- An Improvement of the Palladium-Catalyzed [4+2] Cycloaddition of o -(Silylmethyl)benzyl Carbonates with Alkenes
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The palladium complex, which is generated in situ from Pd(η 3-C3H5)Cp and tris(4-methoxy-3,5-dimethylphenyl)phosphine, catalyzed the [4+2] cycloaddition of o-(silylmethyl)benzyl carbonates with alkenes. The reaction of the
- Jin, Yushu,Ishizuka, Kentaro,Kuwano, Ryoichi
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- Diastereoselective Synthesis of CF3-Substituted Spiroisochromans by [1,5]-Hydride Shift/Cyclization/Intramolecular Friedel-Crafts Reaction Sequence
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Developed herein is a diastereoselective synthesis of CF3-substituted spiroisochromans via C(sp3)-H bond functionalization involving sequential transformations ([1,5]-hydride shift/cyclization/elimination of MeOH/intramolecular Friedel-Crafts reaction).
- Tamura, Risa,Kitamura, Eriko,Tsutsumi, Ryosuke,Yamanaka, Masahiro,Akiyama, Takahiko,Mori, Keiji
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- COMPOUND, COMPOSITION, ORGANIC ELECTROLUMINESCENT ELEMENT, AND ELECTRONIC APPLIANCE
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A compound is represented by a formula (20) below. In the formula (20), a least one pair of a pair of X21 and X22, a pair of X22 and X23 and a pair of X23 and X24 are carbon atoms to be bon
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Paragraph 0582-0583
(2019/11/21)
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- Synthetic process of 9,9-ialkyl fluorene derivative
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The invention discloses a synthetic process of a 9,9-ialkyl fluorene derivative. According to the synthetic process, 2-hydroxybenzoic acid compound serves as an initiator, esterification is conductedfirstly by using alkanol, then esterification is conducted firstly by using trifluoromethanesulfonic acid, Suzuki coupled reaction is conducted on the obtained esters and Phenylboric acid compounds, after biphenyl-2-methyl formate compound is obtained and introduced into alkyl through the Grignard reagent or organolithium, reflux reaction is conducted under catalysis of Lewis acid, and dehydrationcyclizing is conducted to obtain the 9,9-ialkyl fluorene derivative. Compared with the prior art, the synthetic process of the 9,9-ialkyl fluorene derivative has the characteristics that raw materials are easy to obtain, operation of the technology is easy, the yield of each step is high, the purification step is simple, products with complex structures can be synthesized, and the enlarged industrial prospects are achieved.
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- First Total Syntheses of Tetracenomycins C and X
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The first total syntheses of tetracenomycins C and X were achieved, featuring 1) preparation of a hexasubstituted naphthonitrile oxide by successive benzyne cycloadditions and an oxidative ring-opening reaction; 2) a novel ortho-quinone mono-acetal as the A-ring unit; 3) construction of three contiguous stereogenic centers by an asymmetric benzoin cyclization, an isoxazole oxidation, and a stereoselective reduction.
- Sato, Shogo,Sakata, Keiichiro,Hashimoto, Yoshimitsu,Takikawa, Hiroshi,Suzuki, Keisuke
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supporting information
p. 12608 - 12613
(2017/09/11)
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- Organic electroluminescent element and electronic device
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Provided are an organic EL element having even higher efficiency of light emission, an electronic device provided with the organic EL element, and a compound represented by formula (1) whereby the organic EL element can be provided. (In the formula, Ar1 is a substituted or unsubstituted naphthalene ring; a substituent and R11 through R18 on the naphthalene ring are at least one species selected from the group consisting of a hydrogen atom, a fluorine atom, a cyano group, an alkyl group, a cycloalkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, a group represented by -Si(R101)(R102)(R103), and a group represented by -Z-Ra; R1 and R2 each independently represent a hydrogen atom, an alkyl group, a cycloalkyl group, a group represented by -Si(R101)(R102)(R103), an aryl group, or a heteroaryl group, Z in each instance thereof representing a single bond, an arylene group, a heteroarylene group, or a divalent linking group configured from 2 to 4 arylene groups or heteroarylene groups bonded together; Ra represents a group represented by -N(R104)(R105), an aryl group, or a heteroaryl group; and R101 through R105 represent hydrogen atoms, alkyl groups, cycloalkyl groups, aryl groups, or heteroaryl groups. At least one of the substituent and R11 through R18 on the naphthalene ring is a group represented by -Z-Ra.)
