- Design, synthesis and antifungal activity of new schiff bases bearing 2-aminothiophene derivatives obtained by molecular simplification
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Seventeen Schiff bases bearing 2-aminothiophene derivatives were designed and synthesized using molecular simplification. The resulting compounds (4a-4q) were evaluated for their in vitro antifungal activity against dermatophytes. Prediction of their drug
- Luna, Isadora S.,Neves, Wendell W.,De Lima-Neto, Reginaldo G.,Albuquerque, Amanda P. B.,Pitta, Maíra G. R.,Rêgo, Moacyr J. B. M.,Neves, Rejane P.,Scotti, Marcus T.,Mendon?a, Francisco J. B.
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p. 1017 - 1029
(2021/05/19)
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- 6-Cinnamoyl-4-arylaminothienopyrimidines as highly potent cytotoxic agents: Design, synthesis and structure-activity relationship studies
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In this paper, we described the synthesis and cytotoxic activities of two new series of thieno[2,3-d]pyrimidine and thieno[3,2-d] pyrimidine derivatives. Most of the synthesized compounds had significant antiproliferative activities against PC3, MDA-MB-23
- Aghcheli, Ayoub,Bakhshaiesh, Tayebeh Oghabi,Esmaeili, Rezvan,Foroumadi, Alireza,Hasanvand, Zaman,Khalaj, Ali,Moghimi, Setareh,Nazeri, Elahe,Salarinejad, Somayeh,Toolabi, Mahsa
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supporting information
(2019/11/03)
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- HPK1 inhibitor and application thereof
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The invention belongs to the technical field of medicines, and specifically relates to an HPK1 inhibitor compound as shown in a formula (I) which is described in the specification or a pharmaceutically-acceptable salt and a stereoisomer of the HPK1 inhibi
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Paragraph 0272-0274
(2019/05/16)
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- Facile pathway for synthesis of two efficient catalysts for preparation of 2-aminothiophenes and tetrahydrobenzo[b]pyrans
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Abstract: We report here a new magnetically recyclable catalyst consisting of iron-substituted Keggin-type heteropolyacid (HPA) grafted on modified Fe3O4 nanoparticles. The synthesized hybrid nanomaterial exhibited the excellent catalytic efficiency in condensation reaction for the preparation of tetrahydrobenzo[b]pyrans under solvent-free conditions as well as in the synthesis of 2-aminothiophenes via Gewald reaction. It must be noted that, HPA supported magnetite nanoparticles catalyzed the preparation of tetrahydrobenzo[b]pyrans, whereas for Gewald reaction amine-functionalized magnetite nanoparticles acted as a catalyst. Different characterization techniques such as Fourier transform infrared (FT-IR), X-ray powder diffraction (XRD), field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM) and vibrating sample magnetometer (VSM) were used to characterize the hybrid nanomaterial. The reusability of catalyst was affirmed by using in consecutive runs for five times. Performance of prepared catalyst was compared with the various previously reported catalysts; the newly synthesized catalysts found to be most efficient with regard to reaction time, yield and ease of catalyst separation. Graphical Abstract: [Figure not available: see fulltext.].
- Saadati-Moshtaghin, Hamid Reza,Zonoz, Farrokhzad Mohammadi
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p. 2195 - 2213
(2017/12/18)
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- Ethylene diamine grafted nanoporous UiO-66 as an efficient basic catalyst in the multi-component synthesis of 2-aminithiophenes
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This study demonstrates ED-UiO-66 as a novel and effective solid nanoporous basic catalyst prepared through the amine grafting onto the pores of UiO-66. The manufactured nanoparticles were identified by FT-IR, XRD, TGA, FESEM, TEM, CHN and BET and the characterization results certified formation of a single phase nanoporous substance with the medium grain size less than 90?nm. The synthesized material was employed as an efficient catalyst for the preparation of 2-aminotiophenes through the Gewald method. This thermochemically stable nanocatalyst was environmentally safe, reusable and economic. Therefore, this methodology can be simply extended for industrial goals.
