibited moderate to excellent proteasome inhibitory activity. In particular, compound 18x proved to be the most po
HALOALLYLAMINE COMPOUNDS AND APPLICATION THEREOF
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Paragraph 0363-0365, (2021/10/15)
The present invention relates to the technical field of pharmaceuticals. Specifically, the present invention relates to a halo-allylamine compound, or a pharmaceutically acceptable salt, an ester, a stereoisomer or a tautomer thereof, and a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, and use in preventing and/or treating a disease related to or mediated by the SSAO/VAP-1 protein,wherein R1, R2, R3, R4, R5, R6, L1 and Cy1 are defined in the specification.
1,4-Palladium Shift/C(sp3)-H Activation Strategy for the Remote Construction of Five-Membered Rings
Rocaboy, Ronan,Baudoin, Olivier
supporting information, p. 1434 - 1437 (2019/02/19)
1,n-Metal shift is an elegant alternative approach enabling the functionalization of remote C-H bonds from simple precursors. In this work, we report a novel and simple Pd0-catalyzed domino reaction involving 1,4-palladium shift and C(sp3)-H activation and leading to (fused) five-membered rings. This method allowed access to a broad range of valuable arylidene γ-lactams and indanones and was applied to the formal synthesis of (-)-pyrrolam.
Synthesis of β-Lactams by Palladium(0)-Catalyzed C(sp3)?H Carbamoylation
Dailler, David,Rocaboy, Ronan,Baudoin, Olivier
supporting information, p. 7218 - 7222 (2017/06/13)
A general and user-friendly synthesis of β-lactams is reported that makes use of Pd0-catalyzed carbamoylation of C(sp3)?H bonds, and operates under stoichiometric carbon monoxide in a two-chamber reactor. This reaction is compatible with a range of primary, secondary and activated tertiary C?H bonds, in contrast to previous methods based on C(sp3)?H activation. In addition, the feasibility of an enantioselective version using a chiral phosphonite ligand is demonstrated. Finally, this method can be employed to synthesize valuable enantiopure free β-lactams and β-amino acids.
COMPOUNDS FOR THE MODULATION OF MYC ACTIVITY
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Paragraph 590; 591-592, (2017/01/31)
The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.
Promiscuous behavior of Rhizomucor miehei lipase in the synthesis of N-substituted β-amino esters
Monsalve, Leandro N.,Gillanders, Florencia,Baldessari, Alicia
experimental part, p. 1164 - 1170 (2012/04/10)
A mild and efficient procedure for the aza-Michael addition of amines to acrylates by using lipases as catalysts is reported. Various lipases, mono- and bifunctional amines, alkyl acrylates, and reaction parameters were studied. Under the optimal conditio
A quantitative structure-activity relationship study of herbicidal analogues of α-hydroxy-substituted 3-benzylidenepyrrolidene-2,4-diones
Zhu, You-Quan,Liu, Pei,Si, Xue-Kai,Zou, Xiao-Mao,Liu, Bin,Song, Hai-Bin,Yang, Hua-Zheng
, p. 7200 - 7205 (2008/02/03)
A series of pyrrolidine-2,4-dione and piperidine-2,4-dione derivatives were prepared and evaluated for their herbicidal activities where some of these compounds exhibited good bioactivity against Echinochloa crus-galli in comparison with sulcotrione. Quan
RuCl3 in poly(ethylene glycol): A highly efficient and recyclable catalyst for the conjugate addition of nitrogen and sulfur nucleophiles
Zhang, Huaxing,Zhang, Yuhong,Liu, Leifang,Xu, Hailiang,Wang, Yanguang
, p. 2129 - 2136 (2007/10/03)
The 1,4-conjugate addition of primary, secondary and aromatic amines, thiols, and carbamate to α,β-unsaturated compounds mediated by a catalytic amount (0.5 mol%) of RuCl3 in poly(ethylene glycol) (PEG) provides the desired β-substituted carbonyls in high yields. In particular, we found that primary aliphatic and aromatic amines produced the single adducts as the sole products in very high yields with RuCl3-PEG. RuCl 3-PEG was readily recycled via solvent precipitation with efficient recyclability as evidenced by high yields. Its properties of low sensitivity toward moisture and oxygen, high tolerance of different functional groups, and efficient recyclability make RuCl3-PEG suitable for both laboratory and industrial scale synthesis of β-substituted carbonyls. Georg Thieme Verlag Stuttgart.
Decarboxylation Reaction. X. Introduction of a Carbon unit at the α-Position of Amines by Reaction of Hexahydro-1,3,5-triazines with Carboxylic Acids
Fukawa, Hidemichi,Terao, Yoshiyasu,Achiwa, Kazuo,Sehiya, Minoru
, p. 94 - 99 (2007/10/02)
An efficient method for introducing a carbon unit at the α-position of alicyclic amines is described.The method involves the reaction of monocyclic or tetracyclic hexahydro-1,3,5-triazines with trichloroacetic acid, cyanoacetic acid, malonic acid and their derivatives, which are introduced into the α-position of amines in the decarboxylated form.Keywords --- 1,3,5-trialkylhexahydro-1,3,5-triazine; trimer of alicyclic imine; decarboxylation; β-amino acid; carboxylic acid
The Conformational Analysis of Saturated Heterocycles. Part 100. 1-Oxa-3-azacyclohexanes
Katritzky, Alan R.,Baker, Victor J.,Brito-Palma, Fernando M. S.
, p. 1739 - 1745 (2007/10/02)
Conformational equilibria and barriers to ring and nitrogen inversion are determined by 1H and 13C n.m.r. for 13 1-oxa-3-azacyclohexanes and correlated with recent work on the conformational analysis of saturated heterocycles.
