10250-27-8Relevant articles and documents
ELECTROREDUCTION OF 2-OXAZOLINES
Ryan, Christopher M.,Kariv-Miller, Essie
, p. 6807 - 6810 (1988)
The cathodic behavior of 2-phenyl-4,4-dimethyl-2-oxazoline (4), 2,4,4-trimethyl-2-oxazoline (7) and 2-(1,1-dimethylethyl)-4,4-dimethyl-2-oxazoline (8) at Hg electrodes was investigated.A reduction peak for 4 at -2.49V (SCE), was observed by cyclic voltamm
A new approach to the synthesis of N-arylakyl aminoalcohols
Leskovsek,Urleb
, p. 1415 - 1424 (1994)
N-arylmethyl substituted aminoalcohols were prepared by enantioselective reductive amination of different aromatic and heteroaromatic aldehydes using aminoalcohols and NaBH3CN as a catalyst. The reaction of optically active aminoalcohols afforded optically pure products.
Structure-based drug design of novel potent and selective tetrahydropyrazolo[1,5-a]pyrazines as ATR inhibitors
Barsanti, Paul A.,Aversa, Robert J.,Jin, Xianming,Pan, Yue,Lu, Yipin,Elling, Robert,Jain, Rama,Knapp, Mark,Lan, Jiong,Lin, Xiaodong,Rudewicz, Patrick,Sim, Janet,Taricani, Lorena,Thomas, George,Xiao, Linda,Yue, Qin
, p. 37 - 41 (2015)
A saturation strategy focused on improving the selectivity and physicochemical properties of ATR inhibitor HTS hit 1 led to a novel series of highly potent and selective tetrahydropyrazolo[1,5-a]pyrazines. Use of PI3Kα mutants as ATR crystal structure surrogates was instrumental in providing cocrystal structures to guide the medicinal chemistry designs. Detailed DMPK studies involving cyanide and GSH as trapping agents during microsomal incubations, in addition to deuterium-labeled compounds as mechanistic probes uncovered the molecular basis for the observed CYP3A4 TDI in the series. (Chemical Equation Presented).
HETEROARYL(HETEROCYCLYL)METHANOL COMPOUNDS USEFUL IN THE TREATMENT OF HYPERGLYCAEMIA
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Page/Page column 59; 60, (2020/10/09)
There is herein provided a compound of formula I (I) or a pharmaceutically acceptable salt thereof, wherein the ring comprising Q1 to Q5, R1, m, X1 and ring A have meanings as provided in the description.
HETEROCYCLYL(PHENYL)METHANOL COMPOUNDS USEFUL IN THE TREATMENT OF HYPERGLYCAEMIA
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Page/Page column 67-68, (2020/10/09)
There is herein provided a compound of formula I or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, ring A, n and y have meanings as provided in the description.
Direct Conversion of N-Alkylamines to N-Propargylamines through C-H Activation Promoted by Lewis Acid/Organocopper Catalysis: Application to Late-Stage Functionalization of Bioactive Molecules
Chan, Jessica Z.,Yesilcimen, Ahmet,Cao, Min,Zhang, Yuyang,Zhang, Bochao,Wasa, Masayuki
supporting information, p. 16493 - 16505 (2020/10/26)
An efficient catalytic method to convert an α-C-H bond of N-alkylamines into an α-C-alkynyl bond was developed. In the past, such transformations were carried out under oxidative conditions, and the enantioselective variants were confined to tetrahydroisoquinoline derivatives. Here, we disclose a method for the union of N-alkylamines and trimethylsilyl alkynes, without the presence of an external oxidant and promoted through cooperative actions of two Lewis acids, B(C6F5)3 and a Cu-based complex. A variety of propargylamines can be synthesized in high diastereo-and enantioselectivity. The utility of the approach is demonstrated by the late-stage site-selective modification of bioactive amines. Kinetic investigations that shed light on various mechanistic nuances of the catalytic process are presented.
Microwave-Assisted CuCl-Catalyzed Three-Component Reactions of Alkynes, Aldehydes, and Amino Alcohols
Chen, Ning,Li, Xiang,Xu, Jiaxi
supporting information, p. 3336 - 3344 (2019/08/28)
A microwave (MW)-assisted three-component coupling of amino alcohols, aldehydes, and alkynes is developed under catalysis by CuCl. Compared with thermal conditions, MW irradiation greatly increases the reaction efficiency. The reactions of various primary N -alkyl/arylamino alcohols, aliphatic/aromatic aldehydes, and alkynes are systematically investigated, affording the desired products in moderate to good yields. Notably, acetylene is also an effective reactant under the current MW-assisted conditions.
Selective Reductive Elimination at Alkyl Palladium(IV) by Dissociative Ligand Ionization: Catalytic C(sp3)?H Amination to Azetidines
Nappi, Manuel,He, Chuan,Whitehurst, William G.,Chappell, Ben G. N.,Gaunt, Matthew J.
supporting information, p. 3178 - 3182 (2018/02/28)
A palladium(II)-catalyzed γ-C?H amination of cyclic alkyl amines to deliver highly substituted azetidines is reported. The use of a benziodoxole tosylate oxidant in combination with AgOAc was found to be crucial for controlling a selective reductive elimination pathway to the azetidines. The process is tolerant of a range of functional groups, including structural features derived from chiral α-amino alcohols, and leads to the diastereoselective formation of enantiopure azetidines.
AROMATIC COMPOUND
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Paragraph 0937; 0938, (2016/05/19)
Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity and a GLP-1 secretagogue action, is useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and affords superior efficacy.
Synthesis and antibacterial activity of aromatic and heteroaromatic amino alcohols
de Almeida, Camila G.,Reis, Samira G.,de Almeida, Angelina M.,Diniz, Claudio G.,da Silva, Vania L.,Le Hyaric, Mireille
, p. 876 - 880 (2012/06/18)
Two series of aromatic and heteroaromatic amino alcohols were synthesized from alcohols and aldehydes and evaluated for their antibacterial activities. All the octylated compounds displayed a better activity against the four bacteria tested when evaluated by the agar diffusion method and were selected for the evaluation of minimal inhibitory concentration. The best results were obtained for p-octyloxybenzyl derivatives against Staphylococcus epidermidis (minimal inhibitory concentrations = 32μm).