- Erfaninia,Tayebee,Dusek,Amini
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- A green chemical approach: a straightforward one-pot synthesis of 2-aminothiophene derivatives via Gewald reaction in deep eutectic solvents
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Abstract: The synergic effect of choline chloride/urea as a deep eutectic solvent was investigated in the synthesis of 2-aminothiophene derivatives via a three-component cyclocondensation of a ketone or an aldehyde with activated nitriles and elemental sulfur catalyzed by NaOH as cheap and highly accessible base. The advantages of this catalytic protocol are eco-friendly, easy to set up, reusability, and a simple separation and purification of products without using chromatography in high yields at short times. Graphical abstract: [Figure not available: see fulltext.]
- Shaabani, Ahmad,Hooshmand, Seyyed Emad,Afaridoun, Hadi
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p. 711 - 716
(2017/03/17)
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- TiO2/nanoclinoptilolite as an efficient nanocatalyst in the synthesis of substituted 2-aminothiophenes
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TiO2/nanoclinoptilolite (TiO2/NCP) was prepared by the mediation of hexadecyltrimethylammonium (HDTMA) as surfactant and used as an effective heterogeneous nanocatalyst for the preparation of substituted 2-aminotiophenes. The modified HDTMA/NCP was impregnated with titanium(IV) chloride solution followed by calcination at 500?°C for 20?h. The obtained nanocomposite was characterized using Fourier transform infrared spectroscopy, field emission scanning electron microscopy, inductively coupled plasma optical emission spectroscopy and X-ray diffraction. Moreover, the prepared nanocomposite had high stability and recoverability under mild and solvent-free conditions.
- Javadi, Farzad,Tayebee, Reza,Bahramian, Bahram
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- Optical properties of thiophene-containing liquid crystalline and hybrid liquid crystalline materials
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We report new mesogens made of thiophene and stilbene moieties as main building blocks that exhibit nematic and/or smectic phases. The liquid crystalline properties of their thiophene/azobenzene analogues have been found to be strongly suppressed compared to their thiophene/stilbene analogues. In twinned "bent-core" thiophene/azobenzene compound relatively strong fluorescence was found. A new hybrid material built of AuNPs coated with a thiophene-containing mesogenic ligand that forms a smectic phase is shown. In solutions of thiophene-mesogen coated AuNPs an unusual decrease of the ligand fluorescence decay rate was observed. Fluorescence lifetime increase is ascribed to two-point anchoring of ligand molecules resulting in molecule orientation tangential to the AuNP surface. UV-Visible absorption and fluorescence data of all synthesised compounds are presented. the Partner Organisations 2014.
- Romiszewski, Jerzy,Puterová-Tokarová, Zita,Mieczkowski, Jozef,Gorecka, Ewa
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supporting information
p. 2927 - 2934
(2014/07/07)
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- Easy single-step preparation of ZnO nano-particles by sedimentation method and studying their catalytic performance in the synthesis of 2-aminothiophenes via Gewald reaction
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Zinc oxide is a multi-purpose active material with important catalytic applications. In this study, nano-sized ZnO particles were easily synthesized through sedimentation of zinc acetate di-hydrate in absolute ethanol and were characterized by XRD and SEM. The XRD results indicated pure wurtzite structure with the average particle size of 26.9 nm for the nano-particles. It was observed that size of ZnO nano-particles was decreased while solution concentration was increased. This observation would be explained considering enhancing nucleation processes of nano-particles at high concentration of zinc acetate. The prepared nano-particles (2.5 mol%) were used as catalyst for the fast and efficient synthesis of 2-aminothiophenes under solvent free conditions. The three-component mixture of a carbonyl compound, malonodinitrile, and elemental sulfur was converted into the corresponding 2-aminothiophene in moderate to high yields with excellent selectivity.
- Tayebee, Reza,Javadi, Farzad,Argi, Gholamreza
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- KG-60-piperazine as a new heterogeneous catalyst for gewald three-component reaction
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Piperazine supported on amorphous silica (KG-60-piperazine) as a basic catalyst acts in the Gewald three-component reaction of some aldehydes and ketones with malononitrile as well as ethyl cyanoacetate. The catalyst shows general utility with a variety of starting carbonyl compounds. Moreover, the catalyst can be reused for four additional cycles without significant loss of the activity. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications to view the free supplemental file.
