- Chroman-4-one hydrazones derivatives: synthesis, characterization, and in vitro and in vivo antileishmanial effects
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In searching for better therapeutic alternatives to treat cutaneous leishmaniasis (CL), this study aimed to obtain and evaluate the efficacy and toxicity of new chroman-4-one hydrazones derivatives. Compounds were prepared and characterized, and then transformed into hydrazonas for molecular optimization. Their cytotoxicity was tested in different cell types using an in vitro MTT assay and the efficacy was evaluated using an in vitro macrophage intracellular amastigotes of Leishmania (Viannia) panamensis and L. (V) braziliensis by flow cytometry. The therapeutic effect of two formulations of chroman-4-one hydrazones on the CL induced by L. (V) braziliensis in golden hamsters was determined according to the size of lesions after treatment. The effect of these compounds in the production of inflammatory mediators and cell migration was also determined by in vitro assays using human fibroblasts models. Neither cytotoxicity nor genotoxicity was observed. The benzoic acid hydrazone derivative 2-(2,3-dihydro-4H-1-benzopyran-4-ylidene) hydrazide (4), produced a higher percentage of clinical cures, followed by benzoic acid, 2-(2,3-dihydro-4H-1-benzothiopyran-4-ylidene) hydrazide (3), while benzoic acid, 2-(2,3-dihydro-1,1-dioxide-4H-1-benzothiopyran-4-ylidene) hydrazide (5) and 4-pyridinecarboxylic acid, 2-(4H-1-benzopyran-4-ylidene) hydrazide (6) caused a poor therapeutic response. The compound 4 also showed an effect in the inflammatory and fibroblast migration processes. In conclusion, this is the first report of antileishmanial activity combined with inflammatory and wound healing properties. Results obtained here suggest that this strategy could be a good alternative for development of new drugs for the treatment of CL.
- Upegui, Yulieth,Rios, Karina,Qui?ones, Wiston,Echeverri, Fernando,Archbold, Rosendo,Murillo, Javier D.,Torres, Fernando,Escobar, Gustavo,Vélez, Iván D.,Robledo, Sara M.
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Read Online
- New class of benzothiophene morpholine analogues with high selectivity and affinity were designed and evaluated for anti-drug addiction
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To probe the mechanism of dopamine receptors in drug addiction and look for potential new methods for treating this disease, we have designed and synthesized benzothiophene morpholine analogues that were considered as dopamine D3 receptor-selective ligands. Radioligand binding assay was used to determine the binding affinity of target compounds. Members of this class have great selectivity and binding affinity in D3 receptor. In addition, the ability of these compounds to mitigate the symptoms of addiction from opioids was investigated in animal behavior patterns, and we have found that two compounds (18a and 18d) have good affinity in the D3R and exhibit the efficacy of anti-drug addiction in morphine-dependent mice induced by naloxone.
- Cai, Jin,Wang, Yuhong,Chen, Xixi,Ji, Min
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p. 634 - 649
(2022/03/01)
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- Chitosan as a chiral ligand and organocatalyst: Preparation conditions-property-catalytic performance relationships
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Chitosan is an abundant and renewable chirality source of natural origin. The effect of the preparation conditions by alkaline hydrolysis of chitin on the properties of chitosan was studied. The materials obtained were used as ligands in the ruthenium-catalysed asymmetric transfer hydrogenation of aromatic prochiral ketones and oxidative kinetic resolution of benzylic alcohols as well as organocatalysts in the Michael addition of isobutyraldehyde to N-substituted maleimides. The degrees of deacetylation of the prepared materials were determined by 1H NMR, FT-IR and UV-vis spectroscopy, the molecular weights by viscosity measurements, their crystallinity by WAXRD, and their morphology by SEM and TEM investigations. The materials were also characterized by Raman spectroscopy. The biopolymers which have molecular weights in a narrow (200-230 kDa) range and appropriate (80-95%) degrees of deacetylation were the most efficient ligands in the enantioselective transfer hydrogenation, whereas in the oxidative kinetic resolution the activity of the complexes and the stereoselectivity increased with the degree of deacetylation. The chirality of the chitosan was sufficient to obtain enantioselection in the Michael addition of isobutyraldehyde to maleimides in the aqueous phase. Interestingly, the biopolymer afforded the opposite enantiomer in excess compared to the monomer, d-glucosamine. In this reaction, good correlation between the degree of deacetylation and the catalytic activity was found. These results are novel steps in the application of this natural, biocompatible and biodegradable polymer in developing environmentally benign methods for the production of optically pure fine chemicals.
