- Synthesis and properties of a series of iridium complexes with imidazolo[2,1-b]thiazole derivatives as primary ligands
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3-Methyl-6-phenylimidazo[2,1-b]thiazole (mpmt) and 3-methyl-6-(4-(trifluoromethyl)phenyl)imidazo[2,1-b]thiazole (mtfpmt) were easily prepared from thiourea, acetone (or trifluoroacetone), and α-bromoacetophenone as novel primary ligands. These were used to synthesize ten phosphorescent iridium complexes with picolinate (pic), isoquinoline-5-carboxylic acid (3-IQA), quinoline-2-carboxylic acid (2-QA), phenyl isoquinoline (piq), and 1,4-difluorophenyl pyrimidine (dfppy) as ancillary ligands. Their structures, photoluminescence, and electrochemistry were investigated. The introduction of trifluoromethyl groups at the phenyl ring of mpmt and to mtfpmt blue shifts the emission spectra of Ir3+ complexes by about 50 nm, and the corresponding emission peaks in CH2Cl2, which shifted from 545 to 613 nm, were observed at room temperature with an increase in the corresponding internal quantum efficiencies (IQEs) from 5.8% to 31.6%. Constructed with title complexes as emitters, LED chips based on InGaN chip excitation show good performances. Particularly, a device based on (mpmt)2Ir(2-QA) showed the best red light emission with a CIE (0.64, 0.30), a CRI of 72.0, and a color purity that was over 80%. Also, a device based on (mpmt)2Ir(3-IQA) provided a maximum luminescence efficiency of 3.01 lm W?1. These results suggest that the title complexes have potential applications in LED chips and OLEDs.
- Yin, Xin-ying,Yang, Zhi-yu,Huang, Guo-li,Bian, Jian-jian,Wang, Deng-qiang,Wang, Qin,Teng, Ming-yu,Wang, Zheng-liang,Zhang, Jie
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- Inhibitory effect of 2-aminothiazole derivatives in oxidation reactions
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The kinetics and mechanism of inhibitory effect of 2-aminothiazole derivatives in the radical-initiated oxidation of cumene were studied.
- Karpov,Pekarevskii,Potekhin
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Read Online
- Nanochitosan: A biopolymer catalytic system for the synthesis of 2-aminothiazoles
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A convenient and efficient method is described for the synthesis of 2-aminothiazoles by one-pot reaction of ketone and thiourea using chitosan nanoparticles under mild condition. Nanochitosan was used as a biodegradable and green catalyst for this reaction in satisfactory yields. The attractive advantages of the present process include easy isolation of products, milder and cleaner conditions, higher purity and yields and easier work-up procedure.
- Safari, Javad,Abedi-Jazini, Zahra,Zarnegar, Zohre,Sadeghi, Masoud
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Read Online
- N,O π-Conjugated 4-Substituted 1,3-Thiazole BF2 Complexes: Synthesis and Photophysical Properties
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A series of 1,3-thiazole-based organoboron complexes has been designed and synthesized by acylation of 2-amino 4-subsituted 1,3-thiazoles with (4-dimethylamino)benzoyl chloride and the subsequent BF2 complexation reaction. The influence of substituents in position 4 of the thiazole ring on photophysical properties of the complexes has been investigated. Synthesized thiazolo[3,2-c][1,3,5,2]oxadiazaborinines mainly showed intensive fluorescence in solutions. Complex with a 4,5-unsubstituted thiazole unit demonstrated an aggregation induced emission (AIE) effect and a very high fluorescent quantum yield (94%) in the solid state because of the inhibition of π-π/π-n interactions in the molecular packing.
- Potopnyk, Mykhaylo A.,Lytvyn, Roman,Danyliv, Yan,Ceborska, Magdalena,Bezvikonnyi, Oleksandr,Volyniuk, Dmytro,Gra?ulevi?ius, Juozas Vidas
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- Biocidal and anticorrosive effect of 2-aminothiazole derivatives used as additives to jet fuels
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The effect of 2-aminothiazole derivatives on the biological resistance and corrosion activity of jet fuels was studied under conditions of water condensation.
