- A photoinduced refractive index increase in poly(methyl methacrylate) film doped with N-acetyl-α-dehydroarylalanine naphthyl esters
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The short period of time irradiation of poly(methyl) methacrylate) (PMMA) film doped with N-acetyl-α-dehydrophenylalanine 1-naphthyl ester (1a) or N-acetyl-α-dehydro(1-naphthyl)alanine 1-naphthyl ester (1b) that increases the refractive index of the polym
- Tanaka, Kenta,Nakajima, Haruki,Igarashi, Tetsutaro,Sakurai, Tadamitsu
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Read Online
- A novel synthetic protocol for the synthesis of pulvinones, and naturally occurring Aspulvinone E, molecules of medicinal interest
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A novel two step methodology for readily accessible natural “pulvinone” derivatives in excellent yields has been developed starting from activated precursors, bearing a functionalized 1,3-dioxolane-2,4-diones (OCA’s), as dually protected-activated synthon
- Igglessi-Markopoulou, Olga,Katsamakas, Sotirios,Markopoulos, John,Prousis, Kyriakos C.
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supporting information
(2021/11/22)
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- Concise synthesis and applications of enantiopure spirobiphenoxasilin-diol and its related chiral ligands
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The development of chiral architectures for chiral ligand and catalyst discovery is essential for asymmetric catalysis. Herein, we report the concise synthesis of a Si-centered spirocyclic skeleton, spirobiphenoxasilin-diol (SPOSiOL), and its derived chiral ligands. Using the chemical resolution method, the optical SPOSiOL could be obtained in high yield on a gram scale. Preliminary studies indicated that this ligand scaffold has great potential in transition metal-catalyzed asymmetric reactions. This finding further highlights that the Si-centered spirocyclic scaffolds are of great value in asymmetric catalysis. This journal is
- Liu, Tao,Wang, Biqin,Wang, Peng,Wu, Yichen,Xu, Wen-Qiang,Yang, Lei
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supporting information
p. 13365 - 13368
(2021/12/17)
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- Synthesis, biological evaluation and structure-activity relationships of 5-arylidene tetramic acids with antibacterial activity against methicillin-resistant Staphylococcus aureus
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The steady rise of the antimicrobial resistance is a major global threat to human health that requires the urgent need for novel antibiotics. In this work we report the synthesis of a small library of 3-subsituted-5-arylidene tetramic acids in order to in
- Matiadis, Dimitris,Tsironis, Dimitrios,Stefanou, Valentina,Boussias, Spyridon,Panagiotopoulou, Angeliki,McKee, Vickie,Igglessi-Markopoulou, Olga,Markopoulos, John
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supporting information
(2020/04/08)
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- Pharmaceutical composition and method of treating cancer
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Cytotoxic compounds containing a phenyl core, amide link(s), an imidazolinone or a propenamide moiety. Also described are pharmaceutical compositions incorporating the cytotoxic compounds and methods for treating cancer. These compounds are cytotoxic against breast, prostate, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.
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Page/Page column 47
(2020/12/07)
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- Synthesis of 2-substituted 4-arylidene-5(4h)-oxazolones as potential cytotoxic agents in the presence of lemon juice as a biocatalyst
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Background: The oxazolone class of compounds is known to exert a profound effect on malignant cell proliferation, tumor angiogenesis and /or on the established neoplastic vasculature. Additionally, these compounds are generally known to have a low tendenc
- Anand, Krishnan,Jonnalagadda, Sreekantha B.,Katari, Naresh K.,Lakshmi, Chapala V.,Pal, Manojit,Prasad, Malavattu G.
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p. 625 - 634
(2020/01/21)
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- Copper nitrate-mediated synthesis of 3-aryl isoxazolines and isoxazoles from olefinic azlactones
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A copper nitrate-mediated [2 + 2 + 1] cycloaddition reaction was developed for the expedient synthesis of pharmacologically interesting 3-aryl substituted isoxazolines and isoxazoles through CC bond cleavage. Copper nitrate is employed as a reaction promoter and precursor of nitrile oxides. The given approach features a new mode of cycloaddition from olefinic azlactones, copper nitrate and unsaturated compounds with wide substrate scope, good functional group tolerance and operational simplicity.
