- A convenient synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones under solvent-assisted grinding
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A facile and effective approach for the synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones has been developed. Under solvent-assisted grinding in the presence of 2,4,6-trichloro-1,3,5-triazine, catalytic triphenylphosphine, and sodium carbonate, dehydrati
- Pattarawarapan, Mookda,Jaita, Subin,Phakhodee, Wong
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supporting information
p. 3171 - 3174
(2016/07/06)
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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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- Novel peptide mimetic inhibitors of hepatitis C serine protease derived from isomannide
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Hepatitis C (HCV) infection is a cause of chronic liver disease such as cirrhosis, carcinoma, or liver failure, and the current therapy is effective in only 50% of patients. Serine proteases, which are present in HCV, are the most studied class of proteolytic enzymes, and are a primary target in the drug development field. In this paper, we describe the synthesis and biological studies of a novel class of peptide mimetic compounds as potential HCV serine protease inhibitors. Georg Thieme Verlag Stuttgart.
- Barros, Thalita G.,Pinheiro, Sergio,Williamson, John S.,Tanuri, Amilcar,Pereira, Helena S.,Brindeiro, Rodrigo M.,Neto, Jose B. A.,Antunes, Octavio A. C.,Muri, Estela M. F.
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scheme or table
p. 620 - 626
(2009/06/28)
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- An efficient synthesis of new class of pyrazolo[3,4-b]pyridine-6-one derivatives by a novel cascade reaction
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(Chemical Equation Presented) A novel cascade reaction of 4-arylidene-2-phenyl-1,3-oxazol-5(4H)-one with 3-methyl-l-phenyl-1H-pyrazol-5- amine was described and a number of new pyrazolo[3,4-b]pyridine-6-one derivatives were synthesized. This new protocol has the advantages of shorter time, higher yields, and lower cost as well as easier operation.
- Shi, Feng,Zhang, Junyong,Tu, Shujiang,Jia, Runhong,Zhang, Yan,Jiang, Bo,Jiang, Hong
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p. 1013 - 1017
(2008/03/29)
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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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- Solid support Erlenmeyer synthesis of azlactones using microwaves
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A rapid and efficient protocol for the synthesis of azlactones is reported starting from acetyl/benzoylglycine and various aromatic aldehydes in the presence of acetic anhydride and sodium acetate in dry media using silica gel as solid support under microwave irradiation. The mild conditions, excellent yields, high purity. short reaction time and easy work-up are some of the major advantages of this method.
- Mogilaiah,Prashanthi,Reddy, Ch. Srinivas
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p. 2126 - 2128
(2007/10/03)
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- Study on dry-media microwave azalactone synthesis on different supported KF catalysts: Influence of textural and acid-base properties of supports
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Twenty-five inorganic solids studied as supports for KF were screened with respect to the synthesis of the azalactone obtained by dry-media condensation of p-hydroxybenzaldehyde with hippuric acid in acetic anhydride (1:1:4, molar ratio), in 3 g of 10 wt%
- Bautista, Felipa M.,Campelo, Juan M.,Garcia, Angel,Luna, Diego,Marinas, Jose M.,Romero, Antonio A.
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p. 227 - 234
(2007/10/03)
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- A convenient synthesis of 4-arylidene-2-phenyloxazol-5-ones catalyzed by KF-alumina
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A series of 4-arylidene-2-phenyloxzol-5-ones were synthesized by cyclodehydration-condensation of hippuric acid, aromatic aldehydes and acetic anhydride catalyzed by KF-Alumina.
- Wang, Yucheng,Shi, Daqing,Lu, Zaisheng,Dai, Guiyuan
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p. 707 - 712
(2007/10/03)
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- Synthesis of the marine alkaloid leucettamine B
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The marine natural product leucettamine B 2 has been prepared in good yield via two different routes, starting with glycine or with 3-methyl thiohydantoin, involving simple aldol condensation, and finally transamination of the thiohydantoin derivative.
- Roue, Nathalie,Bergman, Jan
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p. 14729 - 14738
(2007/10/03)
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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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- DIELS-ALDER REACTIONS OF AZLACTONES
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Azlactone 4 reacted with dienes to afford Diels-Alder adducts in good to excellent yields.
- Kraus, George A.,Yu, FuXiang
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p. 2401 - 2408
(2007/10/02)
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- Studies on Infrared Spectra of some Azalactones
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Infrared spectra of some 4-(p-substituted-benzylidene)-2-phenyl-5-oxazolones have been studied with reference to frequency of CN and C=O groups of the ring, which were not significantly influenced by variations of the para-substituent.
- Dhoubhadel, S. P.
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p. 757 - 758
(2007/10/02)
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