- Karpov,Nazarenko,Pekarevskii,Potekhin
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Read Online
- Design and synthesis of new 4-methylthiazole derivatives: In vitro and in silico studies of antimicrobial activity
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The development of resistance against antimicrobial drugs has become a world-wide issue. It is predicted that some or perhaps all the antimicrobial drugs used in clinics will be out of the treatment protocols soon. Therefore, researchers pay more attention to the development of new antimicrobial drugs. For this purpose, we designed and synthesized new 4-methylthiazole-(benz)azole derivatives. The structural elucidation of the compounds was performed by 1H-NMR, 13C-NMR, HSQC, NOESY, HMBC and LC/MS-IT-TOF spectral and elemental analyses. Then, their antimicrobial activity against bacteria and fungi strains was tested. The antibacterial effect of the compounds was found valuable as compared with their anticandidal activity. By combining the findings with molecular docking results, structure-activity relationship (SAR) was explained. Thus, in the development of new antimicrobial agents which can be used as DNA gyrase inhibitors, SAR showed that the products might be used in the discovery of new antimicrobials where their activity is owed to the allosteric effect. Although the effect of compound 3f was modest compared to the reference compound, it was better than the other synthesized compounds. Also, compound 3f has a better allosteric effect and might be a good lead candidate to synthesize new and better active hits. In addition, it was observed that all the synthesized compounds showed half potency against P. aeruginosa compared to the reference drug. On the other hand, no significant difference was seen between compounds against gram-positive or gram-negative bacteria. Briefly, meaningful data to correlate the SAR with thiazole-(benz)azole hybridized compounds were presented in this study. In future projects, the mentioned ideas can be used to synthesize new compounds having better antibacterial activity, particularly against resistant organisms.
- DAWBAA, Sam,EVREN, Asaf Evrim,GüL, ülküye Dudu,NUHA, Demokrat,YAVUZ, ?ule Aybüke,YURTTA?, Leyla
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- Aiding the versatility of simple ammonium ionic liquids by the synthesis of bioactive 1,2,3,4-tetrahydropyrimidine, 2-aminothiazole and quinazolinone derivatives
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Simple ammonium ionic liquids [ILs] are efficient, green, environmentally friendly catalysts in promoting the Biginelli condensation reaction, Hantzsch reaction and Niementowski reaction to afford 1,2,3,4-tetrahydropyrimidine, 2-aminothiazole and quinazolinone derivatives respectively by eliminating the need for harmful volatile organic solvents. These [ILs] are air and water stable, easy to prepare and cost-effective. The effects of the anions and cations present in [IL] on reactions were investigated. The results clearly indicated that the Biginelli condensation reaction, Hantzsch reaction and Niementowski reaction were heavily influenced by the acidity of [IL], and among various ammonium ionic liquids, [Et3NH][HSO4] showed the best catalytic activity. Furthermore, [IL] could be easily separated and reused with a slight loss of its activity. This technique provided a good alternative way for the industrial synthesis of 1,2,3,4-tetrahydropyrimidinones, 2-aminothiazoles and quinazolinones. The present processes are eco-friendly methods for the synthesis of these derivatives authenticated by several green parameters, namely,E-factor, process mass intensity, reaction mass efficiency, atom economy, and carbon efficiency.