- Lin, Yifan,Zhang, Ke,Gao, Mingchun,Jiang, Zheyi,Liu, Jiajie,Ma, Yurui,Wang, Haoyu,Tan, Qitao,Xiao, Junjie,Xu, Bin
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supporting information
p. 5509 - 5513
(2019/06/14)
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- An Atropos Chiral Biphenyl Bisphosphine Ligand Bearing Only 2,2′-Substituents and Its Application in Rh-Catalyzed Asymmetric Hydrogenation
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An atropos chiral biphenyl bisphosphine ligand bearing only 2,2′-substituents was rationally designed and easily synthesized utilizing a bulky chiral t-butylmethylphosphino block. Computational results showed a large difference in the free energies betwee
- Jia, Jia,Ling, Zheng,Zhang, Zhenfeng,Tamura, Ken,Gridnev, Ilya D.,Imamoto, Tsuneo,Zhang, Wanbin
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supporting information
p. 738 - 743
(2017/12/26)
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- Development of benzylidene-methyloxazolone based AIEgens and decipherment of their working mechanism
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Based on an analogue of green fluorescent protein chromophore benzylidene-methyloxazolone (BMO), a series of fluorophores with an additional phenyl group, BMO-PH, BMO-PF, BMO-PM and BMO-PC, have been prepared and are found to be AIE-active. Their solutions are weakly emissive and their aggregation or solid states are highly emissive. Although these compounds readily undergo efficient E/Z isomerization (EZI) upon UV irradiation in solution, the intramolecular rotation around the double bond and phenyl rotation around the single bond serve as the key non-radiative decay channels to dissipate the excited-state energies. The EZI is only the phenomenal result. In aggregates, these intramolecular motions are greatly restricted by multiple intermolecular interactions, resulting in the AIE effect. To ensure a high solid-state quantum yield, prevention of detrimental π-π stacking is of essence. An additional phenyl group to BMO is found to increase the π-π distance and weaken the π-π interaction. Thus, the quantum yields are increased. Strong electron-donating groups and extended conjugation are effective at tuning the emission color bathochromically. Based on these principles, we succeeded in increasing the solid-state quantum yield up to 50% and obtaining a red emission maximum of 635 nm. Moreover, these compounds are promising for applications in photoswitches and fluorescent patterns, and their crystals are good candidates for luminescent waveguides with low light loss efficiency.
- Jiang, Meijuan,He, Zikai,Zhang, Yilin,Sung, Herman H. Y.,Lam, Jacky W. Y.,Peng, Qian,Yan, Yongli,Wong, Kam Sing,Williams, Ian D.,Zhao, Yongsheng,Tang, Ben Zhong
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supporting information
p. 7191 - 7199
(2017/08/04)
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- Green fluorescent protein chromophore derivatives as a new class of aldose reductase inhibitors
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A number of (Z)-4-arylmethylene-1H-imidazol-5(4H)-ones, which are related to the fluorescent chromophore of the Aequorea green fluorescent protein (GFP), have been synthesized and evaluated their in vitro inhibitory activity against recombinant human aldo
- Saito, Ryota,Hoshi, Maiko,Kato, Akihiro,Ishikawa, Chikako,Komatsu, Toshiya
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p. 965 - 974
(2016/10/25)
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- Construction of Chiral-Fused Tricyclic γ-Lactams via a trans-Perhydroindolic Acid-Catalyzed Asymmetric Domino Reaction
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An asymmetric domino reaction was developed utilizing readily available cyclic α-dehydroamino ketones and aldehydes, which when subjected a 2-iodoxybenzoic acid (IBX)-mediated oxidation gives pyrrolidinone-containing tricyclic derivatives. trans-Perhydroi
- An, Qianjin,Shen, Jiefeng,Liu, Delong,Liu, Yangang,Zhang, Wanbin
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supporting information
p. 2925 - 2928
(2017/06/07)
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- 4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors
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This study reports on a preliminary structure-activity relationship exploration of 4-aryliden-2-methyloxazol-5(4H)-one-based compounds as MAGL/FAAH inhibitors. Our results highlight that this scaffold may serve for the development of selective MAGL inhibi
- Granchi, Carlotta,Rizzolio, Flavio,Bordoni, Vittorio,Caligiuri, Isabella,Manera, Clementina,Macchia, Marco,Minutolo, Filippo,Martinelli, Adriano,Giordano, Antonio,Tuccinardi, Tiziano
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p. 137 - 146
(2016/01/12)
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- Synthesis of Indole-2-carboxylate Derivatives via Palladium-Catalyzed Aerobic Amination of Aryl C-H Bonds
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A direct oxidative C-H amination affording 1-acetyl indolecarboxylates starting from 2-acetamido-3-arylacrylates has been achieved. Indole-2-carboxylates can be targeted with a straightforward deacetylation of the initial reaction products. The C-H amination reaction is carried out using a catalytic Pd(II) source with oxygen as the terminal oxidant. The scope and application of this chemistry is demonstrated with good to high yields for numerous electron-rich and electron-poor substrates. Further reaction of selected products via Suzuki arylation and deacetylation provides access to highly functionalized indole structures.
