- Synthesis of E-stilbene azomethines as potent antimicrobial and antioxidant agents
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A series of new extensively conjugated E -stilbene azomethines (5a–5h) were synthesized and screened for their antioxidant and antimicrobial activity. The compounds were tested against bacterial (Escherichia coli, Staphylococcus aureus, Klebsiella pneumon
- Iqbal, Ahsan,Khan, Zulfiqar Ali,Shahzad, Sohail Anjum,Usman, Muhammad,Khan, Shakeel Ahmad,Fauq, Abdul H.,Bari, Ayesha,Sajid, Muhammad Aamir
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Read Online
- Synthesis and evaluation of antitumor activity of dibenzodiazepine derivatives
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Abstract: A series of dibenzodiazepine 2-position derivatives, bearing N-methylpiperazine at the C-11 position, were prepared by using a concise approach. Their inhibitory activities of tumor cell proliferation in vitro were tested in five cell lines, including breast cancer cell BCAP37, gastric cancer cell SGC7901, liver cancer cell HepG2, cervical cancer cell HeLa and acute promyelocytic leukemia cell HL-60. Several compounds showed efficient tumor activity with IC50 values down to 0.30?μM. These compounds are expected to be a new class of potential anticancer lead compounds. Graphic abstract: [Figure not available: see fulltext.]
- Cao, Ke,Yan, Jianwei,Yan, Fulin,Yin, Tiantian
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- Synthesis and antiproliferative activity of substituted benzopyranoisoindoles: A new class of cytotoxic compounds
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A series of novel aminosubstituted benzopyranoisoindoles possessing structural analogy to an active nitracrine metabolite are reported. The compounds exhibited interesting cytotoxic activity against a panel of cell lines, which was maximized by the presen
- Hadjipavlou, Christiana,Kostakis, Ioannis K.,Pouli, Nicole,Marakos, Panagiotis,Pratsinis, Harris,Kletsas, Dimitris
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- Synthesis, spectroscopic and computational evaluation of a xanthene-based fluorogenic derivatization reagent for the determination of primary amines
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To detect an analyte, typically at the sub-nanomolar scale, extremely sensitive analytical tools are required. Fluorescence is the spectroscopy of choice to achieve such a level due to its non-invasive nature and efficiency in accurately probing the sub-n
- Barnoin, Guillaume,Burger, Alain,Dotsikas, Yannis,Gikas, Evagelos,Kalampaliki, Amalia D.,Kostakis, Ioannis K.,Le, Hoang-Ngoan,Mallick, Suman,Michel, Beno?t Y.,More, Yogesh W.,Vincent, Steve
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- Synthesis, modeling studies and evaluation of E-stilbene hydrazides as potent anticancer agents
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A group of new thermodynamically more stable E-2-styrylbenzohydrazide derivatives (5a-i) were synthesized via palladium catalyzed Mizoroki-Heck reaction conditions. All synthesized compounds were characterized by UV-visible, FT-IR, 1H NMR, sup
- Iqbal, Ahsan,Khan, Zulfiqar Ali,Shahzad, Sohail Anjum,Ahmad Khan, Shakeel,Raza Naqvi, Syed Ali,Bari, Ayesha,Amjad, Hira,Umar, Muhammad Ihtisham
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Read Online
- Preparation of Functionalized Diorganomagnesium Reagents in Toluene via Bromine or Iodine/Magnesium-Exchange Reactions
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A wide range of polyfunctionalized di(hetero)aryl- and dialkenyl-magnesium reagents are prepared in toluene within 10 to 120 minutes between 78 C and 25 C via an I/Mg- or Br/Mg-exchange reaction using reagents of the general formula R2Mg (R = sBu, Mes). Highly sensitive functional groups, such as triazene or nitro, are tolerated in these exchange reactions, enabling the synthesis of various functionalized (hetero)arene and alkene derivatives after quenching with several electrophiles including allyl bromides, acyl chlorides, aldehydes, ketones, and aryl iodides.
