- Catalytic removal of tert-butyldimethylsilyl (TBS) ether by PVP-I
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A mild, efficient and rapid protocol the deprotection of alcoholic TBDMS ethers using PVP-1 as catalyst in methanol, the procedure of deprotection of various TBDMS ethers were found to be very convenient, easy work-up, high yielding.
- Ke, Yanxiong,Lu, Guangying,Ren, Jiangmeng,Wang, Di,Zeng, Bu-Bing
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- Copper-Catalyzed Cascade Cyclization of Indolyl Homopropargyl Amides: Stereospecific Construction of Bridged Aza-[n.2.1] Skeletons
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Catalytic cycloisomerization-initiated cascade cyclizations of terminal alkynes have received tremendous interest, and been widely used in the facile synthesis of a diverse array of valuable complex heterocycles. However, these tandem reactions have been mostly limited to noble-metal catalysis, and are initiated by an exo-cyclization pathway. Reported herein is an unprecedented copper-catalyzed endo-cyclization-initiated tandem reaction of indolyl homopropargyl amides, where copper catalyzes both the hydroamination and Friedel–Crafts alkylation process. This method allows the practical and atom-economical synthesis of valuable bridged aza-[n.2.1] skeletons (n=3–6) with wide substrate scope, and excellent diastereoselectivity and enantioselectivity by a chirality-transfer strategy. Moreover, the mechanistic rationale for this novel cascade cyclization is also strongly supported by control experiments, and is distinctively different from the related gold catalysis.
- Tan, Tong-De,Zhu, Xin-Qi,Bu, Hao-Zhen,Deng, Guocheng,Chen, Yang-Bo,Liu, Rai-Shung,Ye, Long-Wu
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supporting information
p. 9632 - 9639
(2019/06/27)
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- 1,2,5-oxadiazole derivative used as indoleamine 2,3-dioxygenase inhibitor
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The invention belongs to the technical field of 1,2,5-oxadiazole derivatives, and particularly relates to a 1,2,5-oxadiazole derivative or a pharmaceutically acceptable salt thereof which is used as an indoleamine 2,3-dioxygenase inhibitor. The structure of the 1,2,5-oxadiazole derivative or the pharmaceutically acceptable salt thereof used as the IDO inhibitor is shown in the following formula I.The invention provides a general formula compound I with a novel structure. Experimental results show that some compounds have excellent IDO inhibitory activity and permeation performance at the sametime. The compound is expected to be marketed as a tumor molecular immunotherapeutic drug for cancer treatment.
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Paragraph 0113-0116
(2019/10/01)
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- Method for preparing D-(+)-alpha-(2-thiopheneethylamino)-alpha-(2-chlorophenyl)methyl acetate hydrochloride
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The invention provides a novel method for preparing D-(+)-alpha-(2-thiopheneethylamino)-alpha-(2-chlorophenyl)methyl acetate hydrochloride, aiming at solving the technical problems of a traditional synthesis technology of the D-(+)-alpha-(2-thiopheneethylamino)-alpha-(2-chlorophenyl)methyl acetate hydrochloride that the technology is complicated, the cost is high and the yield is low. The method comprises the following steps: 1) preparing 2-bromothiophene; 2) preparing 2-thiopheneethanol; 3) preparing 2-thiopheneethanol p-toluenesulfonate; 4) preparing L-(+)-o-chlorophenylglycine methyl esterL-tartrate; 5) preparing the D-(+)-alpha-(2-thiopheneethylamino)-alpha-(2-chlorophenyl)methyl acetate hydrochloride. The preparation method provided by the invention is low in cost, high in yield andhigh in safety and is suitable for industrial production.
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Paragraph 0009; 0057; 0064; 0066; 0075; 0082; 0093; 0102
(2018/12/14)
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- Selective ligand-free cobalt-catalysed reduction of esters to aldehydes or alcohols
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Cobalt(ii) salts combined with NaBHEt3 and eventually a base catalyse efficiently and selectively the reduction of esters to aldehydes or alcohols through hydrosilylation by using phenylsilane. Catalyst characterisation by XRD, XPS, TEM and STEM analyses indicates the materials were partially crystalline with the presence of cobalt nanoparticles. Control experiments suggested low valent Co(0) was the active catalytic species involved.