- Kolcsár, Vanessza Judit,Sz?ll?si, Gy?rgy
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p. 7652 - 7666
(2021/12/13)
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- Synthesis of benzothiazonine by rhodium-catalyzed denitrogenative transannulation of 1-sulfonyl-1,2,3-triazole and thiochromone
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A facile synthesis of multi-functionalized benzothiazonine was achieved by the rhodium-catalyzed denitrogenative annulation of 1-sulfonyl-1,2,3-triazole and thiochromone. In view of the excellent atom economy, broad substrate scope and easy availability of starting materials, the protocol provided an efficient strategy for the construction of mediumN,S-heterocycles.
- Duan, Shengguo,Jablasone, Saygbechi T.,Li, Chuan-Ying,Xu, Ze-Feng,Ye, Zihang
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p. 5758 - 5761
(2021/07/12)
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- Synthesis method of 2,3-dihydrothiochromene-4-one and derivative thereof
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The invention discloses a synthesis method of 2,3-dihydrothiochromene-4-one and a derivative thereof. The synthesis method is characterized in that a substituted and unsubstituted aromatic thiophenolcompound is used as a raw material, and reacts with acrylic acid to generate corresponding aromatic thiopropionic acid, and cyclizing is performed under the action of concentrated sulfuric acid to obtain the corresponding 2,3-dihydrothiochromene-4-one and the derivative thereof. According to the invention, the raw materials use acrylic acid and concentrated sulfuric acid, so that the raw materialsare easy to obtain, the cost is low, and the feeding is easy; and the post-treatment only needs acidification, extraction, washing and solvent evaporation, so that the method is simple in post-treatment, high in yield, low in cost and suitable for industrial production.
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- Cu(I)-Catalyzed Enantioselective Alkynylation of Thiochromones
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A highly efficient asymmetric synthesis of chiral thiochromanones is developed via Cu(I)/phosphoramidite catalyzed asymmetric alkynylation of thiochromones under mild reaction conditions. The catalyst system is tolerant of various thiochromone precursors and terminal alkynes. The established asymmetric transformation provides different enatiomeric-enriched thiochromanones with more molecular complexity and enables access to chiral thioflavanones, a subgroup of flavonoid by further functionalization.
- Chang, Xiaoyong,Lin, Zhenyang,Meng, Ling,Ngai, Ka Yan,Wang, Jun
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p. 1155 - 1159
(2020/02/26)
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- Synthesis and anti cervical cancer activity of novel 5H-thiochromeno [4,3-d]pyrimidines
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A series of novel 5H-Thiochromeno[4,3-d]pyrimidine derivatives were synthesized, purified and characterized by different spectroscopy techniques such as1H NMR,13C NMR, Mass and Elemental Analysis. The new compounds were evaluated for their anti-cervical cancer activity on Human Cervical Cell Line HeLa. They were found to be potent anti-cervical cancer agents with GI50 values less than 10 μg/mL with respect to positive control drug Adriamycin.
- Naliapara, Yogesh,Pandya, Dhananjay
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p. 294 - 302
(2020/04/21)
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- Synthesis of Novel Pterocarpen Analogues via [3?+?2] Coupling-Elimination Cascade of α,α-Dicyanoolefins with Quinone Monoimines
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By employing triethylamine as a catalyst, [3?+?2] coupling-elimination cascade of α,α-dicyanoolefins with quinone monoimines was realized. The reactions afforded various novel pterocarpen analogues with generally moderate yields (up to 75%). In addition, a plausible reaction mechanism was proposed.