- Kakati, Praachi,Singh, Preeti,Yadav, Priyanka,Awasthi, Satish Kumar
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p. 6724 - 6738
(2021/04/22)
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- Synthesis and photoelectric properties of IrIIIcomplexes using fluorobenzylimidazole[2,1-b]thiazole derivatives as primary ligands
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3-Methyl-6-(3,5-difluorophenyl)imidazo[2,1-b]thiazole (mdfpit) and 3-methyl-6-(3,4,5-trifluorophenyl)imidazo[2,1-b]thiazole (mtfpit) were easily prepared from thiourea, acetone, and 3,5-difluorobenzoyl bromide or 3,4,5-trifluorobenzoyl bromide. These were used as primary ligands to synthesize twelve phosphorescent IrIIIcomplexes with picolinic acid (pic), isoquinoline-3-carboxylic acid (3-IQA), quinoline-2-carboxylic acid (2-QA), 2-(pyridin-2-yl)phenol (2-ylppy), 2-(2,4-difluorophenyl)pyridine (dfppy), and pyridine-2-sulfonic acid (2-sappy) as auxiliary ligands. Their structures, photoluminescence, and electrochemical properties were investigated. Upon introducing more fluorine atoms into the benzene ring of the primary ligand, the thermal stability, photoluminescence quantum yield (PLQY), LUMO energy level, and luminous efficiency of the resulting IrIIIcomplexes are significantly improved, and the photoluminescence emission spectra are blue-shifted. Their maximum emission wavelengths are present in the range of 517-618 nm, and the luminous colors span from the green to red light region. Using the synthesized IrIIIcomplexes as emitters, LED chips based on InGaN chip excitation were developed, which showed good performances. Among all LEDs, the PLQY of the (mtfpmt)2Ir(pic) based LED is 58.4%, and the luminous efficiency is as high as 17.11 lm W?1; the luminous efficiency of the (mdfpmt)2Ir(2-QA) based LED is 3.41 lm W?1with CIE coordinates of 0.60 and 0.38, which are very similar to the saturated standard red light emission. The results demonstrate the potential of the studied IrIIIcomplexes as candidates for LED materials.
- Liu, Xiao-Qing,Rong, Mei-Zhu,Si, Peng-Bin,Teng, Ming-Yu,Wang, Qin,Wang, Yu-Fei,Wang, Zheng-Liang,Zhang, Jie,Zhe, Hai-Feng,Zhou, Ai-Hui
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p. 18796 - 18804
(2021/10/26)
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- Synthesis of 6-membered-ring fused thiazine-dicarboxylates and thiazole-pyrimidines via one-pot three-component reactions
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A facile and efficient one-pot three-component reaction method for the synthesis of thiazine-dicarboxylates is reported. Reaction of an isocyanide and dialkyl acetylenedicarboxylate with 2-amino-4H-1,3-thiazin-4-one derivatives containing both an acidic proton and an internal nucleophile gave the products in good yields of 76–85%. The reactivity of dialkyl acetylenedicarboxylates was further tested in the synthesis of thiazole-pyrimidines where a two-component reaction of 2-aminothiazole with dialkyl acetylenedicarboxylates was successfully converted to a more efficient three-component reaction of a thiourea, α-haloketone and dialkyl acetylenedicarboxylate (DMAD/DEtAD) to give thiazole-pyrimidines in good yields of 70–91%.
- Bode, Moira L.,Coyanis, Elena Mabel,Fernandes, Manuel A.,Fish, Muhammad Q.,Mohlala, Reagan L.
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- Iridium complex with 3-methyl-6-phenylimidazole[2, 1-b]thiazole derivative as main ligand
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The invention discloses ten iridium (III) complexes, which are characterized in that: the main ligands of the complexes are 3-methyl-6-phenylimidazole[2, 1-b]thiazole (mpmt) and 3-methyl-6-(4-(trifluoromethyl)phenyl)imidazo[2, 1-b]thiazole (mtfpmt) respectively, and the auxiliary ligands are 2-picolinic acid (pic), isoquinoline-3-formic acid (3-IQA), quinoline-2-carboxylic acid (2-QA), 1-phenylisoquinoline (piq) and 2-(2, 4-difluorophenyl)pyridine (dfppy) respectively, and the structures are shown as the specification, wherein the definition of X substituent group is selected from one of twogroups of complexes. Light-emitting diodes prepared from the complexes have a maximum emission wavelength of 540.3-627.8nm and light-emitting efficiency of 0.18-3.01 lm.W, wherein (mtfpmt)2Ir(pic)emits pure green light, and (mpmt)2Ir(2-QA) emits pure red light, and the color purity is high. near white light can be obtained after mixing of the light emitted by (mtfpmt)2Ir(dfppy) and a galliumnitride chip, therefore the complexes can be used for making of white light LED. Excellent performance of the devices indicates that the complexes have application value in preparation of organic photoluminescent and electroluminescent devices. The invention discloses a structure and a synthesis method of the complexes, and a structure and a preparation method of organic photoluminescent devices.