- Rysak, Vincent,Descamps-Mandine, Armel,Simon, Pardis,Blanchard, Florent,Burylo, Laurence,Trentesaux, Martine,Vandewalle, Maxence,Collière, Vincent,Agbossou-Niedercorn, Francine,Michon, Christophe
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p. 3504 - 3512
(2018/07/29)
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- Structure-Odor Correlations in Homologous Series of Mercapto Furans and Mercapto Thiophenes Synthesized by Changing the Structural Motifs of the Key Coffee Odorant Furan-2-ylmethanethiol
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Furan-2-ylmethanethiol (2-furfurylthiol; 2-FFT, 1) is long-known as a key odorant in roast and ground coffee and was also previously identified in a wide range of thermally treated foods such as meat, bread, and roasted sesame seeds. Its unique coffee-like odor quality elicited at very low concentrations, and the fact that only a very few compounds showing a similar structure have previously been described in foods make 1 a suitable candidate for structure-odor activity studies. To gain insight into the structural features needed to evoke a coffee-like odor at low concentrations, 46 heterocyclic mercaptans and thio ethers were synthesized, 32 of them for the first time, and their odor qualities and odor thresholds were determined. A movement of the mercapto group to the 3-position kept the coffee-like aroma but led to an increase in odor threshold. A separation of the thiol group from the furan ring by an elongation of the carbon side chain caused a loss of the coffee-like odor and also led to an increase in odor thresholds, especially for ω-(furan-2-yl)alkane-1-thiols with six or seven carbon atoms in the side chain. A displacement of the furan ring by a thiophene ring had no significant influence on the odor properties of most of the compounds studied, but the newly synthesized longer-chain 1-(furan-2-yl)- and 1-(thiophene-2-yl)alkane-1-thiols elicited interesting passion fruit-like scents. In total, only 4 out of the 46 compounds also showed a coffee-like odor quality like 1, but none showed a lower odor threshold. Besides the odor attributes, also retention indices, mass spectra, and NMR data of the synthesized compounds were elaborated, which are helpful in possible future identification of these compounds in trace levels in foods or other materials.
- Schoenauer, Sebastian,Schieberle, Peter
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p. 4189 - 4199
(2018/05/01)
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- A Versatile Iridium(III) Metallacycle Catalyst for the Effective Hydrosilylation of Carbonyl and Carboxylic Acid Derivatives
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A versatile iridium(III) metallacycle catalysed rapidly and selectively the reduction of a large array of challenging esters and carboxylic acids as well as various ketones and aldehydes. The reactions proceeded in high yields at room temperature by hydrosilylation followed by desilylation. Although the reactions of various aldehydes and ketones resulted exclusively in alcohols, the hydrosilylation of esters led to alcohols or ethers, depending on the type of substrate. Regarding the carboxylic acids, again the nature of the reagent controlled the outcome of the hydrosilylation reaction, either alcohols or aldehydes being formed.
- Corre, Yann,Rysak, Vincent,Trivelli, Xavier,Agbossou-Niedercorn, Francine,Michon, Christophe
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supporting information
p. 4820 - 4826
(2017/09/07)
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- Nucleophilic addition of arylmethylzinc reagents (ArCH2ZnCl) to formaldehyde: An easy access to 2-(hetro)arylethyl alcohols
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The selective addition of arylmethylmagnesium halides with formaldehyde giving arylethyl alcohols is extremely challenging. To circumvent the difficulties, in the current communication, we have reported on the nucleophilic addition of benzyl zinc reagents derived from inexpensive and abundant benzyl chlorides to paraformaldehyde. The reaction investigated herein is hitherto unknown and was found to be selective, operationally simple, atom- and step-economical and high yielding to deliver phenethyl alcohols utilized as key perfumery ingredients in 60–83% yields. After successful establishment of the reaction condition, the reaction was also scaled up successfully to deliver a large-scale preparation of the phenethyl alcohol.
