73604-31-6Relevant academic research and scientific papers
Selective catalysis for the reductive amination of furfural toward furfurylamine by graphene-co-shelled cobalt nanoparticles
Liu, Jianguo,Ma, Longlong,Zhong, Shurong,Zhuang, Xiuzheng
, p. 271 - 284 (2022/01/19)
Amines with functional groups are widely used in the manufacture of pharmaceuticals, agricultural chemicals, and polymers but most of them are still prepared through petrochemical routes. The sustainable production of amines from renewable resources, such as biomass, is thus necessary. For this reason, we developed an eco-friendly, simplified, and highly effective procedure for the preparation of a non-toxic heterogeneous catalyst based on earth-abundant metals, whose catalytic activity on the reductive amination of furfural or other derivatives (more than 24 examples) proved to be broadly available. More surprisingly, the cobalt-supported catalyst was found to be magnetically recoverable and reusable up to eight times with an excellent catalytic activity; on the other hand, the gram-scale tests catalyzed by the same catalyst exhibited the similar yield of the target products in comparison to its smaller scale, which was comparable to the commercial noble-based catalysts. Further results from a series of analytical technologies involving XRD, XPS, TEM/mapping, and in situ FTIR revealed that the structural features of the catalyst are closely in relation to its catalytic mechanisms. In simple terms, the outer graphitic shell is activated by the electronic interaction as well as the induced charge redistribution, enabling the easy substitution of the –NH2 moiety toward functionalized and structurally diverse molecules, even under very mild industrially viable and scalable conditions. Overall, this newly developed catalyst introduces the synthesis of amines from biomass-derived platforms with satisfactory selectivity and carbon balance, providing cost-effective and sustainable access to the wide applications of reductive amination.
Self-regulated catalysis for the selective synthesis of primary amines from carbonyl compounds
Fan, Xiaomeng,Gao, Jin,Gao, Mingxia,Jia, Xiuquan,Ma, Jiping,Xu, Jie
supporting information, p. 7115 - 7121 (2021/09/28)
Most current processes for the general synthesis of primary amines by reductive amination are performed with enormously excessive amounts of hazardous ammonia. It remains unclear how catalysts should be designed to regulate amination reaction dynamics at a low ammonia-to-substrate ratio for the quantitative synthesis of primary amines from the corresponding carbonyl compounds. Herein we show a facile control of the reaction selectivity in the layered boron nitride supported ruthenium catalyzed reductive amination reaction. Specifically, locating ruthenium to the edge surface of layered boron nitride leads to an increased hydrogenation activity owing to the enhanced interfacial electronic effects between ruthenium and the edge surface of boron nitride. This enables self-accelerated reductive amination reactions which quantitatively synthesize structurally diverse primary amines by reductive amination of carbonyl compounds with twofold ammonia. This journal is
2-(3-Hydroxybenzyl)benzo[d]isothiazol-3(2H)-one Mannich base derivatives as potential multifunctional anti-Alzheimer’s agents
He, Yuxi,Xiao, Ganyuan,Yu, Guangjun,Song, Qing,Zhang, Heng,Liu, Zhuoling,Tan, Zhenghuai,Deng, Yong
, p. 1249 - 1264 (2021/05/11)
A series of 2-(3-hydroxybenzyl)benzo[d]isothiazol-3(2H)-one Mannich base derivatives were designed as potential multifunctional agents against Alzheimer’s disease. The twelve derivatives were synthesized and evaluated with various biological activities. I
KINASE INHIBITOR
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Paragraph 0233; 0234, (2021/04/16)
The present invention aims to provide a novel kinase inhibitor and the like, and a therapeutic agent for a disease, a drug discovery screening method and the like utilizing such inhibitor and the like. The compound represented by the following formula (I) and a salt thereof can inhibit plural kinases including LATS (particularly LATS2) which is the major kinase in the Hippo signal transduction pathway. In addition, diseases or tissue damage associated with failure of cellular proliferation can be treated. Therefore, the present invention is beneficial, for example, in the research field of cell functions and diseases, in which the Hippo signal transduction pathway is involved, and the like. Furthermore, it is beneficial in the medical field for the treatment of such diseases and the like. wherein each symbol is as defined in the DESCRIPTION.
ADDITIVE COMPOSITION FOR CULTURE MEDIUM, ADDITIVE COMPOUND FOR CULTURE MEDIUM, AND METHOD FOR CULTURE OF CELLS OR TISSUE USING SAME
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Paragraph 0227-0228, (2020/06/15)
The present invention provides a medium additive composition containing a compound represented by the following formula (I), or a salt thereof: {wherein each symbol is as defined in the DESCRIPTION.}
Method for synthesizing hydroxybenzylamine
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Paragraph 0043-0045, (2020/02/27)
The invention discloses a method for synthesizing hydroxybenzylamine, and belongs to the technical field of organic synthesis. The principle of the method comprises that a demethylation reaction is carried out on methoxybenzylamine under the action of hydrobromic acid; the method is characterized in that methoxybenzylamine and hydrobromic acid are distilled in a reflux state to remove redundant water so as to increase the reaction temperature and increase the concentration of the hydrobromic acid in a reaction mixture, so that the demethylation effect of hydrobromic acid on methoxybenzylamineis enhanced, the reaction time is shortened, and the conversion rate is increased; when no bromomethane gas generation is observed, distillation is continued, excessive hydrobromic acid is recovered to further improve the reaction temperature and the conversion rate, meanwhile, the consumption of the raw material hydrobromic acid is reduced, and the treatment capacity of subsequent steps and the consumption of the raw material sodium hydroxide can also be reduced; therefore, the method has the advantages of simple technological process; the reaction time is short; the product is easy to purify; raw material consumption is low; the reaction yield is high.
