- Cobalt(ii)-catalyzed benzylic oxidations with potassium persulfate in TFA/TFAA
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A cobalt-catalyzed C(sp3)-H oxygenation reaction to furnish aldehyde was herein reported. This transformation demonstrated high chemo-selectivity, and tolerated various methylarenes bearing electron-withdrawing substituents. This reaction provided rapid access to diverse aldehydes form methylarenes. Notably, TFA/TFAA was used for the first time as a mixed solvent in cobalt-catalyzed oxygenation of benzylic methylenes.
- Li, Tianlei,Li, Jishun,Zhu, Zihao,Pan, Weidong,Wu, Song
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p. 20879 - 20883
(2019/07/12)
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- THIAZOLE DERIVATIVE AND APPLICATIONS
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A thiazole derivative serving as a DHODH inhibitor, and applications thereof. The present invention specifically relates to a compound represented by formula I, a pharmaceutical composition containing the compound represented by formula (I), and applications of the compound in the preparation of drugs for treating diseases mediated by the DHODH or drugs for inhibiting the DHODH.
- -
-
Paragraph 0099-0100
(2019/04/16)
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- Nickel-catalyzed reductive defunctionalization of esters in the absence of an external reductant: Activation of C-O bonds
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The nickel-catalyzed reductive cleavage of esters in the absence of an external reductant, which involves the cleavage of an inert acyl C-O bond in O-Alkyl esters is reported. Various groups, such as N-containing heterocycles, esters, amides, and even arene rings can function as a directing group.
- Iyori, Yasuaki,Takahashi, Kenjiro,Yamazaki, Ken,Ano, Yusuke,Chatani, Naoto
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supporting information
p. 13610 - 13613
(2019/11/14)
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- 6,5-BICYCLIC OCTAHYDROPYRROLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
- -
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Page/Page column 45
(2016/07/05)
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- METHYL OXAZOLE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to methyl oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 35
(2016/06/28)
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- ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
- -
-
Page/Page column 46
(2016/07/05)
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- BRIDGED DIAZEPANE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to bridged diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
- -
-
Page/Page column 43
(2016/06/14)
-
- Oxidative cyclization of dialdehydes with alcohols and 1,3-dicarbonyl compounds under Rh(III)/Cu(II) conditions
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For the preparation of 3-alkoxyphthalides from phthalaldehydes and alcohols, a cyclization reaction in the presence of a rhodium(III) catalyst and copper(II) salt is reported. Cyclization of phthalaldehydes also occurs with 1,3-dicarbonyl compounds under similar conditions to produce 3-substituted phthalides in good yields. An acylrhodium(III) species might be a key intermediate in these cyclization reactions.
- Matsuda, Takanori,Suzuki, Kentaro,Abe, Shinya,Kirikae, Haruki,Okada, Noboru
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p. 9264 - 9270
(2015/11/27)
-
- CINNAMIC ACID AMIDE DERIVATIVE
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The present invention provides a cinnamic acid amide derivative having an excellent analgesic action. The cinnamic acid amide derivative of the present invention is a compound showing excellent analgesic actions to not only a nociceptive pain model animal but also a neuropathic pain model animal, which is very useful as an agent for treating various pain diseases showing acute or chronic pains or neuropathic pains.
- -
-
Paragraph 0074; 0085
(2015/11/24)
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- Cobalt carbonyl as an effective CO source in one-pot synthesis of esters from aryl halides
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For the first time, we have successfully applied Co2(CO) 8 as an effective carbonyl source for the Pd catalysed alkoxycarbonylation of aryl halides affording the corresponding aryl esters under mild microwave conditions. A wide variety of esters and carbonyl derivatives were prepared using this protocol.
- Baburajan,Senthilkumaran,Elango, Kuppanagounder P.