- Bhatt,Samant,Pednekar, Suhas
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supporting information
p. 968 - 974
(2017/05/04)
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- One-Carbon Homologation of Primary Alcohols and the Reductive Homologation of Aldehydes Involving a Jocic-Type Reaction
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(Trichloromethyl)carbinols, which are formed in one operation from either alcohols or aldehydes, can be converted into primary alcohols in a Jocic-type reaction involving LiBH4. The net result is a convenient two-step, one-carbon homologation of primary alcohols or a reductive one-carbon homologation of aldehydes featuring a broad substrate scope. The method is step-economical, and it nicely complements established one-carbon homologation strategies. (Trichloromethyl)carbinols, which are formed in one operation from either alcohols or aldehydes, can be converted into primary alcohols in a Jocic-type reaction involving LiBH4. The net result is a convenient two-step, one-carbon homologation of primary alcohols or a reductive one-carbon homologation of aldehydes featuring a broad substrate scope.
- Li, Zhexi,Gupta, Manoj K.,Snowden, Timothy S.
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p. 7009 - 7019
(2015/11/16)
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- Highly efficient and chemoselective zinc-catalyzed hydrosilylation of esters under mild conditions
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A mild and highly efficient catalytic hydrosilylation protocol for room-temperature ester reductions has been developed using diethylzinc as the catalyst. The methodology is operationally simple, displays high functional group tolerance and provides for a facile access to a broad range of different alcohols in excellent yields.
- Kovalenko, Oleksandr O.,Adolfsson, Hans
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supporting information
p. 2785 - 2788
(2015/02/05)
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- Biocatalysed reduction of carboxylic acids to primary alcohols in aqueous medium: A novel synthetic capability of the zygomycete fungus Syncephalastrum racemosum
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Abstract The zygomycete fungus Syncephalastrum racemosum shows the remarkable capability of reducing carboxylic acids to primary alcohols in water medium, at ambient temperature and pressure. The reaction does not require molecular hydrogen, and in most cases affords quantitative transformations. The results herein reported highlight the basic molecular scaffold that can be accepted by the fungus, the effects due to substituents, and also the possibility that carboxylic acids can be generated in the reaction medium by enzymatic hydrolysis of the corresponding methyl esters. This biocatalysed reduction implements the scarcely supplied enzymatic toolbox for the conversion of carboxylic groups into primary alcohols, which can be exploited for the optimisation of sustainable synthetic procedures.
- Brenna, Elisabetta,Cannavale, Flavia,Crotti, Michele,Parmeggiani, Fabio,Romagnolo, Alice,Spina, Federica,Varese, Giovanna Cristina
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- Selective switchable iron-catalyzed hydrosilylation of carboxylic acids
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Selective reduction of carboxylic acids either to aldehydes or alcohols is achieved using a one pot procedure based on iron-catalyzed hydrosilylations. Using phenylsilane and (COD)Fe(CO)3 catalyst under UV-irradiation at rt, alcohols were obtained specifically in good yields, whereas aldehydes were selectively obtained using TMDS and (t-PBO)Fe(CO)3 catalyst under thermal activation.
- Misal Castro, Luis C.,Li, Haoquan,Sortais, Jean-Baptiste,Darcel, Christophe
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supporting information
p. 10514 - 10516,3
(2020/09/02)
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- Iron-catalyzed hydrosilylation of esters
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The first hydrosilylation of esters catalyzed by a well defined iron complex has been developed. Esters are converted to the corresponding alcohols at 100 °C, under solvent-free conditions and visible light activation. Copyright
- Bezier, David,Venkanna, Gopaladasu T.,Castro, Luis C. Misal,Zheng, Jianxia,Roisnel, Thierry,Sortais, Jean-Baptiste,Darcel, Christophe
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supporting information; experimental part
p. 1879 - 1884
(2012/09/22)
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- Microwave-assisted synthesis of 5-substituted 2-aminothiophenes starting from arylacetaldehydes
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An easy three-step pathway for the synthesis of arylacet-aldehydes from the corresponding carboxylic acids in very high yields is described. Their use as precursors of 5-substituted-2-aminothiophenes is illustrated via a microwave-assisted Gewald reaction. This method allows obtaining the expected compounds in a shorter time and with better yields and purities than the classical procedures. Georg Thieme Verlag Stuttgart - New York.