- Chen, Hui,Zhao, Sihan,Cheng, Shaobing,Dai, Xingjie,Xu, Xiaoying,Yuan, Weicheng,Zhang, Xiaomei
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p. 1672 - 1683
(2019/04/08)
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- Development of conjugate addition of lithium dialkylcuprates to thiochromones: Synthesis of 2-alkylthiochroman-4-ones and additional synthetic applications
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Lithium dialkylcuprates undergo conjugate addition to thiochromones to afford 2-alkylthiochroman-4-ones in good yields. This approach provide an efficient and general synthetic approach to privileged sulfur-containing structural motifs and valuable precursors for many pharmaceuticals, starting from common substrates-thiochromones. Good yields of 2-alkyl-substituted thiochroman-4-ones are attained with lithium dialkylcuprates, lithium alkylcyanocuprates or substoichiometric amount of copper salts. The use of commercially available inexpensive alkyllithium reagents will expedite the synthesis of a large library of 2-alkyl substituted thiochroman-4-ones for additional synthetic applications.
- Bass, Shekinah A.,Parker, Dynasty M.,Bellinger, Tania J.,Eaton, Aireal S.,Dibble, Angelica S.,Koroma, Kaata L.,Sekyi, Sylvia A.,Pollard, David A.,Guo, Fenghai
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- Cu-Catalyzed Conjugate Addition of Grignard Reagents to Thiochromones: An Enantioselective Pathway for Accessing 2-Alkylthiochromanones
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The enantioselective incorporation of alkyl groups in thiochromones was realized for the first time by a Cu/(R, S)-PPF-P t Bu 2 -catalyzed conjugate addition of Grignard reagents to thiochromones. With this method, a series of 2-methylthiochromanones were obtained in good yields (up to 96% yield) with moderate-to-good ee values (up to 87% ee). The established method expedites the synthesis of a large library of chiral thiochromanones for further synthetic applications and biological studies.
- Luo, Shihui,Meng, Ling,Yang, Qingxiong,Wang, Jun
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p. 2071 - 2075
(2018/09/18)
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- Hydrazone derivatives enhance antileishmanial activity of thiochroman-4-ones
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Cutaneous leishmaniasis (CL) is a neglected tropical disease, which causes severe skin lesions. Due to the lack of effective vaccines, and toxicity or reduced effectiveness of available drugs in addition to complex and prolonged treatments, there is an urgent need to develop alternatives for the treatment for CL with different mechanisms of action. In our effort to search for new promising hits against Leishmania parasites we prepared 18 acyl hydrazone derivatives of thiochroman-4-ones. Compounds were evaluated for their in vitro antileishmanial activity against the intracellular amastigote form of Leishmania panamensis and cytotoxic activity against human monocytes (U-937 ATCC CRL-1593.2). Our results show that derivatization of the thiochroman-4-ones with acyl hydrazones significantly enhances the antileishmanial activity. Among the compounds tested semicarbazone and thiosemicarbazone derivatives of thioflavanone 19 and 20 displayed the highest antileishmanial activities, with EC50 values of 5.4 and 5.1 μM and low cytotoxicities (100.2 and 50.1 μM respectively), resulting in higher indexes of selectivity (IS).
- Vargas, Esteban,Echeverri, Fernando,Upegui, Yulieth A.,Robledo, Sara M.,Qui?ones, Wiston
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- Rh-Catalyzed Conjugate Addition of Arylzinc Chlorides to Thiochromones: A Highly Enantioselective Pathway for Accessing Chiral Thioflavanones
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A highly efficient asymmetric synthesis of chiral thioflavanones is developed via conjugate addition of arylzinc reagents to thiochromones using Rh(COD)Cl2/(R)-3,4,5-MeO-MeOBIPHEP catalyst. This method overcomes catalyst poisoning and substrate inertness and affords a series of chiral thioflavanones (2-arylthiochroman-4-ones) in good yields (up to 91% yield) with excellent ee values (up to 97% ee). The established asymmetric synthesis paves the way for further pharmaceutical studies.