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Paragraph 0029-0031
(2020/03/12)
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- A process for the preparation method of thiabendazole
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The invention relates to a new method for synthesizing thiabendazole. Acetone and chlorine are taken as starting materials to synthesize chloroacetone, chloroacetone not subjected to separation can directly react with thiocarbamide to obtain 2-Amino-4-methylthiazole which is subjected to diazotization to obtain 4-methylthiazole, and 4-methylthiazole is oxidized to produce 4-thiazolecarboxylic acid, and finally, 4-thiazolecarboxylic acid reacts with o-phenylenediamine to obtain the target object thiabendazole. The thiabendazole is a broad-spectrum anthelmintic, can repel roundworms, hookworms, whipworms, pinworms, strongyloises stercoralis and trichinization, is also a broad-spectrum efficient disinfectant and is widely used as a fruit fresh-keeping agent and a bactericidal mildew inhibitor in various fields over the past decade in China.
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Paragraph 0055; 0058; 0059
(2018/04/01)
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- C[sbnd]N bond formation in alicyclic and heterocyclic compounds by amine-modified nanoclay
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In the current protocol, amine functionalized montmorillonite K10 nanoclay (NH2-MMT) was applied to catalyze the formation of C[sbnd]N bonds in the synthesis of azines and 2-aminothiazoles at room temperature. In comparison with the current methods of C[sbnd]N bond formation, this approach displays specific advantages include atom economy, clean conversion, design for energy efficiency, the use of nontoxic and heterogeneous catalyst, higher purity and yields, safer solvent and reagents for this organic transformation.
- Zarnegar, Zohre,Alizadeh, Roghayeh,Ahmadzadeh, Majid,Safari, Javad
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- Carbon tetrabromide mediated oxidative cyclocondensation of ketones and thioureas: An easy access to 2-aminothiazoles
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A simple, mild, and efficient one-pot method for the synthesis of substituted 2-aminothiazoles has been reported. The reaction involves the formation of sulfenyl bromide as an umpolung intermediate of nucleophilic sulfur, which is responsible for C-S bond formation leading to oxidative cyclization of ketones and thioureas to furnish the desired products. Carbon tetrabromide was used as a convenient and mild brominating reagent under basic condition at room temperature to give 2-aminothiazoles in good to excellent yields.
- Keshari, Twinkle,Kapoorr, Ritu,Yadav, Lal Dhar S.
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supporting information
p. 5623 - 5627
(2015/09/21)
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- Synthesis of 2-aminothiazole derivatives from easily available thiourea and alkyl/aryl ketones using aqueous NaICl2
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A simple methodology was developed to synthesize substituted aminothiazoles from the corresponding thiourea and substituted ketones using aqueous NaICl2 at reflux temperature in THF. The products were obtained in good to excellent yields.
- Ghodse, Shrikant M.,Telvekar, Vikas N.
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p. 472 - 474
(2015/03/05)
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- Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors
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Novel series of N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides were discovered as potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitors. SAR studies of the RORγt HTS hit 6a led to identification of thiazole ketone amide 8h and thiophene ketone amide 9g with high binding affinity and inhibitory activity of Th17 cell differentiation. Compound 8h showed in vivo efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models via oral administration.
