34381-71-0Relevant academic research and scientific papers
CHIROPTICAL PROPERTIES OF 2-SUBSTITUTED PYRROLIDINES
Ringdahl, Bjorn,Pereira, Wilfred E.,Craig, J. Cymerman
, p. 1659 - 1662 (1981)
The CD spectra of L-2-methylpyrrolidine, L-prolinol, and their N-methylated derivatives have been determined.As in the 2-substituted piperidines, N-methylation results in an inversion of the sign of the Cotton effects (CE).However, the sign of the long-wavelength CE does not follow the simple helicity rule found for 2-substituted piperidines, since the pyrrolidine ring is itself chiral and makes its own contributions to the observed CE's.The rotational contribution due to pyrrolidine ring chirality appears to be opposite in sign to and larger in magnitude than that due to the 2-substituent in both the secondary and the tertiary amines.
ENANTIOSELECTIVE EPOXIDATION OF AN ALLYLIC ALCOHOL CATALYZED BY (ACETYLACETONATO)(L-N-METHYLPROLINOL)DIOXOMOLYBDENUM. THE DECREASE OF ENANTIOSELECTIVITY WITH CHEMICAL CONVERSION
Coleman-Kammula, S.,Duim-Koolstra, E. Th.
, p. 53 - 56 (1983)
Epoxidation of 3-methyl-2-buten-1-ol with cumene hydroperoxide catalyzed by MoO2(acac)2 in the presence of L-N-methylprolinol yields epoxy alcohol of 50percent optical purity at relatively low conversions.This enantioselectivity decreases with increase in conversion, which is due to the destruction of the chirality of the catalyst via oxidation of the chiral ligand or its replacement.It is possible to maintain the initial chiral selectivity of 50percent AT over 80percent conversion by periodically adding more chiral ligand.
Pyrimidine derivative and application thereof in medicines
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Paragraph 0706; 0712-0714, (2021/07/21)
The invention discloses a pyrimidine derivative and application thereof in medicines, and particularly relates to a novel pyrimidine derivative and a pharmaceutical composition containing the compound. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition in preparation of drugs for treating KRAS G12C-mediated diseases and/or symptoms, especially in preparation of drugs for treating cancers.
FUMAGILLOL COMPOUNDS AND METHODS OF MAKING AND USING SAME
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, (2018/03/06)
Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
Chiral and Redox-Active Room-Temperature Ionic Liquids Based on Ferrocene and l-Proline
Bouvet, Carola B.,Krautscheid, Harald
supporting information, p. 4573 - 4580 (2016/10/11)
The syntheses of room-temperature ionic liquids (RTILs) combining the naturally occurring amino acid l-proline and ferrocene (Fc) building blocks are reported. After quaternization of ({[(2S)-N-methylpyrrolidine-2-yl]methyleneoxy}carbonyl)ferrocene (1) with alkyl iodides and anion exchange, the resulting diastereomeric (1S,2S)- and (1R,2S)-[(ferrocenylcarbonyl)oxy]methylene-N,N-dialkylpyrrolidine-1-ium RTILs are redox-active and air- and water-stable. They are also thermally stable up to 263 °C. The electrochemical FeII/FeIIIpotential is shifted to +0.28 V versus Fc/Fc+. Before anion exchange, several iodide derivatives were obtained as crystalline products, and their crystal structures are reported. According to the NMR spectroscopic data cation–anion aggregates are present in the non-coordinating solvent CDCl3. In contrast, in the polar solvent [D6]dimethyl sulfoxide ([D6]DMSO), the ion pairs are separated.
6-AMINO QUINAZOLINE OR 3-CYANO QUINOLINE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 44; 45, (2016/10/08)
The present disclosure relates to 6-amino quinazoline or 3-cyano quinoline derivatives, preparation processes and pharmaceutical compositions containing them. Specifically, the present disclosure relates to novel 6-amino quinazoline or 3-cyano quinoline derivatives presented by formula (I), or its tautomer, enantiomer, diastereomer, racemate or pharmaceutically acceptable salts thereof, or metabolite, metabolic precursor or prodrug thereof, and the uses for treatment especially for protein kinase inhibitors, in which each substitute group of general formula (I) is as defined in the specification.
PHARMACEUTICALLY ACCEPTABLE SALT OF (E)-N-[4-[[3-CHLORO-4-(2-PYRIDYLMETHOXY)PHENYL]AMINO]-3-CYANO-7-ETHOXY-6-QUINOLYL]-3-[(2R)-1-METHYLPYRROLIDIN-2-YL]PROP-2-ENAMIDE, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
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Page/Page column 0032; 0033, (2014/01/23)
Provided as represented by formula (I) is a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl] -3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, a preparation method therefor, and a use thereof as a therapeutic agent and especially as a protein kinase inhibitor.
PHARMACEUTICALLY ACCEPTABLE SALT OF (E)-N-[4-[[3-CHLORO-4-(2-PYRIDYLMETHOXY)PHENYL]AMINO]-3-CYANO-7-ETHOXY-6-QUINOLYL]-3-[(2R)-1-METHYLPYRROLIDIN-2-YL]PROP-2-ENAMIDE, PREPARATION METHOD THEREOF, AND MEDICAL USE THEREOF
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Paragraph 0037; 0038, (2014/02/15)
Provided as represented by formula (I) is a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, a preparation method thereof, and a use thereof as a therapeutic agent, and especially as a protein kinase inhibitor.
6-AMINO QUINAZOLINE OR 3-CYANO QUINOLINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
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, (2012/07/13)
6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof are disclosed. Specifically, the present disclosure discloses novel 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (I), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, and their uses as treatment agents especially as protein kinase inhibitors, in which each substitutent group of general formula (I) is as defined in the specification.
Asymmetric addition of terminal alkynes to n-(Diphenylphosphinoyl)imines promoted by stoichiometric amounts of a proline-derlved ss-amino alcohol
Yan, Wenjin,Mao, Bin,Zhn, Shaoqun,Jiang, Xianxing,Liu, Zhongli,Wang, Rui
supporting information; experimental part, p. 3790 - 3794 (2009/12/07)
A new synthetic methodology for the preparation of optically active propargylamines is described. The alkynylation of aromatic, heteroaromatic, aliphatic and α,β-unsaturated N-(di-phenylphosphinoyl)imines was investigated by using dieth-ylzinc and a proline-derived β-amino alcohol, N-(Diphenylphosphinoyl)-protected propargylic amines can be synthesized in high yields and with good to excellent: enantio-selectivities.
