- Copper-Catalyzed Asymmetric Three-Component Borylstannation: Enantioselective Formation of C-Sn Bond
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In summary, a first copper-catalyzed synthesis of α-aryl-β-borylstannane compounds was accomplished through three-component borylstannation of aryl-substituted alkenes. In the exploration of an asymmetric variant, chiral sulfinylphosphine ligands proved a
- Jia, Tao,Cao, Peng,Wang, Ding,Lou, Yazhou,Liao, Jian
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Read Online
- PROCESS FOR PRODUCTION OF HYDROXYTYROSOL USING ORGANOMETALLIC COMPOUNDS
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Disclosed is a process for the production of a 4-(2-hydroxyalkyl)-1,2-benzenediol, comprising the steps of (a) providing protected 1,2-benzenediol having the 1,2-hydroxyl groups protected, (b) halogenating the protected 1,2-benzenediol to obtain a protected 4-halo-1,2-benzenediol having the 1,2-hydroxyl groups protected, (c) reacting, in the presence of a metal or organometallic compound, the protected 4-halo-1,2-benzenediol to protected 4-(2-hydroxyalkyl)-1,2-benzenediol having the 1,2-hydroxyl groups protected, and (d) deprotecting the protected 4-(2-hydroxyalkyl)-1,2-benzenediol to obtain the 4-(2-hydroxyalkyl)-1,2-benzenediol. Also disclosed is the use of 1,2-benzenediol for the production of hydroxytyrosol.
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Page/Page column 16-17
(2012/02/02)
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- Cu(II)-impregnated sulfated MCM-41: An efficient and convenient protocol for the synthesis of 1,3-benzodioxoles
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An efficient synthesis of 1,3-benzodioxoles was achieved from catechol with different aldehydes and ketones using Cu(II) impregnated sulfated MCM-41 as an efficient and reusable catalyst. Copyright Taylor & Francis Group, LLC.
- Sivakumar,Ramesh,Lalitha
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experimental part
p. 91 - 93
(2011/03/23)
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- Microwave-assisted synthesis of 1,3-benzodioxole derivatives from catechol and ketones or aldehydes
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An efficient synthetic procedure for the preparation of a diverse library of 1,3-benzodioxoles was developed by applying controlled microwave heating in comparison with currently available conventional heating. Reactions were completed in less than 3 h. The isolation of product is simple, the isolated yields are good to excellent, and this method is applicable to large scale production.
- Pingali, Subramanya R.K.,Jursic, Branko S.
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experimental part
p. 4371 - 4374
(2011/09/19)
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- Diallylation of 2,2-dialkylbenzodioxoles from TiCl4-mediated allylsilane reaction
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Reaction of aliphatic ketones with catechol afforded 2,2-dialkylbenzodioxoles. Treatment of these benzodioxoles with allyltrimethylsilane in the presence of titanium tetrachloride led to 4,4-dialkylhepta-1,6-dienes resulting from a diallylation process. R
- Galy, Nicolas,Moraleda, Delphine,Santelli, Maurice
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body text
p. 5238 - 5240
(2009/12/06)
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- NEW PHARMACEUTICAL COMPOUNDS
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Compounds of formula (I), wherein R1-R4, X, Y and Z are as defined in claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.
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Page/Page column 40
(2008/06/13)
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- (4-PIPERIDINYL)-1H-2-BENZOPYRAN DERIVATIVES USEFUL AS ANTIPSYCHOTIC AGENTS
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The present invention comprises (4-Piperidinyl)-1H-2-Benzopyran derivatives useful as antipsychotic agents, their intermediates, pharmaceutical compositions and methods of making these compounds. These compounds are useful in treating psychosis.
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- An efficient and convenient method for preparation of 2,2-disubstituted and 2-monosubstituted 1,3-benzodioxoles from ketones and aldehydes with catechol catalysed by zro2/so42-
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The title compounds have been synthesised by reaction of catechol with ketones and aldehydes catalysed by ZrO2/SO42- solid superacid in high yields. Ketones gave better yields than aldehydes.
- Jin,Zhang,Wang,Guo,Li
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p. 289 - 291
(2007/10/03)
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- (4-PIPERIDINYL)-1H-2-BENZOPYRAN DERIVATIVES USEFUL AS ANTIPSYCHOTIC AGENTS
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The present invention comprises (4-Piperidinyl)-1H-2-Benzopyran derivatives useful as antipsychotic agents, their intermediates, pharmaceutical compositions and methods of making these compounds. These compounds are useful in treating psychosis.