- Meng, Ling,Jin, Ming Yu,Wang, Jun
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p. 4986 - 4989
(2016/10/14)
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- Borontribromide-mediated C-C bond formation in cyclic ketones: A transition metal free approach
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Borontribromide (BBr3) is a well-known demethylating agent. The current investigation was focused on a new application of borontribromide as a C-C bond forming agent in cyclic ketones. In this study, borontribromide mediated C-C bond formation reactions of tetralones, chromenone, thiochromenone and indanones were explored. A methoxy group containing ketones showed selective C-C bond formation reaction instead of demethylation of the methoxy group. MM2 steric energy calculations for the final products showed that the reaction favored the formation of exo- or endo-cyclic double bond containing products, depending upon their low MM2 steric energy in a specific frame structure, as observed in X-ray crystallography. A comprehensive crystallographic and pi-stacking analysis of product 10a demonstrated the formation of 10a as an enantiomeric mixture, and its centre of inversion was stabilized by a set of three unique pi-pi interactions.
- Ahmad, Imran,Pathak, Vinay,Vasudev, Prema G.,Maurya, Hardesh K.,Gupta, Atul
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p. 24619 - 24634
(2014/07/07)
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- Aerobic oxidation of alcohols by using a completely metal-free catalytic system
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A metal-free reaction system of air, NH4NO3(cat), 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO)(cat), and H +(cat) is introduced as a simple, safe, inexpensive, efficient and chemoselective mediator for aerobic oxidation of various primary and secondary benzyl and alkyl alcohols, including those bearing oxidizable heteroatoms (N, S, O) to the corresponding aldehydes or ketones. Air oxygen under slight overpressure plays the role of the terminal oxidant, which is catalytically activated by redox cycles of nitrogen oxides released from a catalytic amount of NH4NO3 and cocatalyzed by TEMPO (nitroxyl radical compound), under acidic conditions, which are essential for an overall activation of the reaction system. The synthetic value of this reaction system and its green chemical profile was illustrated by a 10 g scale-up experiment, performed in an open-air system by using a renewable and reusable polymer-supported form of TEMPO (OXYNITROXS100). The reaction solvent was recovered by distillation under atmospheric pressure, and the pure final product was isolated under reduced pressure; the acid activators (HCl or H 2SO4) were recovered as ammonium salts. A metal-free reaction system of air/NH4NO3(cat)/TEMPO (cat)/H+(cat) is introduced as a simple, safe, inexpensive, efficient and chemoselective mediator for aerobic oxidation of various primary and secondary benzyl, alkyl and allyl alcohols, including those bearing oxidizable heteroatoms (N, S, O) to the corresponding aldehydes or ketones. Copyright
- Prebil, Rok,Stavber, Gaj,Stavber, Stojan
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supporting information
p. 395 - 402
(2014/01/23)
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- Aerobic Oxidation of Alcohols by Using a Completely Metal-Free Catalytic System
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A metal-free reaction system of air, NH4NO3(cat), 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO)(cat), and H+(cat) is introduced as a simple, safe, inexpensive, efficient and chemoselective mediator for aerobic oxidation of various primary and secondary benzyl and alkyl alcohols, including those bearing oxidizable heteroatoms (N, S, O) to the corresponding aldehydes or ketones. Air oxygen under slight overpressure plays the role of the terminal oxidant, which is catalytically activated by redox cycles of nitrogen oxides released from a catalytic amount of NH4NO3 and cocatalyzed by TEMPO (nitroxyl radical compound), under acidic conditions, which are essential for an overall activation of the reaction system. The synthetic value of this reaction system and its green chemical profile was illustrated by a 10 g scale-up experiment, performed in an open-air system by using a renewable and reusable polymer-supported form of TEMPO (OXYNITROXS100). The reaction solvent was recovered by distillation under atmospheric pressure, and the pure final product was isolated under reduced pressure; the acid activators (HCl or H2SO4) were recovered as ammonium salts.
