- Organocatalytic Atroposelective Construction of Axially Chiral N-Aryl Benzimidazoles Involving Carbon-Carbon Bond Cleavage
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Axially chiral compounds widely occur in natural products, biologically active molecules, ligands, and catalysts, and their efficient and enantioselective synthesis is highly desirable. Herein, we report a novel method for the atroposelective construction of axially chiral N-aryl benzimidazoles with chiral phosphoric acid as the organocatalyst via reaction of N1-(aryl)benzene-1,2-diamines with multicarbonyl compounds. The present method provided the target products in high yields (up to 89percent) with excellent enantioselectivity (up to 98percent ee).
- Man, Ningning,Lou, Zhenbang,Li, Yuming,Yang, Haijun,Zhao, Yufen,Fu, Hua
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supporting information
p. 6382 - 6387
(2020/09/02)
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- Phosphorescent organic compound, preparation method thereof and organic electroluminescent device
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The invention discloses a phosphorescent organic compound, a preparation method thereof and an organic electroluminescent device, which belong to the field of chemical synthesis and photoelectric materials. The structural general formula is shown in the s
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Paragraph 0034-0038; 0050-0054; 0058-0062
(2020/06/20)
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- Phosphorescent organic compound, preparation method thereof and organic electroluminescent device
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The invention discloses a phosphorescent organic compound, a preparation method of the phosphorescent organic compound and an organic electroluminescent device, and belongs to the field of chemical synthesis and photoelectric materials. The structural gen
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Paragraph 0034-0038; 0050-0054; 0058-0062
(2020/12/30)
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- HIGH STRESS RESISTANT PLANT GROWTH REGULATOR AND PREPARATION METHOD AND USE THEREOF
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Disclosed are a high stress resistant plant growth regulator and a preparation and use thereof. In particular, the compound provided by the present invention is an ABA substitute for significantly improving the stress resistance of plants, and therefore has a very wide application prospect.
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Paragraph 0262-0263
(2019/01/15)
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- CALICHEAMICIN DERIVATIVES AND ANTIBODY DRUG CONJUGATES THEREOF
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The present invention is directed to novel calicheamicin derivatives useful as payloads in antibody-drug-conjugates (ADC's), and to payload-linker compounds and ADC compounds comprising the same; to pharmaceutical compositions comprising the same and to methods for using the same to treat pathological conditions such as cancer.
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Page/Page column 193
(2018/08/20)
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- Synthesis and structural analysis of conjugated benzoxazaborine derivatives
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Benzoxazaborine derivatives were synthesized by the dehydration condensation reaction of 2-aminobenzyl alcohols with arylboronic acids. The insensitivity of the benzoxazaborines to hydrolysis allowed these compounds to be isolated by silica gel column chr
- Ohishi, Tomoyuki,Igarashi, Kaori,Kadosono, Hiroki,Kikkawa, Shoko,Azumaya, Isao,Yokoyama, Akihiro
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supporting information
p. 4153 - 4157
(2018/10/24)
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- CARBAMATE QUINABACTIN
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The present invention relates to novel sulfonamide derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants, improving plant tolerance to abiotic stress (including environmental and chemical stresses), inhibiting seed germination and/or safening a plant against phytotoxic effects of chemicals.
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Paragraph 0163; 0164
(2018/02/23)
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- Organic small molecule luminescent material and organic electroluminescent device prepared from same
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The invention belongs to the field of organic photoelectric material technology, and discloses an organic small molecule luminescent material and an organic electroluminescent device prepared from same. The organic small molecule luminescent material uses
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Paragraph 0027; 0028; 0029; 0030
(2016/10/07)
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- Palladium-catalyzed direct coupling of 2-vinylanilines and isocyanides: An efficient synthesis of 2-aminoquinolines
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Palladium-catalyzed oxidative coupling of 2-vinylanilines and isocyanides constitutes a direct, facile, and efficient approach to 2-aminoquinolines. The procedure, employing palladium acetate and silver carbonate, is attractive in terms of assembly efficiency, functional group tolerance, and operational simplicity. A variety of 2-aminoquinolines were prepared in good to excellent yields.