- Desaintjean, Alexandre,Danton, Fanny,Knochel, Paul
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supporting information
p. 4461 - 4476
(2021/08/13)
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- Ynoate-Initiated Selective C-N Esterification of Tertiary Amines under Transition-Metal and Oxidant-Free Conditions
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An efficient and selective method for metal-and oxidant-free deaminated esterification of tertiary amines is presented. In this protocol, ynoates play a key role to activate the Csp 3-N bond through a process of in situ generation of zwitterionic salts. The transformations show that Csp 3-N bond in the zwitterionic species has a lower dissociation energy than Csp 2-N bond, leading to break preferentially and be trapped by carboxylic acids to generate the corresponding products in moderate to good yield.
- Sun, Feixiang,Feng, Huangdi,Huang, Liliang,Huang, Junhai
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supporting information
p. 713 - 717
(2021/01/14)
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- A predictive model for additions to: N -alkyl pyridiniums
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Disclosed in this communication is a thorough study on the dearomative addition of organomagnesium nucleophiles to N-alkyl pyridinium electrophiles. The regiochemical outcomes have observable and predictable trends associated with the substituent patterns on the pyridinium electrophile. Often, the substituent effects can be either additive, giving high selectivities, or ablative, giving competing outcomes. Additionally, the nature of the organometallic nucleophilic component was also investigated for its role in the regioselective outcome. The effects of either reactive component are important to both the overall reactivity and site of nucleophilic addition. The utility of these observed trends is demonstrated in a concise, dearomative synthesis of a tricyclic compound shown to have insecticidal activity. This journal is
- Knight, Brian J.,Tolchin, Zachary A.,Smith, Joel M.
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supporting information
p. 2693 - 2696
(2021/03/18)
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- Lipshutz-type bis(amido)argentates for directed: Ortho argentation
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Bis(amido)argentate (TMP)2Ag(CN)Li2 (3, TMP-Ag-ate; TMP = 2,2,6,6-tetramethylpiperidido) was designed as a tool for chemoselective aromatic functionalization via unprecedented directed ortho argentation (DoAg). X-Ray crystallographic analysis showed that 3 takes a structure analogous to that of the corresponding Lipshutz cuprate. DoAg with this TMP-Ag-ate afforded multifunctional aromatics in high yields in processes that exhibited high chemoselectivity and compatibility with a wide range of functional groups. These included organometallics- A nd transition metal-susceptible substituents such as methyl ester, aldehyde, vinyl, iodo, (trifluoromethanesulfonyl)oxy and nitro groups. The arylargentates displayed good reactivity with various electrophiles. Chalcogen (S, Se, and Te) installation and azo coupling reactions also proceeded efficiently.
- Tezuka, Noriyuki,Hirano, Keiichi,Peel, Andrew J.,Wheatley, Andrew E. H.,Miyamoto, Kazunori,Uchiyama, Masanobu
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p. 1855 - 1861
(2020/03/03)
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- Synthesis and antimicrobial activity of new prenylated 2-pyrone derivatives
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A series of new monoprenylated and diprenylated 2-pyrone derivatives with different halogen substituents were synthesized from the corresponding 6-aryl-4-hydroxy-2-pyrones by prenylation reactions. The compounds were evaluated for antibacterial activity and displayed significant in vitro activity with the highest activity shown by the monoprenylated 6-aryl-2-pyrones. All the compounds except the bromine-containing analogs were active against one or more tested bacteria, with Escherichia coli being the most susceptible of the test organisms. With the remarkable antibacterial activity of eight of the compounds against a drug-resistant β-lactamase-producing Klebsiella pneumoniae, a synergistic evaluation between each of these compounds and ampicillin was undertaken. Out of the eight combinations studied, synergistic effects were observed with two compounds, 4-(3-methylbut-2-enoxy)-6-phenyl-2H-pyran-2-one and 6-(4-fluorophenyl)-4-(3-methylbut-2-enoxy)-2H-pyran-2-one. Both compounds, at half the individual MIC values, were able to lower the MIC of ampicillin in combinations from 2500 to 2.4 μg/mL (1/1041 of MIC).