- Revelant, Germain,Dunand, Sandrine,Hesse, Stephanie,Kirsch, Gilbert
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experimental part
p. 2935 - 2940
(2011/11/01)
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- InBr3-catalyzed deoxygenation of carboxylic acids with a hydrosilane: Reductive conversion of aliphatic or aromatic carboxylic acids to primary alcohols or diphenylmethanes
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A simple and practical procedure for the direct reduction of aliphatic carboxylic acids with a variety of functional groups to a primary alcohol using the mild reducing reagent tetramethyldisiloxane (TMDS), in the presence of a catalytic amount of InBr3 has been developed. This simple reducing system, when used together with a hydrosilane, allows the preparation of the diphenylmethane derivative directly from an aromatic carboxylic acid and an aromatic compound. Copyright
- Sakai, Norio,Kawana, Keita,Ikeda, Reiko,Nakaike, Yumi,Konakahara, Takeo
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experimental part
p. 3178 - 3183
(2011/06/28)
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- Zinc-catalyzed chemoselective reduction of esters to alcohols
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Economical alcohols! A general and chemoselective catalytic reduction of esters to alcohols using inexpensive zinc acetate and silanes has been developed. The operational simplicity and the high functional group tolerance, without the need for protecting and deprotecting steps, make this procedure particularly attractive for organic synthesis. Copyright
- Das, Shoubhik,Moeller, Konstanze,Junge, Kathrin,Beller, Matthias
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experimental part
p. 7414 - 7417
(2011/08/05)
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- Investigation of the aroma-active compounds formed in the maillard reaction between glutathione and reducing sugars
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Aroma-active compounds formed during the thermal reaction between glutathione (GSH) and reducing sugars were analyzed by gas chromatography-mass spectrometry (GC-MS) and GC-olfactometry (GC-O) with aroma extract dilution analysis (AEDA). Application of AEDA to glutathione Maillard reaction products (GSH MRPs) led to the identification of 19 aroma-active compounds in the thermal reaction of glutathione with glucose or fructose. In addition, the carbohydrate module labeling (CAMOLA) approach was also employed to elucidate the formation pathways for selected target sulfur aroma compounds, such as 5-methylthiophene-2-carbaldehyde and 3-methylthiophene-2-carbaldehyde, which have not been reported previously. The intact carbon skeleton of glucose via 3-deoxyhexosone is incorporated into 5-methylthiophene-2-carbaldehyde with the hydrogen sulfide of GSH. On the other hand, the formation of 3-methylthiophene2-carbaldehyde may occur via the recombination of a C-4 sugar fragment and mercaptoacetaldehyde.
- Lee, Sang Mi,Jo, Ye-Jin,Kim, Young-Suk
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experimental part
p. 3116 - 3124
(2011/08/05)
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- SUBSTITUTED 4-AMINO-PIPERIDINES
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The present invention relates to new substituted 4-amino-piperidine opioid receptor modulators, pharmaceutical compositions thereof, and methods of use thereof
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Page/Page column 26
(2010/02/17)
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- Novel, one-pot procedure for the synthesis of 2-arylethanol derivatives
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An efficient one-pot synthesis of 2-arylethanol derivatives using ethylene sulfate as a C2 building block is described. High yields are obtained upon trapping of aryllithium intermediates generated by halogen-metal exchange or directed metalation with ethylene sulfate. The resulting heteroaryl or phenylethanol derivatives represent versatile building blocks for the synthesis of annulated pyran derivatives by oxa-Pictet-Spengler reaction.
- Schlaeger, Torsten,Oberdorf, Christoph,Tewes, Bastian,Wuensch, Bernhard
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p. 1793 - 1797
(2008/12/22)
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- Simple reduction of heteroaromatic esters to alcohols using a sodium borohydride-methanol system
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Some heteroaromatic esters were reduced to the corresponding alcohols by using a sodium borohydride-methanol system. The reduction was completed within 0.15-2.0 h in refluxing THF. The alcohol products were isolated after aqueous workup in moderate to excellent yield (48-97%). Copyright Taylor & Francis, Inc.
- Boechat, Nubia,Da Costa, Jorge Carlos Santos,De Souza Mendonca, Jorge,Paes, Karla Ceodaro,Fernandes, Elisa Lopes,De Oliveira, Pedro Santos Mello,Vasconcelos, Thatyana Rocha Alves,De Souza, Marcus Vinicius Nora
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p. 3187 - 3190
(2007/10/03)
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- Method for preparing a thiopene derivative
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The invention relates to a process for preparing 2-thienyl-2-ethanol, in which:a) thiophene is metallated using an alkali metal, in the presence of an electron transfer agent,b) the compound obtained is treated with ethylene oxide,c) the thienyl derivative thus formed is hydrolyzed, to give the desired compound.2-Thienyl-2-ethanol is a synthetic intermediate.
