- Atropisomeric Properties of 9-Methyl-1,4-benzodiazepin-2-ones
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The atropisomeric and conformational properties of 1,4-benzodiazepin-2-ones were investigated by freezing the conformation with a methyl group at the C9 of 1,4-benzodiazepine. It was revealed that 1,4-benzodiazepin-2-ones exist only as a pair of enantiome
- Tanaka, Ryoko,Makino, Kosho,Tabata, Hidetsugu,Oshitari, Tetsuta,Natsugari, Hideaki,Takahashi, Hideyo
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p. 4682 - 4688
(2021/09/08)
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- HERBICIDAL COMPOUNDS
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The present invention relates to herbicidally active cinnolinium derivatives and formulations comprising such derivatives. The invention further extends to herbicidal mixtures comprising a cinnolinium derivative as described herein and at least one additional herbicidal active ingredient. The use of the afore-mentioned cinnolinium derivatives, formulations and/or herbicidal mixtures in controlling undesirable plant growth: in particular the use for the post-emergence control of weeds, also falls within the scope of the present invention.
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Page/Page column 31
(2020/10/28)
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- COMPOUNDS
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Provided are benzoxazolinone sulfonamide derivatives that inhibit Na v1.7 activity, pharmaceutical compositions containing them and their use in therapy for the treatment of diseases mediated by Na v1.7 activity.
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Page/Page column 38
(2018/12/03)
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- Photo-Fries rearrangement of aryl acetamides: Regioselectivity induced by the aqueous micellar green environment
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Photochemical reactions tend to give more than one photoproduct. However, such a reaction can be a powerful synthetic tool when it is possible to conduct it in regioselective conditions yielding a single photoproduct. Water-surfactant solutions as reaction media can be considered as an approach in this context because they show products with different features than those from isotropic solutions. Here we describe results obtained from studying the effect on the prototypical photoreaction, known as the photo-Fries reaction of several substituted acetanilides and α-naphthyl acetamide within surfactant micelles (ionic and non-ionic micelles). This reaction involves homolytic cleavage of a C-N bond to yield a singlet radical pair. The surfactant micelles control the rotational and translational mobility of the radical pair, resulting in noticeable photoproduct selectivity.
- Iguchi, Daniela,Erra-Balsells, Rosa,Bonesi, Sergio M.
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p. 105 - 116
(2016/01/20)
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- Preparation of an N-sec-alkyl 2,6-disubstituted aniline: a key intermediate in the divergent synthesis of S-Metolachlor metabolites
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A simple method to prepare a 2,6-disubstituted aniline containing a N-sec-alkyl group and a carbonyl on one ortho substituent is reported. This method was used to accomplish the first synthesis of side chain oxidized ethylsulfonic acid (ESA) and oxanilic acid (OXA) metabolites of S-Metolachlor (S-Moc) herbicide. The 2,6-disubstituted aniline functionality was installed by a Sugasawa reaction of readily available ortho-toluidine. The N-sec alkyl group was introduced by a Mitsunobu alkylation of the nosyl-activated 2-acetyl-6-methyl-substituted aniline. This crucial step enabled access to the key 2,6-disubstituted aniline intermediate which was used in the divergent synthesis of S-Moc metabolites. A bioinspired synthesis of the keto-ESA metabolite was achieved in one step from the hydroxyl-ESA metabolite using a ruthenium-catalyzed oxidation.[Figure presented]
- Tyagi, Sameer,Gichinga, Moses G.,Cook, Christopher D.,Key, Jeffrey A.,McKillican, Bruce P.,Eberle, William J.,Carlin, Timothy J.,Hunt, David A.,Dowling, Alan J.
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p. 5363 - 5367
(2016/11/16)
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- Effects of structural modifications on the metal binding, anti-amyloid activity, and cholinesterase inhibitory activity of chalcones
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As the number of individuals affected with Alzheimer's disease (AD) increases and the availability of drugs for AD treatment remains limited, the need to develop effective therapeutics for AD becomes more and more pressing. Strategies currently pursued include inhibiting acetylcholinesterase (AChE) and targeting amyloid-β (Aβ) peptides and metal-Aβ complexes. This work presents the design, synthesis, and biochemical evaluation of a series of chalcones, and assesses the relationship between their structures and their ability to bind metal ions and/or Aβ species, and inhibit AChE/BChE activity. Several chalcones were found to exhibit potent disaggregation of pre-formed N-biotinyl Aβ1-42 (bioAβ42) aggregates in vitro in the absence and presence of Cu2+/Zn2+, while others were effective at inhibiting the action of AChE.