- Clagg, Kyle,Hou, Haiyun,Weinstein, Adam B.,Russell, David,Stahl, Shannon S.,Koenig, Stefan G.
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supporting information
p. 3586 - 3589
(2016/08/16)
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- Temperature-controlled bidirectional enantioselectivity in a dynamic catalyst for asymmetric hydrogenation
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Asymmetric catalysis using enantiomerically pure catalysts is one of the most widely used methods for the preparation of enantiomerically pure compounds. The separate synthesis of both enantiomerically pure compounds requires tedious and time-consuming pr
- Storch, Golo,Trapp, Oliver
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supporting information
p. 3580 - 3586
(2015/03/18)
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- Synthesis of Erlenmeyer azlactones using arylsulphonyl chloride as cyclocondensing agent
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A fast and facile procedure for one flask synthesis of (Z)-2-substituted-4- arylmethylene-2-oxazolin-5-ones (3) which are popularly known as Erlenmeyer azlactones, is being reported starting from N-acylglycines (1) and different aromatic aldehydes using arylsulphonyl chloride as cyclocondensing agent in the presence of triethyl amine base and dry benzene. The reaction time is reduced to minute under milder conditions alongwith higher yields of the products.
- Goswami, Limi,Tripathy, Pradeep K.
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p. 281 - 282
(2019/01/21)
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- An efficient and green synthesis of benzylidene-2-N-(carbothioamido)-6-oxo-1,2,5,6-tetrahydro-1-NH-1,2,4-triazine derivatives and their antibacterial activity evaluation
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An efficient and green synthesis of (Z)-3-allkyl-5(benzylidene/substituted benzylidene)-2N-(carbothioamido)-6-oxo-1,2,5,6-tetrahydro-1-NH-1,2,4-triazine derivatives have been developed in good yields and tested for their antibacterial activities against Escherichia coli, Providencia aeruginosa, Pseudomonas azotogensis and Baccilus subtillis. Some of the synthesized compounds possess good activity against Escherichia coli and Baccilus subtillis compared to standard drug streptomycin.
- Rani, V. Anitha,Kumari, Y. Bharathi
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p. 5931 - 5934
(2015/02/19)
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- Oxazolone-based photoswitches: Synthesis and properties
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The synthesis, photophysics and photochemistry of a family of molecular switches inspired by the green fluorescent protein (GFP) chromophore is presented. These compounds can be synthesized in one step and good yields, their photophysical properties may b
- Blanco-Lomas, Marina,Funes-Ardoiz, Ignacio,Campos, Pedro J.,Sampedro, Diego
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supporting information
p. 6611 - 6618
(2013/11/06)
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- Benzylidene-oxazolones as photoswitches: Photochemistry and theoretical calculations
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The photophysics and photochemistry of a family of compounds proposed as efficient molecular photoswitches is presented. The effect of different light sources, substituents and solvents in the photostationary state has been explored. A detailed mechanisti
- Funes-Ardoiz, Ignacio,Blanco-Lomas, Marina,Campos, Pedro J.,Sampedro, Diego
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supporting information
p. 9766 - 9771
(2013/10/22)
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- Synthesis of novel cinnamanilides as potential immunosuppressive agents
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A series of new cinnamanilides (6-40) were synthesized and their immunosuppressive activity and cytotoxicity were evaluated. Most of the cinnamanilides showed good immunosuppressive activity. Among the synthesized compounds, (Z)-N-(4-bromophenyl)-2-methox
- Shi, Lei,Wang, Lu,Wang, Zhi,Zhu, Hai-Liang,Song, Qiao
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experimental part
p. 585 - 593
(2012/02/14)
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- Benzylidene-oxazolones as molecular photoswitches
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The synthesis and photochemical study of a family of molecular switches inspired by the green fluorescent protein (GFP) chromophore is presented. These compounds can be easily synthesized, and their photophysical properties may be tuned. Due to their effi
- Blanco-Lomas, Marina,Campos, Pedro J.,Sampedro, Diego
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supporting information
p. 4334 - 4337
(2012/10/29)
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- Pseudo-peptides derived from isomannide: Inhibitors of serine proteases
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In this paper, we describe the synthesis of a novel class of pseudo-peptides derived from isomannide and several oxazolones as potential inhibitors of serine proteases as well as preliminary pharmacological assays for hepatitis C. Hepatitis C, dengue and West Nile fever are among the most important flaviviruses that share one important serine protease enzyme. Serine proteases belong to the most studied class of proteolytic enzymes and are a primary target in the drug development field. Several pseudo-peptides were obtained in good yields from the reaction of isomannide and oxazolones, and their anti-HCV potential using the HCV replicon-based assay was shown.