- Wang, Yonghui,Cai, Wei,Zhang, Guifeng,Yang, Ting,Liu, Qian,Cheng, Yaobang,Zhou, Ling,Ma, Yingli,Cheng, Ziqiang,Lu, Sijie,Zhao, Yong-Gang,Zhang, Wei,Xiang, Zhijun,Wang, Shuai,Yang, Liuqing,Wu, Qianqian,Orband-Miller, Lisa A.,Xu, Yan,Zhang, Jing,Gao, Ruina,Huxdorf, Melanie,Xiang, Jia-Ning,Zhong, Zhong,Elliott, John D.,Leung, Stewart,Lin, Xichen
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supporting information
p. 692 - 702
(2014/01/23)
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- Synthesis, characterization and antimicrobial studies of a few novel thiazole derivatives
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A series of novel N-[4-(substituted)-1,3-thiazol-2-yl]-2-(substituted) acetamide (9a-m) and methyl 2-(2-(2-(substituted)acetamido)thiazol-4-yl)acetate (9n-o) derivatives have been synthesized and compounds were characterised by spectral and analytical studies. All compounds were screened for their in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumonia by disc diffusion method and for antifungal activity against Penicillium marneffei, Trichophyton mentagrophytes, Aspergillus flavus and Aspergillus fumigatus by serial plate dilution method. Compounds 9b, 9e, 9m and 9o exhibited growth inhibition against all the tested bacterial strains, with MIC values varying from 12.5 to 6.25 μg/ml. Among the compounds tested for antifungal activity, 9a, 9b, 9d, 9j, 9k, 9p and 9n showed wide range of activity against all the tested strains. Most of the newly synthesized compounds were effective against fungal strains rather than bacterial strains. However, some of the compounds like 9a, 9e, 9j, 9k and 9i showed selective sensitivity against some of the bacterial strains whereas they were unable to sustain the growth of other strains.
- Praveen, Aletti S.,Yathirajan, Hemmige S.,Narayana, Badiadka,Sarojini, Balladka K.
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p. 259 - 268
(2014/03/21)
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- NOVEL TRIAZINE COMPOUNDS
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The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/ or the mTOR pathway.
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Page/Page column 60
(2012/08/08)
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- Ligand-free copper-catalyzed regioselective C-2 arylation of imidazo[2,1-b]thiazoles
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An effective, regioselective C-2 arylation of imidazo[2,1-b]thiazoles catalyzed by Cu(I) has been developed. This arylation proceeded smoothly without promotion of the ligands, and various functional (22 samples) groups were well tolerated. Preliminary mechanistic studies of this arylation are also reported.
- Huang, Guoli,Sun, Hongsheng,Qiu, Xiaojie,Jin, Can,Lin, Chen,Shen, Yingzhong,Jiang, Juli,Wang, Leyong
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supporting information; experimental part
p. 5224 - 5227
(2011/12/04)
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- Domino alkylation-cyclization reaction of propargyl bromides with thioureas/thiopyrimidinones: A new facile synthesis of 2-aminothiazoles and 5H-thiazolo[3,2-α]pyrimidin-5-ones
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A new synthesis of 2-aminothiazoles and 5H-thiazolo[ 3,2-α]pyrimidin- 5-ones was developed as a domino alkylation-cyclization reaction of propargyl bromides with thioureas and thiopyrimidinones, respectively. Domino reactions were performed under microwave irradiation leading to desired compounds in a few minutes and high yields. Georg Thieme Verlag Stuttgart.