- Chukwujekwu, Jude C.,Obi, Grace,van Heerden, Fanie R.
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- PROCESS FOR THE PREPARATION OF QUINOLONE BASED COMPOUNDS
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The present invention relates to an improved process for the preparation of quinolone based compounds of general formula (I) using intermediate compound of general formula (XII). Invention also provides an improved process for the preparation of compound of formula (I-a) using intermediate compound of formula (XII-a) and some novel impurities generated during process. Compounds prepared using this process can be used to treat anemia.
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Paragraph 0241; 0248-0249; 0275; 0280-0281; 0303; 0307-0309
(2019/12/06)
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- Dibenzodiazepine*ketone derivative with anti-tumor activity and preparation method and application of dibenzodiazepine*ketone derivative
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The invention discloses a dibenzodiazepine*ketone derivative with anti-tumor activity and a preparation method and application of the dibenzodiazepine*ketone derivative and belongs to the technical field of medicine compounds with anti-tumor activity. Acc
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Paragraph 0033; 0059-0061
(2019/10/01)
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- Metal-Free Synthesis of 4-Chloroisocoumarins by TMSCl-Catalyzed NCS-Induced Chlorinative Annulation of 2-Alkynylaryloate Esters
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4-Chloroisocoumarins can be conveniently prepared from 2-alkynylaryloate esters via the activation of alkynes by electrophilic chlorine, generated in situ from N-chlorosuccinimide (NCS) in the presence of 10 mol % trimethylsilyl chloride (TMSCl), which leads to 6-endo-dig-selective chlorinative annulation to give the desired products in moderate to quantitative yields. The procedure employs readily available reagents and can be conveniently carried out on a wide scope of substrates under mild conditions (0 °C to rt). Furthermore, the reaction is scalable for gram-scale preparation of 4-chloroisocoumarins. Additionally, 4-bromo- and 4-iodoisocoumarins can be prepared in moderate to good yields by replacing NCS with N-bromosuccinimide (NBS) and N-iodosuccinimide (NIS), respectively.
- Norseeda, Krissada,Chaisan, Nattawadee,Thongsornkleeb, Charnsak,Tummatorn, Jumreang,Ruchirawat, Somsak
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p. 16222 - 16236
(2019/12/25)
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- Unprecedented alkylation of carboxylic acids by boron trifluoride etherate
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The alkylation of carboxylic acids by an ethyl moiety of boron trifluoride etherate in the absence of ethyl alcohol from the reaction system is unexpected and novel. Both aromatic and aliphatic carboxylic acids were clearly alkylated affording good yields in short reaction times with the exception of nicotinic acid that necessitated an overnight reaction. It was noted that while ortho-substituted hydroxyl groups of carboxylic acids investigated were not affected by alkylation, those of meta- and para-substituted carboxylic acids were partially etherified. Furthermore, the alkylation reaction was found to be compatible with a range of functional groups such as halogens, amino and nitro groups except for the alkene function of undecylenic acid that underwent polymerisation with concomitant alkylation of its carboxylic acid function.
- Jumbam, Ndze D.,Maganga, Yamkela,Masamba, Wayiza,Mbunye, Nomthandazo I.,Mgoqi, Esethu,Mtwa, Sphumusa
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p. 387 - 392
(2018/09/06)
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- Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety
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A series of trifluoromethyl pyridine derivatives containing 1,3,4-oxadiazole moiety was designed, synthesized and bio-assayed for their insecticidal activity. The result of bio-assays indicated the synthesized compounds exhibited good insecticidal activity against Mythimna separata and Plutella xylostella, most of the title compounds show 100% insecticidal activity at 500 mg L-1 and >80% activity at 250 mg L-1 against the two pests. Compounds E18 and E27 showed LC50 values of 38.5 and 30.8 mg L-1 against Mythimna separata, respectively, which were close to that of avermectin (29.6 mg L-1); compounds E5, E6, E9, E10, E15, E25, E26, and E27 showed 100% activity at 250 mg L-1, which were better than chlorpyrifos (87%). CoMFA and CoMSIA models with good predictability were proposed, which revealed the electron-withdrawing groups with an appropriate bulk at 2- and 4-positions of benzene ring could enhance insecticidal activity.