- Prebil, Rok,Stavber, Gaj,Stavber, Stojan
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supporting information
p. 395 - 402
(2015/10/05)
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- Synthesis, characterization, antimicrobial, anticancer, and antituberculosis activity of some new pyrazole, isoxazole, pyrimidine and benzodiazepine derivatives containing thiochromeno and benzothiepino moieties
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In an attempt to find a new class of antimicrobial, anticancer, and antituberculosis agents, a series of pyrazole, isoxazole, pyrimidine and benzodiazepine derivatives containing thiochromeno and benzothiepino moieties were prepared via the reaction of diketoester 2 and 11 with appropriate chemical reagents. Single crystal XRD studies have been done on compounds 3 and 12. All compounds were evaluated for antimicrobial, anticancer, and antituberculosis activity. The benzodiazepine compounds (9 and 18) displayed the highest activity among the tested compounds with an IC50 equal to 15 and 16 μM for HeLa cells, and 13 and 12 μM for HCT116 cells. They were also found to be more active against H37Rv with an MIC of 7.0 and 6.5 μM compared to other analogues. Similarly these compounds (9 and 18) showed higher activity than chloroamphenicol against Klebsiella pneumoniae and Escherichia coli.
- Palanisamy, Pandaram,Jenniefer, Samson Jegan,Muthiah, Packianathan Thomas,Kumaresan, Sudalaiandi
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p. 19300 - 19310
(2013/10/22)
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- Highly efficient Cu(I)-catalyzed oxidation of alcohols to ketones and aldehydes with diaziridinone
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A novel and efficient Cu(I)-catalyzed oxidation of alcohols has been achieved with di-tert-butyldiaziridinone as the oxidant under mild conditions. A wide variety of primary and secondary alcohols with various functional groups can be oxidized to aldehydes and ketones in high yields. The reaction proceeds under neutral conditions making it compatible with acid- or base-sensitive substrates, and it is amenable to gram scale.
- Zhu, Yingguang,Zhao, Baoguo,Shi, Yian
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supporting information
p. 992 - 995
(2013/04/10)
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- Synthesis and in vitro anti-hepatitis B virus activity of 6H-[1]benzothiopyrano[4,3-b]quinolin-9-ols
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A series of novel 6H-[1]benzothiopyrano[4,3-b]quinoline derivatives were prepared and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in human hepatoblastoma-derived liver Hep-G2 cells. Compounds 10g, 10h, 10j, 10l and 10o were found to be potent anti-HBV compounds with IC50 values less than 50 μM. The most promising compound was 10l, with an IC50 value of 14.7 μM and a SI value of 12.4. This is the first report of the anti-HBV effects of 6H-[1]benzothiopyrano[4,3-b] quinolin-9-ols. Crown Copyright
- Jia, Wei,Liu, Yajing,Li, Wei,Liu, Yan,Zhang, Dajun,Zhang, Peng,Gong, Ping
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experimental part
p. 4569 - 4574
(2009/10/17)
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- Activation of DMSO by phosphonitrilic chloride: An efficient method for oxidation of alcohols
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A variety of alcohols have been oxidized under mild conditions by a dimethylsulfoxide (DMSO)-chlorophosphazene complex. Sensitive groups such as silyl and tetrahydropyranyl (THP) ethers are stable under this condition. Copyright Taylor & Francis Group, LLC.
- Pandey, Sanjay K.,Bisai, Alakesh,Singh, Vinod K.
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p. 4099 - 4103
(2008/03/13)
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- SUBSTITUTED BENZO-CONDENSED CYCLOHEXANONE DERIVATIVES AND THE USE THEREOF FOR MEDICAMENT PRODUCTION
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The invention relates to substituted benzo-condensed cyclohexanone derivatives, to a method for the production thereof, to medicaments containing said derivatives and to the use of the inventive compounds for producing medicaments.