- Castagnolo, Daniele,Pagano, Mafalda,Bernardini, Martina,Botta, Maurizio
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experimental part
p. 2093 - 2096
(2011/04/15)
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- Synthesis and biological activity evaluation of 1,2,3-thiadiazole derivatives as potential elicitors with highly systemic acquired resistance
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Elicitors provide a broad spectrum of systemic acquired resistance by altering the physical and physiological status of the host plants and, therefore, are among the most successful directions in modern pesticide development for plant protection. To develop a novel elicitor with highly systemic acquired resistance, two series of thiazole- and oxadiazole-containing thiadiazole derivatives were rationally designed and synthesized according to the principle of combination of bioactive substructures in this work. Their structures were characterized by 1H nuclear magnetic resonance (NMR), infrared (IR), high-resolution mass spectrometry (HRMS), or elemental analysis. Their potential systemic acquired resistance as an elicitor was also evaluated; bioassay results indicated that, among the 23 compounds synthesized, three compounds, 10a, 10d, and 12b, displayed better systemic acquired resistance than the positive control, tiadinil, a commercialized 1,2,3-thiadiazolebased elicitor. In addition, three other compounds, 10f, 12c, and 12j, exhibited a certain degree of fungus growth inhibition In vitro or In vivo. Our results demonstrated that, in combination of bioactive substructures is an interesting exploration for novel pesticide development, thiazole-and oxadiazole-containing thiadiazole derivatives are potential elicitors with good systemic acquired resistance.
- Fan, Zhijin,Shi, Zugui,Zhang, Haike,Liu, Xiufeng,Bao, Lili,Ma, Lin,Zuo, Xiang,Zheng, Qinxiang,Mi, Na
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experimental part
p. 4279 - 4286
(2010/06/16)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- One-pot synthesis of 2-aminothiazoles using supported reagents
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A simple and efficient method has been developed for the synthesis of 2-aminothiazoles from α-bromo ketones in one-pot using a supported reagents system, KSCN/SiO2-RNH3OAc/Al2O3, in which α-bromo ketone reacts first with KSCN/SiO2 and the product, α-thiocyano ketone, reacts with RNH3OAc/Al2O3 to give the final product, 2-aminothiazole, in high yield.
- Kodomari, Mitsuo,Aoyama, Tadashi,Suzuki, Yoshitada
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p. 1717 - 1720
(2007/10/03)
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- Thiazole, imidazole and oxazole compounds and treatments of disorders associated with protein aging
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Provided are, among other things, compounds of formula I or IA, . Also provided are methods of treatment with such compounds.
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- Method for treating glaucoma IIB
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Provided is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing amount or ocular accommodation improving amount of a compound of the formula I or IA, wherein J is oxygen, sulfur, or N—Rd.
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- Kinetics of reaction of chloroacetone with thioureas
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The second order rate constants for the reactions of chloroacetone with thiourea, phenylthiourea and p-substituted phenylthioureas have been evaluated in ethanol medium. The rate of reaction is first order with respect to chloroacetone and first order with respect to thioureas. The effect of substituents on the rate of reaction is also studied. Thermodynamic parameters are used to explain the nature of reaction. Possible mechanism for the reaction is suggested.
- Zaware,Mane,Ingle
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p. 213 - 214
(2008/04/18)
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- Condensation of thiourea derivatives with carbonyl compounds: One-pot synthesis of N-alkyl-1, 3-thiazol-2-amines and of 3-alkyl-1, 3-thiazolimines
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The reactions of ketones and AT-substituted thioureas, in the presence of HC1 (or HBr) and DMSO afford mixtures of the title compounds which are easily separated on a silica gel column. This method avoids the classical use of a-haloketones. The mechanism of these reactions involves the enolization of ketones and the activation of thiourea sulfur, probably by oxygen transfer from DMSO.
- Boga, Carla,Forlani, Luciano,Silvestroni, Cristian,Corradi, Anna Bonamartini,Sgarabotto, Paolo
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p. 1363 - 1368
(2007/10/03)
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- A novel thiazolium type peptide coupling reagent for hindered amino acids
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A highly efficient coupling reagent, 2-bromo-3-ethyl-4-methyl thiazolium tetrafluoroborate (BEMT), was designed, synthesized and successfully applied to the synthesis of oligopeptides containing N-alkyl or α-C-dialkyl amino acids. Its efficiency was evaluated by HPLC and 1H NMR methods, and demonstrated by synthesis of a number of N-methyl-rich peptide segments with good yields and negligible racemization. The mechanism of coupling was studied by HPLC, 1H NMR and IR monitoring; it is proposed that labile (acyloxy)thiazolium salts and N-protected amino acid bromides were the major active intermediates with concomitant formation of N-ethyl-4-methyl thiazolidones and a small amount of oxazolones and N-protected amino acid anhydrides.