- Wang, Lijie,Ferguson, Jamie,Zeng, Fanlong
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supporting information
p. 11486 - 11491
(2015/12/04)
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- One-pot ring-closing metathesis/1,3-dipolar cycloaddition through assisted tandem ruthenium catalysis: Synthesis of a dye with isoindolo[2,1-a]quinoline structure
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The one-pot tandem reaction of N-alkyl-N-allyl-2-vinylaniline derivatives with benzo- or naphthoquinones and a ruthenium-alkylidene catalyst leads to isoindolo[2,1-a]quinolines in a variety of colors, which can be altered by exchanging the substituent on the core heterocycle (see scheme). This reaction offers a new synthetic method for π-conjugated small molecules from simple aniline derivatives. Copyright
- Arisawa, Mitsuhiro,Fujii, Yuki,Kato, Hiroshige,Fukuda, Hayato,Matsumoto, Takashi,Ito, Mika,Abe, Hiroshi,Ito, Yoshihiro,Shuto, Satoshi
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supporting information
p. 1003 - 1007
(2013/03/13)
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- Synthesis and SERCA activities of structurally simplified cyclopiazonic acid analogues
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The indole alkaloid cyclopiazonic acid (CPA) is one of the few known nanomolar inhibitors of sarco(endo)plasmic reticulum Ca2+-ATPase (SERCA) besides the anticancer drug thapsigargin and the antiplasmoidal terpenoid artemisinin. Due to its less complex structure CPA represents an attractive lead structure for the development of novel antimalarial drugs or for applications in the field of plant protection. We report here the first syntheses of structurally simplified CPA fragments and discuss their SERCA activities on the basis of published crystal structures of CPA-SERCA complexes.
- Yao, Sheng,Gallenkamp, Daniel,Woelfel, Katharina,Lueke, Bettina,Schindler, Michael,Scherkenbeck, Juergen
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scheme or table
p. 4669 - 4678
(2011/09/12)
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- Amides as precursors of imidoyl radicals in cyclisation reactions
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Amides have been successfully used as precursors of imidoyl radicals for radical cyclisation. The amides have been converted to imidoyl selanides via reaction with phosgene to yield imidoyl chlorides followed by reaction with potassium phenylselanide. Imidoyl selanides were reacted with tributyltin hydride (Bu3SnH) as the radical mediator with triethylborane or AIBN as initiators to yield imidoyl radicals for cyclisation reactions. Imidoyl radicals have been cyclised onto alkenes to yield 2,3-substituted-indoles and -quinolines and also onto pyrroles and indoles to give bi- and tricyclic heteroarenes.
- Bowman, W. Russell,Fletcher, Anthony J.,Pedersen, Jan M.,Lovell, Peter J.,Elsegood, Mark R.J.,Hernández López, Elena,McKee, Vickie,Potts, Graeme B.S.