- Xu,Wang,Luo,Yu,Guo,Fu,Zhao,Wu
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p. 6306 - 6314
(2018/02/19)
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- Dibenzozepine compound and preparation method and application thereof
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The invention discloses a dibenzozepine compound and a preparation method and application thereof. The structure of the dibenzozepine compound is as shown in the general formula 1 or general formula 2, wherein R1 is selected from methyl, hydrogen, chlorin
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Paragraph 0058; 0059; 0060
(2018/10/11)
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- A general electrochemical strategy for the Sandmeyer reaction
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Herein we report a general electrochemical strategy for the Sandmeyer reaction. Using electricity as the driving force, this protocol employs a simple and inexpensive halogen source, such as NBS, CBrCl3, CH2I2, CCl4, LiCl and NaBr for the halogenation of aryl diazonium salts. In addition, we found that these electrochemical reactions could be performed using anilines as the starting material in a one-pot fashion. Furthermore, the practicality of this process was demonstrated in the multigram scale synthesis of aryl halides using highly inexpensive graphite as the electrode. A series of detailed mechanism studies have been performed, including radical clock and radical scavenger study, cyclic voltammetry analysis and in situ electron paramagnetic resonance (EPR) analysis.
- Liu, Qianyi,Sun, Beiqi,Liu, Zheng,Kao, Yi,Dong, Bo-Wei,Jiang, Shang-Da,Li, Feng,Liu, Guoquan,Yang, Yang,Mo, Fanyang
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p. 8731 - 8737
(2018/12/10)
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- Efficient copper-catalyzed Sonogashira coupling reactions and simulation studies
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A practical copper-catalyzed I-substitutions of alkyl-2-iodobenzoates with alkynes have been developed using Cu powder as a catalyst under solvent, cocatalyst, and base-free conditions. This reaction system is new, facile, efficient, and economical that g
- Ali, Imran,Nighot, Dnyaneshwar,Lone, Mohammad Nadeem,Jain, Arvind
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supporting information
p. 1175 - 1184
(2017/06/09)
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- One-pot dichlorinative deamidation of primary β-ketoamides
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An approach to the dichlorinative deamidation of primary β-ketoamides through ketonic cleavage is described, and a series of α,α-dichloroketones were furnished mostly in the presence of TEMPO. Based on control experiments, a mechanism involving tandem dichlorination and deamidation is proposed to interpret the observed reactivity.
- Zheng, Congke,Zhang, Xiaohui,Ijaz Hussain, Muhammad,Huang, Mingming,Liu, Qing,Xiong, Yan,Zhu, Xiangming
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supporting information
p. 574 - 577
(2017/01/16)
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- Synthesis and antibacterial activity of some new quinaxaline-benzohydrazides
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Quinoxalines have been found to exhibit various biological activities such as antibacterial, antifungal, anti-tubercular, anxiolytic, anticancer, antioxidant, anti-inflammatory, anti-HIV, antihelmintic and anticonvulsant. The present study aims towards synthesis, characterization and determination of antimicrobial susceptibility testing of various novel quinoxaline derivatives. The quinoxaline-benzohydrazides 6a-m have been obtained by the condensation of quinoxaline-2-carboxaldehyde 4 with various benzohydrazides 5a-m in ethanol at reflux temperature. All the newly synthesized quinoxaline-benzohydrazide derivatives have been characterized by 1H NMR, IR and mass spectroscopic analysis. The synthesized quinoxaline-benzohydrazides 6a-m have been screened for antibacterial activity. Most of the compounds show significant antibacterial activity.