- Fosso, Marina Y.,LeVine, Harry,Green, Keith D.,Tsodikov, Oleg V.,Garneau-Tsodikova, Sylvie
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supporting information
p. 9418 - 9426
(2015/09/15)
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- QUINAZOLINE DERIVATIVES AS PDE10A ENZYME INHIBITORS
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This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The pr
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Page/Page column 54; 55
(2013/04/24)
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- Selenium-promoted intramolecular oxidative amidation of 2-(arylamino)acetophenones for the synthesis of N-arylisatins
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A convenient method for the synthesis of N-arylisatins from 2-(arylamino)acetophenones by using SeO2 as an oxidant is described. Various substituted N-arylisatins were selectively obtained in good to excellent yields. The reaction tolerates a wide range of functionalities. Copyright
- Liu, Yong,Chen, Hui,Hu, Xiong,Zhou, Wang,Deng, Guo-Jun
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supporting information
p. 4229 - 4232
(2013/07/26)
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- Highly stereoselective chemoenzymatic synthesis of the 3 h -isobenzofuran skeleton. access to enantiopure 3-methylphthalides
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A straightforward synthesis of (S)-3-methylphthalides has been developed, with the key asymmetric step being the bioreduction of 2-acetylbenzonitriles. Enzymatic processes have been found to be highly dependent on the pH value, with acidic conditions being required to avoid undesired side reactions. Baker's yeast was found to be the best biocatalyst acting in a highly stereoselective fashion. The simple treatment of the reaction crudes with aqueous HCl has provided access to enantiopure (S)-3-methylphthalides in moderate to excellent yields.
- Mangas-Sanchez, Juan,Busto, Eduardo,Gotor-Fernandez, Vicente,Gotor, Vicente
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supporting information; experimental part
p. 1444 - 1447
(2012/06/01)
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- Dual CCK-A and CCK-B receptor antagonists (II). Preparation and structure activity relationships of 5-alkyl-9-methyl-1,4-benzodiazepines and discovery of FR208419
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In our continuing research for dual CCK-A and -B antagonists, according to our hypothesis that dual CCKA and -B antagonists should be more efficacious than selective CCK-A antagonists for the treatment of pancreatitis, we have prepared various 5-alkyl-9-m
- Tabuchi, Seiichiro,Ito, Harunobu,Sogabe, Hajime,Kuno, Masako,Kinoshita, Takayoshi,Katumi, Ikuyo,Yamamoto, Naoko,Mitsui, Hitoshi,Satoh, Yoshinari
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- SURFACE PHOTOCHEMISTRY: THE AMIDE PHOTO-FRIES REARRANGEMENT
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The Photo-Fries rearrangement of eight anilides on the surface of dry silica gel has been examined.The rearrangement occurs quite cleanly, giving somewhat more of the para isomer than that obtained in methanolic solution.A test for intermolecularity on the silica gel surface showed that, as in solution, the radical pair intermediates do not separate.This contrasts with the behaviour of a previously reported dibenzyl ketone derivate.
- Magdy, M.,Malik, Abdel-,Mayo, Paul de
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p. 1275 - 1278
(2007/10/02)
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- Herbicidal N-haloacetyl-2-methyl-6-substituted methoxymethylanilines
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Compounds of the formula STR1 wherein R1 is alkyl or alkoxy; R2 is alkenyl having 2 to 10 carbon atoms, substituted alkyl of 1 to 10 carbon atoms or substituted alkenyl of 1 to 10 carbon atoms substituted with 1 or 2 hydroxy groups or 1 or 2 alkoxy groups of 1 to 4 carbon atoms or 1 or 2 alkenyloxy groups of 2 to 4 carbon atoms; acyl, and ketal group of the formula STR2 wherein n=2, 3 or 4, R4 is alkyl and R5 is hydrogen or alkyl, an oxime of the formula STR3 wherein R6 is hydrogen or alkyl; R3 is hydrogen or alkyl; X is halo have herbicidal activity.
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- Herbicidal N-haloacetyl-2-substituted-6-acylanilines
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Compounds of the formula: STR1 wherein X is halo; m and n are 0 or 1; R1 and R3 are hydrogen, alkyl or are joined to form a carbocyclic ring; R2 and R4 are hydrogen or alkyl; R5 and R6 are
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- Herbicidal N-haloacetyl-2-alkyl-6-acylanilines
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Compounds of the formula STR1 wherein R1 is alkyl or alkoxy; R2 is substituted alkly or substituted alkenly containing 1 or 2 hydroxy or alkoxy substituents, acyl, and ketal group of the formula STR2 wherein n=2, 3 or 4, R4/sup
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- Ortho-acylated anilide derivatives and salts thereof
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Ortho-acylated anilide derivatives represented by the formula: STR1 wherein R1, R2 and R3 are each C1 - 3 alkyl, and n is 1 or 2, and salts thereof.
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