- Barros, Thalita G.,Pinheiro, Sergio,Williamson,Tanuri, Amilcar,Gomes Jr.,Pereira, Helena S.,Brindeiro,Neto, Jose B. A.,Antunes,Muri, Estela M. F.
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scheme or table
p. 701 - 709
(2010/08/05)
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- New and convenient route for the synthesis of some new pyrazol-5-yl-1H- imidazole derivatives
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A simple and efficient method for the synthesis of some new pyrazol-5-yl-1H-imidazoles 4a-h is described. In this method oxazolones 5a-h were produced as minor products. The X-ray analysis confirmed the structures of 4 and 5. The Japan Institute of Heterocyclic Chemistry.
- Zonouzi, Afsaneh,Mirzazadeh, Roghieh,Talebi, Marzieh,Jafarypoor, Razieh,Peivandi, Azadeh,Ng, Seik Weng
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experimental part
p. 2131 - 2138
(2011/04/18)
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- Isomerization in fluorescent protein chromophores involves addition/elimination
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The green fluorescent protein (GFP) chromophore undergoes both photochemical and thermal isomerizations. Typically, the Z form is more stable and undergoes photochemical conversion to the E form followed by thermal reversion over a period of seconds or minutes. Although the mechanism of the thermal reversion has been the subject of some investigations, the surprisingly low activation energy for this process has not sparked any controversy. We now show that the chromophore is surprisingly stable in both E and Z forms and that the facile thermal reversion is the result of a novel nucleophilic addition/elimination mechanism. This observation may have implications for the intervention of such processes, as well as blinking and kindling, in fluorescent proteins. Copyright
- Dong, Jian,Abulwerdi, Fardokht,Baldridge, Anthony,Kowalik, Janusz,Solntsev, Kyril M.,Tolbert, Laren M.
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supporting information; experimental part
p. 14096 - 14098
(2009/03/11)
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- Efficient formation of a triazole ring via novel ring-opening reaction of (Z)-2-methyl-4-arylmethylene-5(4H)-oxazolones with hydrazides
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The ring-opening mode of the title oxazolones with hydrazide nucleophiles was investigated from both synthetic and mechanistic points of view. It was found that the novel ring-opening reaction proceeded to give (Z)-2-(3-methyl-5-substituted 1,2,4-triazol-
- Maekawa, Kei,Tomoda, Atsushi,Igarashi, Tetsutaro,Sakurai, Tadamitsu
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experimental part
p. 2959 - 2971
(2009/05/31)
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- Practical preparation of Z-α-(N-acetylamino)- and Z-α-(N-benzoylamino)-α,β-unsaturated acids
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An efficient two-step synthetic procedure for the preparation of numerous variations of N-protected α,β-unsaturated α-amino acids and their corresponding esters from N-protected glycine and either aliphatic or aromatic aldehydes was developed. The reaction involved cyclization of the N-protected glycine into oxazolone, condensation with the aldehyde, and ring opening with a base. Copyright Taylor & Francis Group, LLC.
- Jursic, Branko S.,Sagiraju, Sarada,Ancalade, Dustin K.,Clark, Traneil,Stevens, Edwin D.
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p. 1709 - 1714
(2008/02/01)
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- Three distinct reactions of 3,4-dihydroisoquinolines with azlactones: Novel synthesis of imidazoloisoquinolin-3-ones, benzo[a]quinolizin-4-ones, and benzo[d]azocin-4-ones
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(Diagram presented) A facile and direct synthetic entry to tricyclic imidazoloisoquinolin-3-ones and benzo[a]quinolizin-4-ones is reported based on the ring annulation of 1-unsubstituted and 1-substituted dihydroisoquinolines with azlactones under neutral
- Worayuthakarn, Rattana,Thasana, Nopporn,Ruchirawat, Somsak
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p. 5845 - 5848
(2007/10/03)
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- Deracemisation of aryl substituted α-hydroxy esters using Candida parapsilosis ATCC 7330: Effect of substrate structure and mechanism
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Candida parapsilosis ATCC 7330 was found to be an efficient biocatalyst for the deracemisation of aryl α-hydroxy esters (65-85% yield and 90-99% ee). A variety of aryl and aryl substituted α-hydroxy esters were synthesized to reflect steric and electronic effects on biocatalytic deracemisation. The mechanism of this biocatalytic deracemisation was found to be stereoinversion.