- Haripriya,Laxminarayana,Thirumala Chary
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p. 207 - 212
(2017/01/18)
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- Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors
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A novel serie of escitalopram triazoles (60-88) and a tetrazole (89) have been synthesized and subjected to a study to establish the inhibitory potential of these compounds toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Some selectivity in inhibition has been observed. The 4-chlorophenyl- (75, IC50, 6.71 ± 0.25 μM) and 2-methylphenyl- (70, IC50, 9.52 ± 0.23 μM) escitalopram triazole derivatives depicted high AChE inhibition, while 2-fluorophenyl- (76, IC50 = 4.52 ± 0.17 μM) and 4-fluorophenyl- (78, IC50 = 5.31 ± 0.43 μM) have found to be excellent BChE inhibitors. It has also been observed that ortho, meta and para substituted electron donating groups increase the inhibition, while electron withdrawing groups reduce the inhibition. Docking analyses of inhibitors with AChE have depicted the binding energies for 70 and 75 as ΔGbind -6.42 and -6.93 kcal/mol, respectively, while ligands 76 and 78 have shown the binding affinity ΔGbind -9.04 and -8.51 kcal/mol, respectively, for BChE.
- Mehr-Un-Nisa,Munawar, Munawar A.,Chattha, Fauzia A.,Kousar, Samina,Munir, Jawaria,Ismail, Tayaba,Ashraf, Muhammad,Khan, Misbahul A.
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p. 6014 - 6024
(2015/11/11)
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- Synthesis and antimicrobial activity of new imidazole-hydrazone derivatives
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Hydrazones demonstrated significant antimicrobial activity, antitubercular activity and antitumoral activity in medicinal areas. The imidazole nucleus is well known to play an important role in living organisms since it is incorporated into the histidine molecule and many other important biological, pharmacological and therapeutic activities. Condensation of 4-phenyl-1H-imidazole-2-carbaldehyde (3) with various selected benzohydrazides (4a-m) resulted in imidazole-hydrazone derivatives (5a-m). They were evaluated for antibacterial and antifungal activity against A. Niger, C. albicans (fungal strains), E. coli and P. aeruginosa (Gram-negative bacteria), S. aureus and S. pyogenes (Gram-positive bacteria) using griseofluvin (for fungi) and ciprofloxacin (for bacteria) as the standard drugs. In general, it is observed that most of the compounds were found to be potent against both the bacterial and fungal strains.
- Prasanna, V. Laxmi,Narender
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p. 3605 - 3608
(2015/12/24)
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- Photo-induced Metal-Catalyst-Free Aromatic Finkelstein Reaction
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The facile iodination of aromatic compounds under mild conditions is a great challenge for both organic and medicinal chemistry. Particularly, the synthesis of functionalized aryl iodides by light has long been considered impossible due to their photo-lability, which actually makes aryl iodides popular starting materials in many photo-substitution reactions. Herein, a photo-induced halogen exchange in aryl or vinyl halides has been discovered for the first time. A broad scope of aryl iodides can be prepared in high yields at room temperature under exceptionally mild conditions without any metal or photo-redox catalysts. The presence of a catalytic amount of elemental iodine could promote the reaction significantly.
- Li, Lu,Liu, Wenbo,Zeng, Huiying,Mu, Xiaoyue,Cosa, Gonzalo,Mi, Zetian,Li, Chao-Jun
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supporting information
p. 8328 - 8331
(2015/07/15)
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- N-picolinamides as ligands for Ullmann-type homocoupling reactions
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The use of N-phenylpicolinamide (NPPA) as a ligand in Ullmann-type homocoupling reactions of aryl iodides and bromides in common solvents, such as DMF and MeCN has been successfully demonstrated at room temperature. In addition, this work provided the first example of the homocoupling of an aryl chloride at 82 °C, which is a relatively low temperature when compared to regular Ullmann reaction temperatures. Also, NPPA was successfully employed in base-and heat free Suzuki reactions, including electron rich and poor aryl halides with heteroarylboronic acids in moderate yields.