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Page/Page column 3-4
(2010/11/30)
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- Smiles-type free radical rearrangement of aromatic sulfonates and sulfonamides: Syntheses of arylethanols and arylethylamines
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Smiles-type free radical rearrangements of arenesulfonates and arenesulfonamides are exploited for synthetic purposes. 4-Substituted benzenesulfonates cause Smiles-type rearrangement only when substituted by an electron withdrawing group. Therefore, ipso-sttack by an alkyl radical on arenesulfonates takes place in an electrophilic manner. Arenesulfonamides rearrange only when the amide nitrogen is substituted by an alkoxycarbonyl group, due to the electron withdrawing nature of this group. Sulfonates and the N-ethoxycarbonylsulfonamide derivatives of naphthalene, quinoline, and thiophene cause more rearrangement and show synthetic utility. Aromatic amino acid analogues were synthesized by Smiles-type rearrangement with moderate yields. The radical Smiles-type rearrangement of sulfonate and sulfonamide derivatives can be a useful synthetic route when we understand the electronic character of these reactions.
- Tada, Masaru,Shijima, Hiroyasu,Nakamura, Masaharu
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p. 2499 - 2505
(2007/10/03)
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- 2-substituted-(2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1- yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 1. Effects of alkyl, arylalkyl, and diarylalkyl substitution
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In this paper, we describe the synthesis of a series of α-substituted analogues of the potent and selective group II metabotropic glutamate receptor (mGluR) agonist (1S,1'S,2'S)-carboxy-cyclopropylglycine (2, L-CCG 1). Incorporation of a substituent on the amino acid carbon converted the agonist 2 into an antagonist. All of the compounds were prepared and tested as a aeries of four isomers, i.e., two racemic diastereomers. We explored alkyl substitution, both normal and terminally branched; phenylalkyl and diphenylalkyl substitution; and a variety of aromatic and carbocyclic surrogates for phenyl. Affinity for group II mGluRs was measured using [3H]glutamic acid (Glu) binding in rat forebrain membranes. Antagonist activity was confirmed for these compounds by measuring their ability to antagonize (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin-stimulated cyclic-AMP in RGT cells transfected with human mGluR2 and mGluR3. We found that while alkyl substitution provided no increase in affinity relative to 2, phenylethyl and diphenylethyl substitution, as in 105 and 109, respectively, were quite beneficial. The affinity of 109 was further enhanced when the two aromatic rings were joined by an oxygen or sulfur atom to form the tricyclic xanthylmethyl and thioxanthylmethyl amino acids 113 and 114, respectively. Amino acid 113, with an IC50 of 0.010 μM in the [3H]Glu binding assay, was 52-fold more potent than 2, whose IC50 was 0.47 μM.
- Ornstein, Paul L.,Bleisch, Thomas J.,Arnold, M. Brian,Wright, Rebecca A.,Johnson, Bryan G.,Schoepp, Darryle D.
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p. 346 - 357
(2007/10/03)
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- Thienothiophenes. Part 2. Synthesis, metallation and bromine→lithium exchange reactions of thieno[3,2-b]thiophene and its polybromo derivatives
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Methods for the large-scale synthesis of thieno[3,2-b]thiophene [including a catalytic vapour-phase reaction (at 550°C) between 2-(2-thienyl)ethanol and carbon disulfide], its 2-carboxylic acid and its 3,6-dibromo and 2,3,5,6-tetrabromo derivatives are reported. With 2 mol equiv. of butyllithium thieno[3,2-6]thiophene gives its 2,5-dilithiated derivative and its 3,6-dibromo derivative gives the 3,6-dilithiated compound. By quenching with suitable electrophilic reagents these dilithiated compounds have been converted into various 2,5- or 3,6-disubstituted thieno[3,2-6]thiophenes, respectively. Likewise 2,3,5,6-tetrabromothieno[3,2-b]thiophene has been converted into 2,5-disubstituted 3,6-dibromothieno[3,2-b]thiophenes.