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Page/Page column 61-62
(2008/06/13)
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- A rapid and efficient synthesis of thiochroman-4-ones under microwave irradiation
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Thiochroman-4-ones were synthesised by the cyclization of β-arylthiopropionic acids which were prepared by the condensation of the arylthiols with chloropropionic acid under microwave irriadiation within 4min.
- Li, Ji-Tai,Li, Hong-Ya,Li, Hui-Zhang,Xiao, Li-Wei
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p. 394 - 395
(2007/10/03)
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- Wet silica-supported permanganate for the cleavage of semicarbazones and phenylhydrazones under solvent-free conditions
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Wet silica-supported potassium permanganate was used as an inexpensive and efficient reagent for conversion of semicarbazones and phenylhydrazones to the corresponding carbonyl compounds under solid-state conditions.
- Hajipour, Abdol R.,Adibi, Hadi,Ruoho, Arnold E.
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p. 4553 - 4555
(2007/10/03)
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- Chalcogeno Morita-Baylis-Hillman Reaction of 2-(Methylchalcogeno)phenyl Vinyl Ketones with Aldehydes, Ketones, and α-Dicarbonyl Compounds
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Reactions of 2-(methylchalcogeno)phenyl vinyl ketones 1 and 4 with aldehydes 5 were conducted in the presence of BF3·Et 2O. The reaction was quenched by addition of Et3N and gave the Morita-Baylis-Hillman adducts 6-7 in good yields. When the reaction mixture of 1 with 5a was worked up with saturated aqueous NaHCO3, the sulfonium salt 8a was obtained together with 6. Ketones 10, α-diketones, and α-oxo esters 13, which hardly react in the traditional Morita-Baylis-Hillman reaction, similarly reacted with 2-(methylchalcogeno)phenyl vinyl ketones 1 and 4 to give the Morita-Baylis-Hillman adducts 11-12 and 14-15. Selenochromanones 9 and 16 were obtained together with 7 and 15 from reactions of seleno derivative 4, with 5 and 13 as by-products. The formation mechanism for the sulfonium salt syn-trans-8a is discussed. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
- Kinoshita, Hironori,Kinoshita, Sayaka,Munechika, Yukari,Iwamura, Tatsunori,Watanabe, Shin-Ichi,Kataoka, Tadashi
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p. 4852 - 4861
(2007/10/03)
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- An alternative to the Swern oxidation
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A variety of alcohols have been oxidized under mild conditions by the DMSO-Ph3P·X2 complexes. The reaction does not produce any Pummerer product. A mechanism for the reaction is proposed.
- Bisai, Alakesh,Chandrasekhar,Singh, Vinod K.
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p. 8355 - 8357
(2007/10/03)
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- High-throughput purification of solution-phase periodinane mediated oxidation reactions utilizing a novel thiosulfate resin
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A simple and efficient methodology for sequestering byproducts and excess starting reagent from the solution-phase Dess-Martin and Grieco-Dess- Martin periodinane mediated oxidation of primary or secondary alcohols to aldehydes or ketones is described. The periodinane oxidations are carried out under mild conditions followed by treatment with a novel thiosulfate resin which reduces any remaining I(V) and I(III) periodinane species to an I(I) species. Quantitative removal of the I(I) species from the solution is achieved by using a base functionalized resin followed by filtration and evaporation to afford highly pure aldehyde or ketone products. Utilization of this sequestration methodology for periodinane mediated oxidations allows for the high-throughput purification and work-up of parallel reaction chambers and is highly amenable to automation procedures.
- Parlow, John J.,Case, Brenda L.,South, Michael S.