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- Asymmetric Diels-Alder reaction of optically active 3-(3,3,3- trifluoropropenylsulfonyl)oxazolidine: Synthesis of (8R)8-trifluoromethyl-2- oxa-6-thia-5-azatricyclo[5.2.2.01,5]-undecane-6,6-dioxide
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Asymmetric Diels-Alder reaction of optically active 3-(3,3,3- trifluoropropenylsulfonyl)-1,3-oxazolidine (1) with several dienes gave adducts regio- and stereoselectively in 69 - 78% de. Acetalization of 2- methoxybutadiene adduct with catechol gave tricy
- Okano, Takashi,Nagai, Tomoyuki,Eguchi, Shoji,Kimoto, Hiroshi
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- Montmorillonite clay catalysis. Part 14. A facile synthesis of 2-substituted and 2,2-disubstituted 1,3-benzodioxoles
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A series of 2-substituted and 2,2-disubstituted 1,3-benzodioxoles have been synthesised by reaction of catechol and pyrogallol with corresponding aldehydes and ketones catalysed by montmorillonite KSF or K-10. The reactions are completed within 2.7-24 h to give satisfactory yields. Ketones give better yields than aldehydes, although highly sterically hindered ketones and diaryl ketones fail to react at all.
- Li, Tong-Shuang,Li, Li-Jun,Lu, Bo,Yang, Feng
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p. 3561 - 3564
(2007/10/03)
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- Synthesis of compounds of interest in proton transfer spectroscopy
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A new series of compounds has been prepared for use in proton transfer spectroscopy. The complexes 6a-6d have been converted into the fully characterised perchlorates 7a-7d and the corresponding anhydro bases 8a-8d.
- Barton,Ozbalik,Sas
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p. 8043 - 8052
(2007/10/02)
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- A Novel Highly Stereoselective Synthesis of Tetrahydrodibenzo-1,4-dioxanes
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The cis- and trans-tetrahydrodibenzo-1,4-dioxanes 2 and 3 were synthesized from 2-bromocyclohexanone in five steps. - Key Words: Dichotomy in SN2 reactions / 1,4-Benzodioxanes, potential biological activity of
- Antus, Sandor,Baitz-Gacs, Eszter,Snatzke, Guenter,Toth, Tamas S.
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p. 1017 - 1020
(2007/10/02)
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- Comparative Toxicities and Analgesic Activities of Three Monomethylated Analogues of Acetaminophen
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Three monomethylated derivatives of 4'-hydroxyacetanilide (acetaminophen) were prepared in order to compare their cytotoxic potential and analgesic activity with that of acetaminophen.Only 4'-hydroxy-methylacetanilide (N-methylacetaminophen) was devoid of cytotoxic effects to hepatic tissue of mice.Results of comparative tissue distribution studies and metabolism studies both in vivo and in vitro in mice indicate that the disposition of N-methylacetaminophen is similar to that of acetaminophen except that it is not oxidized to a toxic metabolite.In contrast, 3'-methyl-4'-hydroxyacetanilide (3-methlacetaminophen) is as hepatotoxic as acetaminophen in mice while 2'-methyl-4'-hydroxyacetanilide (2-methylacetaminophen) is less hepatotoxic.The analgesic potency of the analogues seems to parallel their hepatotoxic potential, and both activities parallel the oxidation potentials in this series of compounds.
- Harvison, Peter J.,Forte, Anthony J.,Nelson, Sidney D.
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p. 1737 - 1743
(2007/10/02)
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- Antioxidant benzodioxole compound
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Novel antioxidant compounds for use in foodstuffs containing oils or fats are described which comprise benzodioxole compounds having the structure STR1 wherein R1 is a hydrogen atom or an alkyl group or an aryl group, R2 is an alkyl group or an aryl group, or R1 and R2 together form a cyclo alkyl group, and R3 is a hydrogen atom or an hydroxyl group.
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- An Improved Method for the Synthesis of 2,2-disubstituted and 2-Monosubstituted 1,3-Benzodioxoles
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The reactions of catechol with ketones and aldehydes have been studied and convenient procedures have been developed for the preparation of the title compounds in high yields.These products undergo virtually quantitative nitration at position 5, thus providing a source of derivatives substituted in the benzene ring.
- Cole, Edward R.,Crank, George,Minh, H. T. Hai
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p. 675 - 680
(2007/10/02)
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