- Rezaei-Seresht, Esmail,Tayebee, Reza,Yasemi, Mohammad
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p. 1859 - 1864
(2013/05/21)
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- An efficient synthesis of 2-aminothiophenes via the gewald reaction catalyzed by an N-methylpiperazine-functionalized polyacrylonitrile fiber
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A new N-methylpiperazine-functionalized polyacrylonitrile fiber has been developed to catalyze the Gewald reaction between 2,5-dihydroxy-1,4-dithiane and activated nitriles to afford 3-substituted 2-aminothiophenes in good to excellent yields (65-91%). Low catalyst loading (8.0 mol%), simple procedure, high yields, excellent recyclability, and reusability (up to 10 times with minimal loss of catalytic activity) are attractive features of this fiber catalyst. Georg Thieme Verlag Stuttgart · New York.
- Ma, Lichao,Yuan, Liwei,Xu, Changzhu,Li, Guowei,Tao, Minli,Zhang, Wenqin
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- NOVEL ANTI-CANCER COMPOUNDS
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The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R0, R1, R2, A, and X have defined meanings as described in claim 1.
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Page/Page column 44; 45
(2014/01/09)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 45-46
(2011/10/05)
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- Tunable spectroscopic and electrochemical properties of conjugated push-push, push-pull and pull-pull thiopheno azomethines
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Novel azomethines consisting uniquely of thiophene units were examined. The highly conjugated compounds were prepared by condensing air stable aminothiophenes with 2-thiophene aldehydes, which were substituted with various electronic groups. The resulting azomethines are highly conjugated and are both reductively and hydrolytically resistant. Various electron donating and accepting groups placed in the 2-position of 5-thiophene carboxaldehyde lead to electronically delocalized push-push, pull-pull, and push-pull azomethines. These electronic groups affect both the HOMO and the LUMO levels, which influence the absorption and emission spectra. Colors spanning the entire visible spectrum ranging from yellow to blue are possible with these nitrogen containing conjugated compounds. Excited state deactivation of the singlet excited state occurs predominately by internal conversion while only a small amount of energy is dissipated by intersystem crossing to the triplet state and by fluorescence. The ensuing fluorescence and phosphorescence of the thiopheno azomethines are similar to those of their thiophene analogues currently used in functional devices, but with the advantage of a low triplet state and tunable HOMO-LUMO energy levels extending from 3.0 to 1.9 eV. Quasi-reversible electrochemical radical cation formation is possible while the oxidation potential is dependent on the nature of the electronic group appended to the thiophene. The crystallographic data of the electronic push-push system show the azomethine bonds are planar and linear and they adopt the E isomer. The Royal Society of Chemistry 2007.
- Dufresne, Stephane,Bourgeaux, Marie,Skene
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p. 1166 - 1177
(2008/02/11)
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- Microwave-assisted synthesis of 2-aminothiophene-3-carboxylic acid derivatives, 3H-thieno[2,3-d]pyrimidin-4-one and 4-chlorothieno[2,3-d]pyrimidine
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A two-minute microwave irradiation allowed the synthesis of several 2-aminothiophene-3-carboxylic acid derivatives. Their efficient transformation to thieno[2,3-d]pyrimidin-4-one and the corresponding 4-chloro derivative is also reported under microwave irradiation.
- Hesse, Stéphanie,Perspicace, Enrico,Kirsch, Gilbert
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p. 5261 - 5264
(2008/02/08)
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- Synthesis of 4-amino-5,6,7,8-tetrahydrothieno[2,3-b]quinolin-5-ol derivatives
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(Chemical Equation Presented) This paper describes the synthesis of 4-amino-5,6,7,8-tetrahydrothieno[2,3-b]quinolin-5-ol derivatives (3a-h) and 4-amino-5,6,7,8-tetrahydrothieno[2,3-b]quinoline (8a) in good yield by three-step procedures starting from 2-am
- Song, Yang-Heon,Seo, Jinmoo
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p. 1439 - 1443
(2008/09/18)
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- Cyanothiophene derivatives, compositions containing such compounds and methods of use
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The present invention addresses substituted cyanothiophene derivatives of the formula I: as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose providing a treatment of diabetes.
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- Novel Compounds
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The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
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- Thienopyrimidine derivatives
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4-Substituted-thieno[2,3-d], [3,2-d], and [3,4-d]pyrimidines having fungicidal, insecticidal, and miticidal utility are disclosed. Related 3-substituted-thieno[2,3-d], [3,2-d], and [3,4-d]pyrimidin-4-(3H)-imines are useful as fungicides, insecticides, and
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