- Baskar,Pandian,Priya,Chadha, Anju
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p. 12296 - 12306
(2007/10/03)
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- A novel route to 2-imidazolin-5-one derivatives via oxidative cyclization of aryl-substituted (Z)-N-acetyl-α-dehydroalanines having a dialkylamino group
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It was found that the reaction of the title compounds [(Z)-1] with oxygen in methanol proceeds according to the first-order kinetics to give (Z)-2-imidazolin-5-one derivatives and hydrogen peroxide in quantitative yields. Analysis of substituent and solve
- Kawasaki, Atsushi,Maekawa, Kei,Kubo, Kanji,Igarashi, Tetsutaro,Sakurai, Tadamitsu
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p. 9517 - 9524
(2007/10/03)
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- Phenylpyruvic acid derivatives as enzyme inhibitors: Therapeutic potential on macrophage migration inhibitory factor
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Phenylpyruvic acid derivatives are obtained by hydrolysing aromatic Z/E azlactones. Keto tautomers interact with enzyme systems such as phenylalanine dehydrogenase or carboxypeptidase A whereas enol tautomers are potential inhibitors on the phenylpyruvate tautomerase activity catalysed by Macrophage Migration Inhibitory Factor (MIF). MIF being a key molecule in immune and inflammatory processes several structures with reasonable interaction with MIF and protocol for specific synthesis are presented. Birkhaeuser Boston 2004.
- Carpy, Alain J. M.,Haasbroek, Petrus P.,Oliver, Douglas W.
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p. 565 - 577
(2007/10/03)
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- Formation of isoquinoline and 1-azetine derivatives via novel photocyclization of substituted α-dehydrophenylalanines
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The irradiation of substituted N-acetyl α-dehydrophenylalanines in MeOH with Pyrex-filtered light was found to give isoquinoline and 1-azetine derivatives in relatively good yields, which may be formed via intramolecular cyclization reactions from the (Z)
- Hoshina, Hideki,Kubo, Kanji,Morita, Asako,Sakurai, Tadamitsu
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p. 2941 - 2951
(2007/10/03)
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- Formation of isoquinoline derivatives by the irradiation of N-acetyl-α-dehydrophenylalanine ethyl ester and its derivatives
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The irradiation of a nitrogen-purged acetonitrile solution of the title compounds (1) with Pyrex filtered light was found to give isoquinoline derivatives (2) via the excited state (Z)-isomers, whereas in methanol 1-azetine derivative was also detected al
- Hoshina, Hideki,Tsuru, Hitoshi,Kubo, Kanji,Igarashi, Tetsutaro,Sakurai, Tadamitsu
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p. 2261 - 2274
(2007/10/03)
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- Synthesis of Symmetrical 2,2′,4,4′-Tetrasubstituted[4,4′-bioxazole]-5,5′(4H, 4′H)-diones and their Reactions with some Nucleophiles
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Several symmetrical 2,2′,4,4′-tetrasubslituted[4,4′-bioxazole]-5,5′(4H, 4′H)-diones 1a-f were obtained by dehydrodimerization of 5(4H)-oxazolones 2a-f. The configurations of four were established; one by X-ray crystallography rac-1c, and three rac-1a, meso-1a and rac-1b by 1H nmr spectroscopy of their derivatives. Upon being heated, the bioxazolones isomerized, presumably by breakage of the 4,4′-carbon-carbon bond to form free radicals followed by their recombination. The results of a crossover experiment were consistent with a radical nature for this isomerization reaction. Treatment of three of the bioxazolones rac-1a, mew-1a and rac-1c with methanol and amine nucleophiles led to ester and amide derivatives 7-11 of α,α′-dehydrodimeric amino acids.
- Andersen, Kenneth K.,Gloster, Daniel F.,Bray, Diana D.,Shoja, Massud,Kjaer, Anders
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p. 317 - 324
(2007/10/03)
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- Fluorescent properties of model chromophores of tyrosine-66 substituted mutants of Aequorea green fluorescent protein (GFP)
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In an ethanol-glass marix at 77 K, model compounds of the chromophores of recombinant GFP-Y66F, GFP-Y66W, and GFP-Y66H exhibited fluorescence properties close to those of the corresponding mutant proteins.