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Paragraph 0025
(2016/10/08)
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- Redox Switching of Orthoquinone-Containing Aromatic Compounds with Hydrogen and Oxygen Gas
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Unique redox switching of orthoquinone-containing pentacyclic aromatic compounds with molecular hydrogen and oxygen in the presence of a palladium nanoparticle catalyst (SAPd) is disclosed. These molecules were predicted by in silico screening before synt
- Urakawa, Kazuki,Sumimoto, Michinori,Arisawa, Mitsuhiro,Matsuda, Masaki,Ishikawa, Hayato
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supporting information
p. 7432 - 7436
(2016/07/06)
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- Photocatalytic Dehydrogenative Lactonization of 2-Arylbenzoic Acids
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A metal-free dehydrogenative lactonization of 2-arylbenzoic acids at room temperature was developed. This work illustrates the first application of visible-light photoredox catalysis in the preparation of benzo-3,4-coumarins, an important structural motif in bioactive molecules. The combination of photocatalyst [Acr+-Mes] with (NH4)2S2O8 as a terminal oxidant provides an economical and environmentally benign entry to different substituted benzocoumarins. Preliminary mechanistic studies suggest that this reaction most likely occurs through a homolytic aromatic substitution pathway.
- Ramirez, Nieves P.,Bosque, Irene,Gonzalez-Gomez, Jose C.
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p. 4550 - 4553
(2015/09/28)
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- CONDENSED POLYCYCLIC AROMATIC COMPOUND, AROMATIC POLYMER, AND METHOD FOR SYNTHESIZING AROMATIC COMPOUND
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Provided is a condensed polycyclic aromatic compound that can be used as a precursor for synthesizing a condensed polycyclic aromatic compound having relatively high solubility. Also provided is a method for synthesizing and using such a novel condensed p
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Paragraph 0282-0284
(2014/06/24)
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- Pd-catalyzed C-H lactonization for expedient synthesis of biaryl lactones and total synthesis of cannabinol
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A practical Pd(II)/Pd(IV)-catalyzed carboxyl-directed C-H activation/C-O cyclization to construct biaryl lactones has been developed. The synthetic utility of this new reaction was demonstrated in an atom-economical and operationally convenient total synthesis of the natural product cannabinol from commercially available starting materials, with the newly developed method used for two key steps.
- Li, Yan,Ding, Yan-Jun,Wang, Jian-Yong,Su, Yi-Ming,Wang, Xi-Sheng
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p. 2574 - 2577
(2013/07/11)
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- Synthesis and evaluation of an O-Aminated naphthol AS-E as a prodrug of CREB-mediated gene transcription inhibition
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An O-Aminated naphthol AS-E was designed as a prodrug to achieve reductive activation and improved aqueous solubility. During the synthesis of this designed compound, a novel transformation from aryl triflates and ethyl acetohydroximate to oxazoles was discovered. Although the initially designed O-Amino naphthol AS-E was not made successfully, the eventually synthesized O-tert-butylamino derivative was found to be biologically inactive, suggesting that reductive N-O cleavage in this compound was not facile due to unfavorable steric and electronic effects.
- Xie, Fuchun,Li, Bingbing X.,Xiao, Xiangshu
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p. 380 - 384
(2013/07/26)
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- Substituted Imidazole 4-Carboxamides as Cholecystokinin-1 Receptor Modulators
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Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.
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Page/Page column 33
(2009/05/28)
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- Pyrrolo(oxo)isoquinolines as 5HT ligands
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The present application describes compounds according to Formula I, pharmaceutical compositions, comprising at least one compound according to Formula I and optionally at least one additional therapeutic agent and methods of treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using compounds according to Formula I or pharmaceutically acceptable salt forms thereof, wherein A, B, D, E, m, n, R3, R7, R8, R9, R10, R11 and X are described herein.
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Page/Page column 65
(2008/06/13)
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- Dynamic kinetic asymmetric transformation of diene monoepoxides: A practical asymmetric synthesis of vinylglycinol, vigabatrin, and ethambutol
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The ability to perform a dynamic kinetic asymmetric transformation (DYKAT) using the palladium-catalyzed asymmetric allylic alkylation (AAA) is explored in the context of butadiene monoepoxide. The versatility of this commercially available, but racemic, four-carbon building block becomes significantly enhanced via conversion of both enantiomers into a single enantiomeric product. The concept is explored in the context of a synthesis of vinylglycinol with phthalimide as the nitrogen source. The success of the project required a new design of the ligand for palladium wherein additional conformational restraints were introduced. Thus, the phthalimide derivative of vinylglycinol was obtained in nearly quantitative yield and had an ee of 98% which, upon crystallization, was enhanced to > 99%. This one-step synthesis of a protected form of vinylglycinol provided short practical syntheses of the title compounds. Vigabatrin requires only four steps, and ethambutol six. The intermediate to the existing synthesis of ethambutol is available in 87% yield in three steps. (R)-Serine derives from oxidative cleavage of the double bond. The reaction of phthalimide and isoprene monoepoxide demonstrates the remarkable ability of the chiral ligands to control both regioselectivity and enantioselectivity and demonstrates the effectiveness of this protocol in creating a quaternary center asymmetrically.
- Trost, Barry M.,Bunt, Richard C.,Lemoine, Remy C.,Calkins, Trevor L.
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p. 5968 - 5976
(2007/10/03)
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