83345-46-4Relevant academic research and scientific papers
N-[4-phenyl-3-(benzoylamino)-1,1,1-trifluoro-butyl-2-yl]-phenylalaninol derivative as well as preparation method and application thereof
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Paragraph 0051-0052; 0089-0092, (2020/11/23)
The present invention discloses an N-[4-phenyl-3-(benzoylamino)-1,1,1-trifluoro-butyl-2-yl]-phenylalaninol derivative, which is a compound represented by a general formula I and a pharmaceutically acceptable salt or hydrate thereof, and wherein R1 and R3
Chiral enantiopure organosilane precursors for the synthesis of periodic mesoporous organosilicas
Cohen, Orit,Abu-Reziq, Raed,Gelman, Dmitri
, p. 1675 - 1685 (2017/11/17)
The manuscript describes synthesis of new chiral organosilica networks starting from modified readily available enantiopure substances such as sugars and amino acids. We report on the successful preparation of robust all-chiral organosilicas by polymerization of the homochiral monomers. When the homochiral organosilane monomers were polymerized in mixtures of polar organic solvents and water in the presence of hydrochloric acid or tetrabutylammonium fluoride as catalysts, mainly spherical microparticles were obtained due to emulsification of the hydrophobic monomers in these mixtures. Polycondensation of the chiral organosilanes in the presence of Pluronic P123 as a template produced ordered mesoporous networks. The new all-chiral materials were characterized by SEM, STEM, BET, SAXS, IR, NMR and TGA.
ORALLY ADMINISTRABLE VIRIDIOFUNGIN DERIVATIVE HAVING ANTI-HCV ACTIVITY
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Paragraph 1801; 1802; 1803, (2015/07/02)
An object of the present invention is to provide a compound that is useful as an orally available anti-HCV agent. The present invention relates to a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. This compound has an anti-HCV activity and is useful as a medicine.
Chiral recyclable fluorous disulfonamide ligand for catalytic enantioselective cyclopropanation of allylic alcohols
Kawashima, Yuya,Ezawa, Tetsuya,Yamamura, Mai,Harada, Taisuke,Noguchi, Takuya,Miura, Tsuyoshi,Imai, Nobuyuki
, p. 8585 - 8592 (2016/01/25)
Allylic alcohols reacted with Et2Zn and CH2I2 in the presence of a catalytic amount of fluorous disulfonamide 3a to afford the corresponding cyclopropylmethanols in 69%-quantitative yields with 49-85% ee. Recovery of the fluorous ligand 3a was readily performed from the reaction mixture by the fluorous solid-phase extraction (FSPE), and the recovered 3a could be reused without a significant loss of the catalytic activity and enantioselectivity.
Two modes of asymmetric polymerization of phenylacetylenes having an L -amino alcohol residue and two hydroxy groups
Jia, Hongge,Li, Jun,Zang, Yu,Aoki, Toshiki,Teraguchi, Masahiro,Kaneko, Takashi
, p. 5134 - 5143 (2013/01/15)
Four novel chiral phenylacetylenes having an L-amino alcohol residue and two hydroxymethyl groups were synthesized and polymerized by an achiral catalyst ((nbd)Rh+[η6-(C6H5)B -(C6H5)3]) or a chiral catalytic system ([Rh(nbd)Cl]2/(S)- or (R)-phenylethylamine ((S)- or (R)-PEA)). The two resulting polymers having an L-valinol or L-phenylalaninol residue showed Cotton effects at wavelengths around 430 nm. This observation indicated that they had an excess of one-handed helical backbones. Positive and negative Cotton effects were observed only for the polymers having an L-valinol residue produced by using (R)- and (S)-PEA as a cocatalyst, respectively, although the monomer had the same chirality. Even when the achiral catalyst was used, the two resulting polymers having an L-valinol or L-phenylalaninol residue showed Cotton effects despite the long distance between the chiral groups and the main chain. We have found the first example of a new type of chiral monomer, that is, a chiral phenylacetylene monomer having an L-amino alcohol residue and two hydroxy groups that was suitable for both modes of asymmetric polymerization, that is, the helix-sense-selective polymerization (HSSP) with the chiral catalytic system and the asymmetric-induced polymerization (AIP) with the achiral catalyst. The other two monomers having L-alaninol and L-tyrosinol were found to be unsuitable to neither HSSP nor AIP because of their polymers' low solubility.
Studies toward the total synthesis of the hirsutellones
Huang, Mingzheng,Huang, Chong,Liu, Bo
experimental part, p. 2797 - 2800 (2009/09/28)
A strategy of tandem ketene-trapping/IMDA toward the total synthesis of the hirsutellones was attempted. The AB ring moiety of the hirsutellones was constructed with the proper stereochemistry.
Catalytic enantioselective cyclopropanation of allylic alcohols using recyclable fluorous disulfonamide ligand
Miura, Tsuyoshi,Itoh, Keisuke,Yasaku, Yumi,Koyata, Naka,Murakami, Yasuoki,Imai, Nobuyuki
, p. 5813 - 5815 (2008/12/22)
Cyclopropanation of allylic alcohols with Et2Zn and CH2I2 in the presence of a catalytic amount of fluorous disulfonamide 3 afforded the corresponding cyclopropylmethanols in 69-96% yield with 49-83% ee. The fluorous ligand 3 was readily recovered from the reaction mixture by the fluorous solid-phase extraction (FSPE) and could be reused without a significant loss of the catalytic activity and enantioselectivity.
Synthesis of a new chiral auxiliary: Non-cross-linked polystyrene bound (4S)-oxazolidine-2-thione
Chen, Jianian,Nie, Junqi,Huang, Yanling,Chen, Zuxing,Yang, Guichun
, p. 696 - 697 (2007/10/03)
A new chiral auxiliary, non-cross-linked polystyrene bound (4S)-oxazolidine-2-thione, was synthesised from L-tyrosine in 24.2% by a seven step method.
S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: Synthesis, antiviral activity, and stability study
Peyrottes, Suzanne,Coussot, Ga?lle,Lefebvre, Isabelle,Imbach, Jean-Louis,Gosselin, Gilles,Aubertin, Anne-Marie,Périgaud, Christian
, p. 782 - 793 (2007/10/03)
The synthesis, antiviral activity, and stability study of phosphotriester derivatives of 3′-azido-2′,3′-dideoxythymidine (AZT) bearing modified L-tyrosinyl residues are reported. These compounds were obtained via phosphoramidite (PIII) chemistr
Tyropeptins A and B, new proteasome inhibitors produced by Kitasatospora sp. MK993-dF2 II. Structure determination and synthesis
Momose, Isao,Sekizawa, Ryuichi,Hirosawa, Sehei,Ikeda, Daishiro,Naganawa, Hiroshi,Inuma, Hironobu,Takeuchi, Tomio
, p. 1004 - 1012 (2007/10/03)
The structures of tyropeptins A and B, new proteasome inhibitors produced by Kitasatospora sp. MK993-dF2, were determined by analysis of various NMR experiments. The 1H and 13C NMR of tyropeptins were complicated due to the presence of an aldehyde group. Therefore, tyropeptins were converted to their alcohols by sodium borohydride. These alcohol derivatives gave assignable NMR spectra. The stereochemistry of tyropeptins were determined by analysis of acid hydrolysis products from tyropeptins, and further confirmed by the total synthesis. The structures of tyropeptins A and B were found to be isovaleryl-L-tyrosyl-L-valyl-DL-tyrosinal and n-butyryl-L-tyrosyl-L-leucyl-DL-tyrosinal, respectively.
