- The Electrolytic Reduction of p-Substituted α-(Methylsulfinyl)-α-(methylthio)acetophenones in Acetonitrile
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p-Substituted α-(methylsulfinyl)-α-(methylthio)-acetophenones (1) exhibit on polarographic reduction, three wavwes.The two last waves corespond to the reductions of p-substituted α-(methylthio)acetophenones (2) and p-substituted acetophenones respectively
- Kunugi, Akira,Takahashi, Norimasa,Abe, Kyo,Hirai, Taketsugu
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- Rh/DuanPhos-Catalyzed Asymmetric Hydrogenation of β-Acetylamino Vinylsulfides: An Approach to Chiral β-Acetylamino Sulfides
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Rh/DuanPhos-catalyzed asymmetric hydrogenation of challenging β-acetylamino vinylsulfides has been developed, affording chiral β-acetylamino sulfides with high yields and excellent ee's (up to 99% ee). This novel methodology provides an efficient and concise synthetic route to chiral β-acetylamino sulfides. The potential utility of this protocol in the synthesis of Apremilast has also been disclosed.
- Gao, Wenchao,Lv, Hui,Zhang, Xumu
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p. 2877 - 2880
(2017/06/07)
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- One-pot preparation of arylethynyl sulfides and bis(arylethynyl) sulfides
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An efficient preparation for arylethynyl sulfides 1 and bis(arylethynyl) sulfides 2 has been accomplished through a one-pot, three-step strategy that starts from arylethanonyl sulfides and bis(arylethanonyl) sulfides, respectively, without the use of various terminal arylacetylenes as substrates. When lithium hexamethyldisilazane (LHMDS), ClP(O)(OEt)2, and LHMDS were sequentially added to a tetrahydrofuran solution of different substrates [arylethanonyl sulfides or bis(arylethanonyl) sulfides], 1 or 2 were obtained in moderate to good yields. The reaction procedure involves the formation of an enol phosphate and a subsequent base-induced elimination. An efficient preparation of arylethynyl sulfides 1 and bis(arylethynyl) sulfides 2 has been accomplished by a one-pot, three-step strategy that starts from arylethanonyl sulfides and bis(arylethanonyl) sulfides, respectively, to give 1 and 2 in moderate to good yields. The reaction mechanism involves the formation of an enol phosphate that undergoes a subsequent base-induced elimination. Copyright
- Su, Qiong,Zhao, Zi-Jian,Xu, Feng,Lou, Peng-Cai,Zhang, Kai,Xie, De-Xun,Shi, Lei,Cai, Qing-Yun,Peng, Zhi-Hong,An, De-Lie
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p. 1551 - 1557
(2013/04/23)
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- SULFUR CONTAINING PYRAZOLE-HETEROCYCLE DERIVATIVES AS CANNABINOID CB1 RECEPTOR ANTAGONISTS
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A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and
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Page/Page column 11
(2011/08/04)
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- Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern
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The cannabinoid CB1/CB2 receptor subtype selectivity in the 1,2-diarylimidazole-4-carboxamide series was boosted by fine-tuning its 5-substitution pattern. The presence of the 5-methylsulfonyl group in 11 led to a greater than ~840-f
- Lange, Jos H.M.,van der Neut, Martina A.W.,Borst, Alice J.M.,Yildirim, Mahmut,van Stuivenberg, Herman H.,van Vliet, Bernard J.,Kruse, Chris G.
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experimental part
p. 2770 - 2775
(2010/07/08)
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- SULFUR CONTAINING PYRAZOLE-HETEROCYCLE DERIVATIVES AS CANNABINOID CB1 RECEPTOR ANTAGONISTS
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A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-re
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Page/Page column 28
(2010/04/27)
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- SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS
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The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to me
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Page/Page column 8
(2008/06/13)
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- Rhodium(II)-mediated reactions of thiobenzoylketene S,N-acetals with α-diazo carbonyl compounds: Synthesis of 2-substituted 3-alkylamino-5-phenylthiophenes
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Treatment of 3-methylamino-3-methylsulfanyl-1-phenylpropenethione 1 with excess (2.5 equiv.) α-diazo carbonyl compounds such as α-diazoketones and α-diazoesters in the presence of a catalytic amount of Rh(II) acetate in CH2Cl2 at rt gave 2-acyl- or 2-aroyl-3-methylamino-5-phenylthiophenes and alkyl 3-methylamino-5-phenylthiophene-2-carboxylates, respectively, as major products along with 1-phenyl-2-methylsulfanylethanones. The formation of the major products indicates that the carbenes or carbenoids generated interact initially with the thione sulfur of 1.
- Song, Hyun Min,Kim, Kyongtae
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p. 2414 - 2417
(2007/10/03)
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- Biocidal alkyl-substituted-(hetero)aryl-ketoxime-O-ethers and the production method thereof
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This invention provides a series of alkyl-substituted-(hetero)aryl-ketoxime-o-ether compounds represented by the general formula (I), a series of intermediate ketones and oxime compounds represented by the general formula (II) and general formula (III), their production method and biological activities. The compounds represented by general formula (I) have excellent biological activity for controlling insects, fungi, and weeds. They show particularly high activity in insect pest control such as in agriculture, horticulture, flower cultivation, and hygiene field. The compounds represented by the general formula (I) have quick and persistent insecticidal activity, without harming the crops. The compounds represented by general formula (II) and (III) that serve as the intermediates also have fairly good biological activity.
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- N-aryl-3-aryl-4-substituted-4,5-dihydro-1H-pyrazole-1-carboxamides and methods of their production
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This invention relates to novel N-aryl-3-aryl-4-substituted-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.
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- A CONVENIENT GENERAL ACCESS TO α-SULFENYLATED ACETOPHENONES AND ALKANONES
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Friedel-Crafts acylation of arenes with methylthio- (1) or phenylthio-acetyl chloride (2) provides ready access to α-methylthio- or α-phenylthio-substituted acetophenones.The acyl chlorides 1 and 2 reacted also with organoaluminium reagents to give α-sulfenylated alkanones.
- Ishibashi, Hiroyuki,Takamuro, Iwao,Mizukami, Yo-ichi,Irie, Maki,Ikeda, Masazumi
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p. 443 - 452
(2007/10/02)
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- Alkadiene derivatives, their preparation, and pharmaceutical compositions containing them
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Substituted alkadienes of the formula: STR1 in which R1 is hydroxy or acetoxy, R2 is hydrogen, carboxy, alkoxycarbonyl, phenyl or benzoyl, and R3 is alkylthio or alkoxy and R4 is naphthoyl or optionally substituted benzoyl, or R3 is alkoxycarbonyl, cycloalkyloxycarbonyl or cyano and R4 is alkyl, naphthyl, optionally substituted phenyl, alkylthio, naphthylmethanethio, optionally substituted benzylthio, optionally substituted phenylthio, naphthylthio, phenethylthio or allylthio, or R3 and R4 form, with the carbon atom to which they are attached, a ring-system of formula: STR2 in which R5 is hydrogen or alkoxy and X is methylene or S inhibit 5-lipoxygenase and are useful, for example, as anti-inflammatories.
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