- Fuller, Lance S.,Iddon, Brian,Smith, Kevin A.
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p. 3465 - 3470
(2007/10/03)
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- An Inexpensive Air-Stable Titanium-Based System for the Conversion of Esters to Primary Alcohols
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Polymethylhydroxiloxane, when combined with titanium(IV) isopropoxide, provides a convenient system for the conversion of esters to the corresponding primary alcohols in the presence of a wide range of functional groups.Reactions are carried out as mixtures of the neat reaction components; workup with aqueous alkaline THF affords primary alcohols in good to excellent yields.The system tolerates primary alkyl bromides and iodides, olefins, epoxides, and alkynes.Steric differentiation of methyl and tert-butyl esters is also possible.The results observed in the parent and related reactions argue against pathways involving Lewis-acid catalysis and anionic hydridosilicate-mediated reductions, and instead support a neutral titanium hydride complex or strongly associated titanium/silane complex as the active reducing agent.
- Reding, Matthew T.,Buchwald, Stephen L.
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p. 7884 - 7890
(2007/10/03)
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- Catalytic reduction of organic carbonyls using metal catalysts
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A process is provided whereby organic carbonyl substrates, including esters, lactones, ketones, amides and imides are reduced in a reaction with a silane reducing reagent and a catalyst. Exemplary catalysts include metal alkoxides and metal aryloxides.
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- An Air-Stable Catalyst System for the Conversion of Esters to Alcohols
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The combination of 5 mol percent of Ti(O-i-Pr)4 with 2.5-3.0 equiv (EtO)3SiH cleanly hydrosilylates esters to silyl ethers at 40-55 deg C, which can be converted to the corresponding primary alcohols via aqueous alkaline hydrolysis in excellent overall yield.The reaction can be carried out in the air, without solvent, and displays a high level of functional group compatibility.
- Berk, Scott C.,Buchwald, Stephen L.
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p. 3751 - 3753
(2007/10/02)
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- A New Reduction of Some Carboxylic Esters with Sodium Borohydride and Zinc Chloride in the Presence of a Tertiary Amine
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In the presence of a tertiary amine, sodium borohydride (NaBH4) combined with zinc chloride (ZnCl2) showed powerful reducing properties and carboxylic esters were smoothly reduced to their corresponding alcohols which were not obtained by reduction with NaBH4 and ZnCl2 alone.Tetrahydrofuran (THF) was an efficient solvent, and the effective molar ratio of the reducing agents, NaBH4:ZnCl2:tertiary amine, was 2:1:1.In particular, aminobenzoates such as anthranilic esters, were reduced to aminobenzyl alcohols with high yields without the addition of a tertiary amine.Further, it was also found that this combination reduced nitro, cyano, and amido groups to their corresponding amino groups.
- Yamakawa, Tomio,Masaki, Mitsuo,Nohira, Hiroyuki
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p. 2730 - 2734
(2007/10/02)
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- SYNTHESE DU DERIVES DU THIOPHENE SUBSTITUES EN POSITION 2 ET 5
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Six new potentially active drugs derivatives of 2,5-disubstituted thiophene are synthesized by a multistep procedure based on the reactivity of α sulfur carbanions: compounds 2, 3, 4 and 8 are symmetrical, substituted by identical functional groups, and compounds 10, 14 are non symmetrical.
- Garrigues, Bernard
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- Process for the preparation of thieno-pyridine derivatives
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This invention relates to a process for the preparation of thieno-pyridine derivatives having the structural formula: STR1 in which R1 represents an optionally substituted alkyl, aryl or aralkyl radical, and R2 and R3 represnt each hydrogen or a lower alkyl, aryl or heterocyclic radical, comprising: (a) reacting a derivative of the formula STR2 in which R2 and R3 are as defined for formula (I) and X represents hydrogen, or an alkali metal, or a radical Mg-Y in which Y represents halogen, with a halo-sulfonyl derivative having the formula: in which Hal represents halogen and R4 represents an optionally substituted alkyl, aryl or aralkyl group, to give a compound having the formula: STR3 (b) subsequently reacting the latter compound with an amine of the formula: in which R1 is as defined for the formula (I), to give a compound having the formula: STR4 and (c) subsequently cyclizing compound (VI) with formaldehyde to give the derivative of the formula (I).
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