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p. 191 - 203
(2007/10/03)
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- SAR studies of 6-(arylamino)-4,4-disubstituted-1-methyl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones as progesterone receptor antagonists
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We previously disclosed that 6-aryl benzoxazin-2-ones were PR modulators. In a continuation of this work we examined the SAR of new 6-arylamino benzoxazinones and found the targets 1-25, with an extra amino linker between the pendent 6-aryl groups and ben
- Kern, Jeffrey C.,Terefenko, Eugene A.,Fensome, Andrew,Unwallla, Ray,Wrobel, Jay,Zhu, Yuan,Cohen, Jeffrey,Winneker, Richard,Zhang, Zhiming,Zhang, Puwen
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p. 189 - 192
(2007/10/03)
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- Studies of 4H-3,1-benzoxazines. 14. Structure and some properties of 2-[2-hydroxyphenyl(naphthyl)]-1,2-dihydro-4H-3,1-benzoxazines
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It has been shown that the condensation of tertiary aminophenylcarbinols with 2-hydroxybenz(naphth)aldehydes gives the corresponding 1,2- dihydrobenzoxazines and their structural Schiff base isomers. The reaction of 2-[2-hydroxyphenyl(naphthyl)]-1,2-dihyd
- Gromachevskaya,Kosulina,Borodavko
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p. 1068 - 1077
(2008/09/16)
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- New long acting beta-2-agonists and their use as medicaments
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The present invention relates to compounds of formula 1 wherein the groups X, Ra, Rb, R1, R1′, R2, R2′, R2″, R2′″, V and n may have the meanings given in the claims an
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Page/Page column 10-11
(2008/06/13)
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- Cyanopyrrole-containing cyclic carbamate and thiocarbamate biaryls and methods for preparing the same
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Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided. Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA /
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Page/Page column 13
(2008/06/13)
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- Synthesis and characterization of poly(1,3-phenylene)-based polyradicals carrying cyclic aminoxyls
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The synthesis and magnetic properties of poly(2,2,4,4-tetramethyl-N-yloxy-1,4-dihydro-2H-3,1-benzoxazine-6,8- diyl-1,3-phenylene) (4) are described. Polyradical 4 was prepared by the Pd-catalyzed cross-coupling reaction of 6,8-dibromo-2,2,4,4-tetramethyl-1,4-dihydro-2H-3,1-benzoxazine and bis(trimethylene) 1,3-phenylenediboronate, followed by oxidation with m-chloroperoxybenzoic acid. The number average molecular weights of 4 determined by SEC (size exclusion chromatography) were ~4120 (15 repeating units), and the spin concentrations determined by EPR were up to 0.75 spin per repeating unit. The EPR spectrum of 4 in a toluene glass matrix showed the ΔMs=2 forbidden transition at g=4.0. A Curie plot of the ΔMs=2 signal intensity vs. 1/T gave a straight line, suggesting that the polyradical is in a triplet ground state or a nearly degenerate singlet-triplet state.
- Oka, Hiroyuki,Tamura, Tomoki,Miura, Yozo,Teki, Yoshio
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p. 1364 - 1369
(2007/10/03)
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- Novel approach to isoindolo[2,1-a]quinolines
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An N-acyliminium ion approach towards the synthesis of isoindolo [2,1- a]quinolines by an intramolecular process is described.
- Pigeon, Pascal,Decroix, Bernard
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p. 2507 - 2516
(2007/10/03)
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- Imidazo-benzoxazinones, the preparation thereof and pharmaceutical compositions containing these compounds
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The invention relates to new imidazo-benzoxazinones of formula STR1 wherein the substituents are defined herein below, which compounds are useful in the treatment of cardiovascular disorders.
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- 4H-3,1-BENZOXAZINES. 2. SYNTHESIS OF 2,4-SUBSTITUTED 1,2-DIHYDRO-4H-3,1-BENZOXAZINES
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The reactions of o-aminophenylcarbinols with carbonyl compounds have been studied.Optimum conditions have been developed for the synthesis of 2-(5-X-2-furyl)-1,2-dihydro-4H-3,1-benzoxazines.It was found that 2,2-disubstituted 1,2-dihydro-4H-3,1-benzoxazines are unstable and are converted upon heating in the presence of acylating agents to 4H-3,1-benzoxazines.
- Gromachevskaya, E.V.,Kul'nevich, V.G.,Kosulina, T.P.,Pustovarov, V.S.
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p. 692 - 697
(2007/10/02)
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- Herbicidal N-haloacetyl-1,2-dihydro-4H-3,1-benzoxazine
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Novel N-haloacetyl-1,2-dihydro-4H-3,1-benzoxazines which have utility as herbicides.
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