- Damkaci, Fehmi,Altay, Esra,Waldron, Matthew,Knopp, Michael A.,Snow, David,Massaro, Nicholas
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supporting information
p. 690 - 693
(2014/01/23)
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- One-pot transformation of carboxylic acids into nitriles
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A variety of aromatic and aliphatic carboxylic acids were smoothly converted into the corresponding nitriles in good yields in a one-pot procedure by treatment with ethyl iodide/K2CO3/18-crown-6, followed by sodium diisobutyl-tert-butoxyaluminium hydride (SDBBA-H), and finally treatment with molecular iodine or 1,3-diiodo-5,5-dimethylhydantoin (DIH), and aqueous ammonia. This method is useful for the conversion of various aromatic and aliphatic carboxylic acids into the corresponding nitriles in a one-pot procedure. A variety of aromatic and aliphatic carboxylic acids were smoothly converted into the corresponding nitriles in good yields in a one-pot procedure by treatment with ethyl iodide/K2CO3/18-crown-6, followed by sodium diisobutyl-tert-butoxyaluminium hydride (SDBBA-H), and finally treatment with molecular iodine or 1,3-diiodo-5,5-dimethylhydantoin (DIH), and aqueous ammonia. Copyright
- Miyagi, Kotaro,Moriyama, Katsuhiko,Togo, Hideo
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p. 5886 - 5892
(2013/09/23)
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- Facile synthesis of 2-iodo-spiro[indene-1,1′-isobenzofuran]-3′- ones via iodine-promoted cascade cyclization
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A novel and efficient synthetic approach to substituted 2-iodo-spiro[indene-1,1′-isobenzofuran]-3′-ones has been developed via an iodine-promoted cascade cyclization of 2-(3-hydroxy-3,3-diarylprop-1-yn- 1-yl)benzoates. This sequential cascade process is concisely conducted at room temperature. Subsequent palladium-catalyzed Sonogashira, Suzuki, and Heck reactions of the resulting iodides proceed smoothly in good yields.
- Zhu, Hai-Tao,Dong, Xue,Wang, Li-Jing,Zhong, Mei-Jin,Liu, Xue-Yuan,Liang, Yong-Min
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supporting information
p. 10748 - 10750,3
(2020/09/02)
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- 2-Iodoxybenzoic acid-mediated transformation of halogenated hydrocarbon in the presence of tetraethyl ammonium bromide
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2-Iodoxybenzoic acid (IBX) has been shown to react with alkyl halides in the presence of tetraethyl ammonium bromide to give 2-iodobenzoate esters. Most of the monohalides and dihalides reacted easily with moderate to good yields. The 2-iodobenzoate ester
- Zhang, Yuan,Han, Jianlei,Xu, Yanjun,Wei, Yuping
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experimental part
p. 303 - 307
(2012/09/25)
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- Cobalt-catalyzed preparation of arylindium reagents from aryl and heteroaryl bromides
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A cobalt-bathophenanthroline catalyst has been developed for the direct preparation of a variety of arylindium reagents from the corresponding aryl and heteroaryl bromides in the presence of indium metal and lithium chloride. The thus-formed arylindium reagents undergo efficient palladium-catalyzed cross-coupling reactions with aryl iodides, tolerating various functional groups including hydroxy and free amino groups.