- Kojima, Satoshi,Ohkawa, Hiroko,Hirano, Takashi,Maki, Shojiro,Niwa, Haruki,Ohashi, Mamoru,Inouye, Satoshi,Tsuji, Frederick I.
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p. 5239 - 5242
(2007/10/03)
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- A Facile Preparation of 4-Arylidene-4,5dihydrooxazol-5-ones using Zeolite as a Cyclodehydrating Agent
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An efficient new method for the azlactonisation of acylamino acids using zeolite under mild conditions is described; the method is fairly general as well as providing high yields.
- Boruah, Anima,Baruah, Partha P.,Sandhu, Jagir S.
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p. 614 - 615
(2007/10/03)
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- Potent, selective tetrahydro-β-carboline antagonists of the serotonin 2B (5HT(2B)) contractile receptor in the rat stomach fundus
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A series of potent, selective 5HT(2B) receptor antagonists has been identified based upon yohimbine, with SAR studies resulting in a 1000-fold increase in 5HT(2B) receptor affinity relative to the starting structure (- log K(B)s > 10.0 have been obtained). These high-affinity tetrahydro-β- carboline antagonists are able to discriminate among the 5HT2 family of serotonin receptors, with members of the series showing selectivities of more than 100-fold versus both the 5HT(2A) and 5HT(2C) receptors based upon radioligand binding and functional assays. As the first compounds reported with such selectivity and enhanced receptor affinity, these tetrahydro-β- carboline antagonists are useful tools for elucidating the role of serotonin acting at the 5HT(2B) receptor in normal and disease physiology.
- Audia, James E.,Evrard, Deborah A.,Murdoch, Gwyn R.,Droste, James J.,Nissen, Jeffrey S.,Schenck, Kathy W.,Fludzinski, Pawel,Lucaites, Virginia L.,Nelson, David L.,Cohen, Marlene L.
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p. 2773 - 2780
(2007/10/03)
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- Synthesis of L-threo- and L-erythro-amino acids: novel probes for conformational analysis of peptide side chains
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An efficient and convenient route for the preparation of L-threo- and L-erythro-amino acids 5 as probes for the conformational analysis of peptide side chains by NMR spectroscopy is described.Stereoselective incorporation of deuterium into the α,β-positions of amino acid 5 was accomplished by catalytic deuteration of dehydroamino acid derivatives 1 and 2 followed by a combination of enzymic optical resilution and the racemization at the 2-position.Using these doubly labelled amino acids, it was possible to obtain vicinal coupling constants between carbonyl carbon and prochiral β-protons, J(13C-1Hβ1) and J(13C1-1Hβ2), through 13C NMR spectroscopy alone.We also demonstrate the determination of the fractional populations of rotamers in respect of the Cα-Cβ bond of the amino acids using the measured coupling constants.
- Oba, Makoto,Ueno, Ryuichi,Fukuoka, Mika,Kainosho, Masatsune,Nishiyama, Kozaburo
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p. 1603 - 1610
(2007/10/02)
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- A modified synthesis of (±)-β-aryllactic acids
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The synthesis of racemic forms of the reportedly active principle of Danshen, namely (±)-β-(3,4-dihydroxyphenyl)lactic acid [(±)3-(3,4-dihydroxyphenyl)-2-hydroxypropanoic acid] and its seven racemic derivatives is reported.
- Wong,Xu,Chang,Lee
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p. 793 - 797
(2007/10/02)
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- Synthesis of (S)-3,4-dihydroxyphenylalanine (L-DOPA) and unnatural α-amino acids via enzymatic resolution using alcalase
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Enzymatic resolution has been used for the synthesis of L-DOPA with high optical purity.N-Acetyl-(R,S)-3,4-methylenedioxyphenylalanine methyl ester (2b) on enzymatic resolution by alcalase (Subtilisin Carlsberg) yields N-acetyl-(S)-3,4-methylenedioxyphenylalanine (3b) which upon acid treatment affords (S)-3,4-dihydroxyphenylalanine (L-DOPA) (4).Several optically active unnatural N-acetylated and N-benzoylated α-amino acids have been prepared by similar enzymatic resolution.
- Tyagi, O D,Boll, P M,Parmar, V S,Taneja, Poonam,Singh, S K
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p. 851 - 854
(2007/10/02)
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