- Li, Peng,Jie, Cheng Xu
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p. 8301 - 8304
(2007/10/03)
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- Synthesis of 2-(aminoacetylamino)thiazole derivatives and comparison of their local anaesthetic activity by the method of action potential
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Some numbers of the family of 2-(aminoacetylamino)thiazoles were synthesized. The structure of these compounds was identified both by elemental as well as by spectroscopic analysis (UV, IR, H-NMR, MS). The possible local anaesthetic action of these compounds was also tested using the sciatic nerve of the frog. None of the tested compounds were found to have local anaesthetic action on in vitro preparations as lidocaine, but one of the compounds showed a similar anaesthetic action to procaine.
- Geronikaki,Theophilidis
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p. 709 - 716
(2007/10/02)
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- Formation of Thioamide Derivatives from Reactions of Isothiocyanates with Oxazol-2-amines
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4-Substituted oxazol-2-amines react with isothiocyanates to give products having a thioamide function at C5.The reaction is considered to be an electrophilic process in competition with the usual reaction of the amino group with the isothiocyanate.The nature of the isothiocyanate and the type of substituent at C4 affect the amount of the thioamide product formed.Some chemical properties of the thioamides are also investigated.
- Crank, George,Khan, Humaid R.
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p. 447 - 458
(2007/10/02)
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- Protection of Primary Amines as N-Substituted 2,5-Dimethylpyrroles
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Protection of primary amine group is achieved by incorporating it into an N-substituted 2,5-dimethylpyrrole system.The method affords protection against strong bases and nucleophiles, heating with concentrated alkali, standard mineral acid work-up conditions, and various other reagents.Phenyl-, pyridil-, thiazolyl-, and alkyl-amines have been studied.All give trisubstituted pyrroles in high yield (>80percent) by reaction with hexane-2,5-dione.The pyrroles from the first three types are stable to storage; even the N-alkyl compounds can be used without difficulty.Regeneration of the amine group, by treatment with hydrxylamine hydrochloride, is efficient (80percent yield) with the phenyl, pyridyl, and alkyl compounds but less satisfactory (60 - 65percent generally but down to 25percent in two cases) with the thiazolyl derivatives.
- Bruekelman, Stephen P.,Leach, (Miss) Susan E.,Meakins, G. Denis,Tirel, Malcolm D.
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p. 2801 - 2807
(2007/10/02)
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- Protection of Primary Amines as N-Substituted 2,5-Dimethylpyrroles
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Protection of a primary amine group against attack by organic or aqueous solutions of strong bases or nucleophiles is achieved by incorporation into an N-substituted 2,5-dimethylpyrrole system from which the amine group is regenerated by treatment with hydroxylamine hydrochloride.
- Breukelman, Stephen P.,Meakins, G. Denis,Tirel, Malcolm D.
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p. 800 - 801
(2007/10/02)
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- An Infrared Study of Rotational Isomerism in Thiazole-2-carboxylates
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A series of alkyl thiazole-2-carboxylates containing a range of substituents at the 4- and 5-positions has been prepared.Solutions of these esters (mostly new compounds) show well resolved doublets in the i.r.C=O region which arise from rotational isomers.The higher wavenumber components are assigned to the more polar carbonyl O,S-anti-s-trans-rotamers and the lower wavenumber components to the carbonyl O,S-syn-s-trans-forms.Small, but systematic, differences between the methyl esters are noted.
- Kaye, Perry T.,Meakins, G. Denis,Willbe, Charles,Williams, Peter R.
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p. 2335 - 2339
(2007/10/02)
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