Design and synthesis of aryloxypropanolamine as β3-adrenergic receptor antagonist in cancer and lipolysis
Jin, Jiyu,Miao, Chunxiao,Wang, Zhilong,Zhang, Wanli,Zhang, Xiongwen,Xie, Xin,Lu, Wei
, p. 757 - 770 (2018/03/26)
β-adrenergic receptors (β-ARs) are broadly distributed in various tissues and regulate a panel of important physiological functions and disease states including cancer. Above all, β3-adrenergic receptor (β3-AR) plays a significant ro
Derivative containing aryloxy substituting propyl-2-hydramine as beta 3 adrenergic receptor antagonist, preparation method and application
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Paragraph 0045-0048, (2017/11/16)
The invention provides a compound containing an aryloxy substituting propyl-2-hydramine shown in the formula I, a preparation method of the compound, in vitro and in vivo biological activity and application, which belong to the technical field of drug syn
N6-benzyladenosine derivatives as novel n-donor ligands of platinum(ii) dichlorido complexes
Starha, Pavel,Popa, Igor,Travnicek, Zdenek,Vanco, Jan
, p. 6990 - 7003 (2013/07/26)
The platinum(II) complexes trans-[PtCl2(Ln)2]·xSolv 1-13 (Solv = H2O or CH3OH), involving N6-benzyladenosine-based N-donor ligands, were synthesized; Ln stands for N6-(2-methoxybenzyl)adenosine (L1, involved in complex 1), N6-(4-methoxybenzyl) adenosine (L2, 2), N6-(2-chlorobenzyl)adenosine (L3, 3), N6-(4-chlorobenzyl)- adenosine (L4, 4), N6-(2-hydroxybenzyl)adenosine (L5, 5), N6-(3-hydroxybenzyl)- adenosine (L6, 6), N6-(2-hydroxy-3-methoxybenzyl) adenosine (L7, 7), N6-(4-fluorobenzyl) adenosine (L8, 8), N6-(4-methylbenzyl) adenosine (L9, 9), 2-chloro-N6-(3-hydroxybenzyl) adenosine (L10, 10), 2-chloro-N6-(4-hydroxybenzyl)adenosine (L11, 11), 2-chloro- N6-(2-hydroxy-3- methoxybenzyl)adenosine (L12, 12) and 2-chloro-N6-(2-hydroxy-5- methylbenzyl)adenosine (L13, 13). The compounds were characterized by elemental analysis, mass spectrometry, IR and multinuclear (1H-, 13C-, 195Pt- and 15N-) and two-dimensional NMR spectroscopy, which proved the N7-coordination mode of the appropriate N6-benzyladenosine derivative and trans-geometry of the title complexes. The complexes 1-13 were found to be non-toxic in vitro against two selected human cancer cell lines (HOS and MCF7; with IC50 > 50.0 μM). However, they were found (by ESI-MS study) to be able to interact with the physiological levels of the sulfur-containing biogenic biomolecule L-methionine by a relatively simple 1:1 exchange mechanism (one Ln molecule was replaced by one L-methionine molecule), thus forming a mixed-nitrogen/sulfur-ligand dichlorido-platinum(II) coordination species.
Inhibitors of farnesyl protein transferase
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, (2008/06/13)
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:, ???G is ???when G is it is optionally substituted, at any available position or positions, with halo, alkyl or substituted alkyl having 1 to 20 carbon atoms, alkoxy, or a combination of these groups;, ???G1is optionally substituted, at any of the available position or positions on the ring, with halo, alkyl or substituted alkyl having 1 to 20 carbon atoms, alkoxy, aryl, aralkyl, hydroxy, alkanoyl, alkanoyloxy, amino, alkylamino, dialkylamino, alkanoylamino, thiol, alkylthio, alkylthiono, alkylsulfonyl, sulfonamido, nitro, cyano, carboxy, carbamyl, N-hydroxycarbamyl, N-alkylcarbamyl, N-dialkylcarbamyl, alkoxycarbonyl, phenyl, substituted phenyl, or a combination of these groups;, ???G2is or -NR6-CH(Q1)-;, ???J, K and L are each, independently, N, NR7, O, S or CR6with the provisos that only one of the groups J, K and L can be O or S, and at least one of the groups J or L must be N, NR7, O or S to form a fused five-membered heteroring; the bond between J and K or K and L may also form one side of a phenyl ring fused to the fused five-membered heteroring;, ???Q is is alkyl, cycloalkyl, substituted alkyl, aryl, pyrrolyl, furyl, thiophenyl, imidazolyl, oxazolyl, thiazolyl, pyrazolyl, pyrrolidyl or pyridyl;, ???Q1, A1and A2are each, independently, H, alkyl, substituted alkyl, phenyl or substituted phenyl;, ???G3is R8, -C(O)OR8, -C(O)NR8R9, -C(O)N(R10)OR8, -C(O)NHSO2R11or -CH2OR8;, ???X is -SH, -OH or -NHR12;, ???X1is -NR13-, -CH2- or -CH(NHR14)-;, ???Y and Z are each, independently, -CH2- or -C(O)-;, ???R1- R14are each, independently, H or alkyl having 1 to 20 carbon atoms;, ???R3may also be substituted alkyl or cycloalkyl; R4, R5and R11may also be aryl or aralkyl; R7, R8, R9and R10may also be aralkyl; and R12, R13and R14may also be substituted alkyl or aralkyl;, ???m is 0 or an integer from 1 to 2;, ???q is 0 or an integer from 1 to 3;, ???t is an integer from 1 to 2; and, ???the dotted line represents an optional double bond.