- Adak, Laksmikanta,Yoshikai, Naohiko
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experimental part
p. 7563 - 7568
(2011/11/12)
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- Deprotonative metalation of substituted aromatics using mixed lithium-cobalt combinations
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The deprotonation of anisole was attempted using different homo- and heteroleptic TMP/Bu mixed lithium-cobalt combinations. Using iodine to intercept the metalated anisole, an optimization of the reaction conditions showed that in THF at room temperature 2 equiv of base were required to suppress the formation of the corresponding 2,2′-dimer. The origin of the dimer was not identified, but its formation was favored with allyl bromide as electrophile. The metalated anisole was efficiently trapped using iodine, anisaldehyde, and chlorodiphenylphosphine, and moderately employing benzophenone, and benzoyl chloride. 1,2-, 1,3-, and 1,4-dimethoxybenzene were similarly converted regioselectively to the corresponding iodides. It was observed that 2-methoxy- and 2,6-dimethoxypyridine were more prone to dimerization than the corresponding benzenes when treated similarly. Involving ethyl benzoate in the metalation-iodination sequence showed that the method was not suitable to functionalize substrates bearing reactive functions.
- Dayaker, Gandrath,Chevallier, Floris,Gros, Philippe C.,Mongin, Florence
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experimental part
p. 8904 - 8910
(2011/01/04)
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- Methods and Compositions for Modulating P300/CBP Activity
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The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.
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Page/Page column 19-20
(2010/09/05)
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- The synthesis and fungicidal activities of 2,6-bis[(3-aryl)-s-triazolo[3,4- b]-[1,3,4]thiadiazole-6-yl]pyridines
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In search of better bioactive compounds, a series of novel 2,6-bis[(3-aryl)-s-triazolo[3,4-b]-[1,3,4]thiadiazole-6-yl]pyridines 2 were synthesized in high yields by the cyclization of 3-aryl-4-amino-5-mercapto-1, 2, 4-triazoles 1 with 2,6-pyridine dicarboxylic acid. 2 exhibited good fungicidal activities against Cerospora beticola sacc. Copyright Taylor & Francis Group, LLC.
- Li, Dejiang,Long, Deqing,Fu, Heqing
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p. 2079 - 2087
(2007/10/03)
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- Esters of 2-iodoxybenzoic acid: Hypervalent iodine oxidizing reagents with a pseudobenziodoxole structure
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Esters of 2-iodoxybenzoic acid (IBX-esters) were prepared by the hypochlorite oxidation of the corresponding 2-iodobenzoate esters and isolated as chemically stable, microcrystalline products. These hypervalent iodine compounds are potentially valuable ox
- Zhdankin, Viktor V.,Koposov, Alexey Y.,Litvinov, Dmitry N.,Ferguson, Michael J.,McDonald, Robert,Luu, Thanh,Tykwinski, Rik R.
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p. 6484 - 6491
(2007/10/03)
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- Synthesis of C2-C3′N-linked macrocyclic taxoids. Novel docetaxel analogues with high tubulin activity
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Novel C2-C3′N-linked macrocyclic taxoids 4 bearing an aromatic ring at position C2 were synthesized. These compounds, tethered between N3′ and the C2-aromatic ring at the ortho, meta, or para position, were constructed by ring-closing metathesis. The para
- Querolle, Olivier,Dubois, Jo?lle,Thoret, Sylviane,Roussi, Fanny,Guéritte, Fran?oise,Guénard, Daniel
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p. 5937 - 5944
(2007/10/03)
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- Novel Extension of Meyers' Methodology: Stereoselective Construction of Axially Chiral 7,5-Fused Bicyclic Lactams
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A novel extension of Meyer's lactamization is reported for the preparation of seven-membered ring lactams 1a-d incorporating a biaryl unit. The required keto-esters 2a-c were readily accessible via the Suzuki coupling reaction. A borylation-Suzuki couplin
- Penhoat, Mael,Levacher, Vincent,Dupas, Georges
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p. 9517 - 9520
(2007/10/03)
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- An efficient general method for esterification of aromatic carboxylic acids
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Treatment of a variety of aromatic carboxylic acids with alcohols in the presence of thionyl chloride results in excellent yields of corresponding esters. This esterification system is compatible with a wide assortment of functional groups.
- Hosangadi, Bhaskar D.,Dave, Rajesh H.
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p. 6375 - 6378
(2007/10/03)
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