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p. 3050 - 3056
(2013/10/01)
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- A synthetic route to chiral C(3)-functionalized phthalides via a Ag(I)-catalyzed allylation/transesterification sequence
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A Ag(I)-catalyzed synthesis of chiral C(3)-substituted phthalides (8a-f) via a Sakurai-Hosomi allylation/transesterification reaction is described (ee ≤86%). A notable feature of this reaction is that it utilizes ortho-substituted aldehydes, which are a class of compounds that generally afford poor levels of stereoinduction when applying most known catalytic asymmetric allylation approaches. It was also found that elongation of the n-alkyl chain length (R1, up to n=6; R2=H) of the starting alkyl 2-formylbenzoates (7g-i) improved the enantiomeric excess (ee) of the product.
- Mirabdolbaghi, Roya,Dudding, Travis
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p. 3287 - 3292
(2013/04/24)
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- An indium-mediated allylative/transesterification DFT-directed approach to chiral C(3)-functionalized phthalides
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A one-pot synthesis of chiral C(3)-substituted phthalides via an indium-mediated allylation/transesterification reaction is described. The development of this reaction was facilitated through the applied use of DFT calculations to rationalize the stereoselection of a chiral In-mediated process. It was discovered that the enantiomeric excess of this reaction depended upon the steric size, chain length, and substitution of the aldehyde employed.
- Mirabdolbaghi, Roya,Dudding, Travis
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supporting information; experimental part
p. 3748 - 3751
(2012/09/07)
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- New efficient route to fused aryltetrahydroindolizinones via N-Acyliminium intermediates
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Straightforward routes to fused tetrahydroindolizinones by two routes A and B, starting either from. 2-formylbenzoic acid and esters or from, β-hydroxy lactones via acyl iminium ions, are described. A plausible mechanism and limitations are given. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009.
- Chiurato, Matteo,Routier, Sylvain,Troin, Yves,Guillaumet, Gerald
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scheme or table
p. 3011 - 3021
(2009/11/30)
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- Liver X receptor (LXR) modulators with dibenz[b,f]-[1,4]oxazepin-11-one, (Z)-dibenz[b,f]azocin-6-one, and 11,12-dihydrodibenz[b,f]azocin-6-one skeletons
-
Conformationally restricted heterocyclic analogs of carba-T0901317 with dibenz[b,f][1,4]oxazepin-11-one, 11,12-dihydrodibenz[b,f)azocin-6-one, and (Z)-dibenz[b,f]-azocin-6-one skeletons were prepared as candidate for liver X receptor (LXR) agonists. In vitro transactivation assay revealed that the activity depends on the nature of the linking group.
- Aoyama, Atsushi,Aoyama, Hiroshi,Makishima, Makoto,Hashimoto, Yuichi,Miyachi, Hiroyuki
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scheme or table
p. 2209 - 2216
(2010/04/29)
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- Stereocontrolled synthesis of the diene and triene macrolactones of oximidines I and II: Organometallic coupling versus standard macrolactonization
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(matrix presented) Stereocontrolled construction of the 12-membered diene and triene lactones 1, 2, and 3, characteristic of the antitumor agent oximidines I and II, are reported and were based on an intramolecular Castro-Stephens coupling for the construction of a cyclic enyne or dienyne followed by stereoselective reduction of the cyclic alkyne for introduction of the cis-olefin of the targets. A comparison of the effectiveness of this protocol is made with standard macrolactonization.
- Coleman, Robert S.,Garg, Rahul
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p. 3487 - 3490
(2007/10/03)
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- Aromatization and hydrogen-shift of 7-substituted 1,3,5-cycloheptatrienes in the presence of palladium(II) acetate
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Reaction of 7-ethoxycarbonyl-1,3,5-cycloheptatriene with palladium(II) acetate afforded 2- and 4-formylbenzoic acid ethyl ester and diethyl maleate via aromatization, and a mixture of position isomers of the cycloheptatriene through hydrogen-shift. The reaction with 7-cyano-1,3,5-cycloheptatriene was also investigated. The reactions are considered to proceed through palladium complexes of the cycloheptatrienes and their norcaradiene isomers.