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p. 6785 - 6796
(2007/10/03)
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- CHROMONE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND USE OF THE SAME
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A chromone derivative of the formula (I): STR1 wherein R. sup. 11 is a pyrazolyl, pyrrolyl, triazolyl, benzotriazolyl, benzimidazolyl, indazolyl, or indolyl group, R 2, R 3, R 4, and R 5 is independently a hydrogen or halogen atom, or a hydroxy or alkoxy group, or an alkoxy group substituted with one or more alkoxy groups, and X is an oxygen or sulfur atom, or a salt thereof is disclosed. The chromone derivative inhibits the activity of matrix metalloproteinase.
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- Oxidation of Alcohols with o-Iodobenzoic Acid (IBX) in DMSO: A New Insight into an Old Hypervalent Iodine Reagent
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The ultracentennial 10-I-4 iodinane oxide IBX (3; o-iodoxybenzoic acid; 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide) represents a new oxidizing reagent that successfully joins to the large family of known oxidants.IBX, in contrast to other valuable oxidants, is inexpensive to prepare and easy to handle, can tolerate moisture and water, and generally gives very good yields.Furthermore, IBX is mild and chemoselective (primary alcohols are converted into aldehydes with no overoxidation to acids; 1,2-diols are converted to α-ketols or α-diketones without oxidative cleavage; amino alcohols are oxidized to amino carbonyls, without protection of the amino group; sensitive heterocycles are not affected; various other functional groups are compatible with IBX oxidation).IBX is versatile (it works in various solvents and it is highly sensitive to temperature variations), and its solutions in DMSO are stable enough to carry out the oxidation reaction easily.
- Frigerio, Marco,Santagostino, Marco,Sputore, Simona,Palmisano, Giovanni
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p. 7272 - 7276
(2007/10/03)
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- ROLE OF THE POLYMER BACKBONE IN THE OXIDATIVE PROPERTIES OF POLYMER - SUPPORTED DICHROMATE
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Crosslinked co/poly(styrene-4-vinylpyridine)/ (1) was converted with hydrogen bromide or alkyl bromide to a pyridinium salt (2) which was further converted in water medium to various immobilized dichromates (3) with CrO3.The insoluble reagent containing 0.6 -1.0 mmol of dichromate on a gram of resin (depending on the structure of the polymer backbone) oxidized several secondary alcohols to ketones.The rate of conversion of alcohols to ketones depended on the structure of the polymer backbone, the structure of the alcohol, and the amount of water (5percent or 20percent) occluded in the reagent 3.
- Zdravkovski, Zoran,Zupan, Marko
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p. 1317 - 1324
(2007/10/02)
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- Dihydrobenzo(B)thiophenes and pharmaceutical compositions thereof useful as antifungals
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2-Alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-2-(1H-azolyl(C1 -C2)alkyl)benzo[b]thiophenes especially 2-alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-3-hydroxy-2-(1H-1-imidazolylmethyl)-4-,5-,6- and 7-halobenzo[b]thiophenes and related derivatives having antifungal activity are disclosed. Pharmaceutical compositions comprising compounds of the invention and their use in treating fungal infections in susceptible hosts such as humans are also disclosed.
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- 2,3-Dihydro-2-(imidazolylmethyl)benzo(b)thiophenes
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This invention relates to 2,3-dihydro-2-(imidazolylmethyl)benzo(b)thiophenes, to intermediates useful in their preparation, and to processes for preparing said intermediates. Also included in the invention are pharmaceutical compositions and the method of use of the compounds as antifungal agents.
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- A general route to the synthesis of 3-alkylidene derivatives of 4-thiochromanone 1,1-dioxide
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The reactions of the trimethylsilyl enol ethers of both 4-thiochromanone and 4-thiochromanone 1,1-dioxide with various carbonyl compounds complexed with titanium tetrachloride give moderate yields of the previously unknown 3-alkylidene condensation products under mild conditions.Other Lewis acids, with the exception of boron trifluoride, were found to be ineffective in this transformation.
- Still, Ian W. J.,Ablenas, Fred J.
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p. 2535 - 2539
(2007/10/02)
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