- Saito,Kozaki,Takahashi
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p. 2187 - 2189
(2007/10/02)
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- BENZOXAZOLE AND RELATED HETEROCYCLIC SUBSTITUTED IMIDAZOLE AND BENZIMIDAZOLE DERIVATIVES
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Novel compounds are disclosed having the formula STR1 wherein X, Y, R 1, R 2, R 3, R 4, and R 5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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-
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- Reactions of 1-Methyl-4-quinolone with 2-Lithio-1,3-dithianes
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Nucleophiles, including lithiated 1,3-dithianes, add to 1-methyl-4-quinolone at the 2-position; in some cases initial adducts were subsequently trapped with added electrophile.
- Griera, Rosa,Rigat, Lluis,Alvarez, Mercedes,Joule, John A.
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p. 1223 - 1228
(2007/10/02)
-
- Synthesis of o-acylarylcarboxylic esters: A new replacement of phenolic hydroxyl by a carbonyl group
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A wide variety of the title esters are prepared in good yields via a new two step replacement of phenolic hydroxyl by an ethoxycarbonyl group.
- Katritzky,Kotali
-
p. 6781 - 6784
(2007/10/02)
-
- 1-carboalkoxyalkyl-3-alkoxy-4-(2'-carboxyphenyl)-azet-2-ones as plant growth regulators and selective herbicides
-
Compounds of the formula: STR1 wherein R1 is lower alkyl of 1 to 6 carbon atoms lower alkenyl of 2 to 6 carbon atoms or benzyl; R2 is lower alkoxy of 1 to 6 carbon atoms, benzyloxy or the group STR2 where R4 is lower alkoxy of 1 to 4 carbon atoms; and R3 is hydrogen, lower alkyl of 1 to 6 carbon atoms, lower alkyl of 1 to 6 carbon atoms substituted with 1 to 3 trihalomethyl groups, lower haloalkyl of 1 to 6 carbon atoms substituted with 1 to 6 halogen atoms, lower alkenyl of 2 to 6 carbon atoms, arylalkyl of 7 to 12 carbon atoms, lower alkoxyalkyl of 2 to 6 carbon atoms, lower alkylthioalkyl of 2 to 6 carbon atoms, or lower cycloalkyl of 3 to 8 carbon atoms are active as plant growth regulators. Certain of these compounds also show activity as selective herbicides.
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- Aldehydes from Nitriles. Formation of N-Alkylnitrilium Ions and Their Reduction to N-Alkylaldimines by Organosilicon Hydrides
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A two-step procedure for the partial reduction of nitriles to aldehydes under mild reaction conditions is presented.This approach involves the N-alkylation of nitriles in dichloromethane solution and reductive capture of the resulting nitrilium ions to N-alkylaldimines with an organosilicon hydride such as triethylsilane or tri-n-hexylsilane.Mild hydrolysis of the aldimines produces aldehydes in generally good-to-excellent yield.Use of both triethyloxonium tetrafluoroborate and isopropyl chloride-iron(III) chloride reagents to effect alkylation is reported.Selective reduction of the nitrile function in polyfunctional substrates is possible with this technique.Over reduction to amines does not occur.Close control of reducing agent and reaction temperatures is not required.Attempts to effect reduction of nirile-boron trifluoride complexes with triethylsilane were unsuccessful, even at elevated temperatures.
- Fry, James L.,Ott, Roger A.
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p. 602 - 607
(2007/10/02)
-
- PHOTOOXYGENATION OF 7-SUBSTITUTED CYCLOHEPTATRIENES
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Photooxygenation of 7-substituted cycloheptatrienes, including the Me, Et, iPr, Ph, CN, COOMe, COOEt, and CONH2 groups was studied, and several products among the tropilidene-type (1 and 2) and norcaradiene-type (3 and 4) endoperoxides, o-substituted benzaldehydes (5), diepoxides (6 and 7), and ketoalcohols (8) were obtained.Mechanism of the formations of the products was discussed.Thermal isomerization of the endoperoxides (1, 3 and 4) to the corresponding diepoxides (10, 6 and 7), and the reaction of the endoperoxides (1 and 3) with triethylamine were examined.
- Asao, Toyonobu,Yagihara, Morio,Kitahara, Yoshio
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p. 985 - 991
(2007/10/02)
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