- Conjugate Addition of Allyltrimethylsilane to Electrophilic Cyclopropanes
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Allyltrimethylsilane undergoes a Lewis-acid-assisted one-pot conjugate addition with cyclopropanes activated by geminal alkoxycarbonyl groups.
- Bambal, Ramesh,Kemmitt, Raymond D. W.
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Read Online
- Novel linker compound and Site-Specific compounds of Antibody-Drug Conjugate Comprising the Same
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The present invention relates to a novel linker compound, and relates to a site-specific antibody-drug conjugate (ADC) compound comprising the same, a method for manufacturing the same, and an anticancer composition comprising the same as an active component. The linker compound produces a uniform ADC compound with excellent site specificity in manufacturing an ADC compound, and the ADC compound comprising the same exhibits an excellent anticancer effect.COPYRIGHT KIPO 2020
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Paragraph 0223; 0321-0326
(2020/02/07)
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- CYCLOBUTANE- AND AZETIDINE-CONTAINING MONO AND SPIROCYCLIC COMPOUNDS AS ALPHA V INTEGRIN INHIBITORS
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The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αv- containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of av-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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Page/Page column 265; 287-289
(2018/05/27)
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- A general synthetic approach to para-cyclophanes via ring-closing metathesis
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A new methodology for the synthesis para-cyclophanes and longithorone C frameworks has been demonstrated via alkylation, ceric ammonium nitrate (CAN) oxidation and ring-closing metathesis as key steps.
- Kotha, Sambasivarao,Shirbhate, Mukesh E.
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p. 1483 - 1494
(2016/02/26)
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- A general synthetic approach to para-cyclophanes via ring-closing metathesis
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A new methodology for the synthesis para-cyclophanes, and longithorone C frameworks has been demonstrated via alkylation, eerie ammonium nitrate (CAN) oxidation and ring-closing metathesis as key steps.
- Kotha, Sambasivarao,Shirbhate, Mukesh E.
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p. 1483 - 1494
(2016/09/09)
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- Intramolecular palladium-catalyzed alkene carboalkynylation
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Abstract Carbocycles are essential building blocks for the synthesis of natural and synthetic bioactive compounds. Herein, we report the first example of palladium-catalyzed intramolecular carboalkynylation of non-activated olefins. Using activated carbon
- Nicolai, Stefano,Swallow, Peter,Waser, Jerome
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supporting information
p. 5959 - 5964
(2015/08/03)
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- Highly functionalized and potent antiviral cyclopentane derivatives formed by a tandem process consisting of organometallic, transition-metal-catalyzed, and radical reaction steps
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A simple modular tandem approach to multiply substituted cyclopentane derivatives is reported, which succeeds by joining organometallic addition, conjugate addition, radical cyclization, and oxygenation steps. The key steps enabling this tandem process are the thus far rarely used isomerization of allylic alkoxides to enolates and single-electron transfer to merge the organometallic step with the radical and oxygenation chemistry. This controlled lineup of multiple electronically contrasting reactive intermediates provides versatile access to highly functionalized cyclopentane derivatives from very simple and readily available commodity precursors. The antiviral activity of the synthesized compounds was screened and a number of compounds showed potent activity against hepatitisC and dengue viruses.
- Jagtap, Pratap R.,Ford, Leigh,Deister, Elmar,Pohl, Radek,Cisarova, Ivana,Hodek, Jan,Weber, Jan,Mackman, Richard,Bahador, Gina,Jahn, Ullrich
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supporting information
p. 10298 - 10304
(2014/08/18)
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- Diversity-oriented approach to macrocyclic cyclophane derivatives via ring-closing metathesis
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A short synthetic approach to the macrocyclic framework of longithorone C is described via ring-closing metathesis using the Grubbs 2nd generation catalyst. Georg Thieme Verlag Stuttgart ? New York.
- Kotha, Sambasivarao,Shirbhate, Mukesh E.
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p. 2183 - 2188
(2012/11/07)
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- Chain-walking strategy for organic synthesis: Catalytic cycloisomerization of 1,n-dienes
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The catalytic construction of carbon-carbon bonds in small organic molecules via chain walking is described. Catalytic cycloisomerization of 1,n-dienes via chain walking was achieved using a palladium-1,10-phenanthroline catalyst to form five-membered-ring products. By means of a cycloisomerization/ hydrogenation protocol, 1,7- to 1,14-dienes were selectively converted to bicyclo[4.3.0]nonane derivatives. The use of chain walking provides a new method in organic synthesis to functionalize unreactive carbon-hydrogen bonds by letting the catalyst look for preferable bond-forming sites by moving around on the substrate.
- Kochi, Takuya,Hamasaki, Taro,Aoyama, Yuka,Kawasaki, Junichi,Kakiuchi, Fumitoshi
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supporting information
p. 16544 - 16547,4
(2020/09/15)
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- Treasures from the Free Radical Renaissance Period - Miscellaneous hexenyl radical kinetic data
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Rate constant data and Arrhenius parameters have been determined for a series of substituted hexenyl radicals of differing electronic and steric demand. Electron-withdrawing groups (CF3, CO2Et) directly attached to the radical centre slighly accelerate 5-exo ring-closure (k cis + ktrans ~ 2.1 × 105 s -1 at 25°) relative to donating groups (OMe; 1.6 × 10 5 s-1 at 25°). Sterically demanding groups (tert-Bu), as expected, slow the cyclization process (1 × 105 s -1). These observations are consistent with subtle changes in activation energy for 5-exo ring-closure. Interestingly, the nature of the solvent would appear to have a significant influence on this chemistry with the cis/trans stereoselectivity sometimes improved as the solvent polarity is increased. Except for the system containing the CF3 (electron-withdrawing) group which displays an increase in the cyclization/capture rate constant (kc/kH), a general decrease in the kc/kH ratio as solvent polarity is increased is noted; these changes have been speculated to arise mainly from changes in kH in the various solvents employed.
- Beckwith, Athelstan L. J.,Schiesser, Carl H.
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supporting information; experimental part
p. 1736 - 1743
(2011/05/03)
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- Targeting the Hsp90 chaperone: Synthesis of novel resorcylic acid macrolactone inhibitors of Hsp90
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A series of benzo-macrolactones has been prepared by chemical synthesis, and evaluated as inhibitors of heat shock protein 90 (Hsp90), an emerging attractive target for novel cancer therapeutic agents. A new synthesis of these resorcylic acid macrolactone analogues of the natural product radicicol is described in which the key steps are the acylation and ring opening of a homophthalic anhydride to give an isocoumarin, followed by a ring-closing metathesis to form the macrocycle. The methodology has been extended to a novel series of macrolactones incorporating a 1,2,3-triazole ring.
- Day, James E. H.,Sharp, Swee Y.,Rowlands, Martin G.,Aherne, Wynne,Workman, Paul,Moody, Christopher J.
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supporting information; experimental part
p. 2758 - 2763
(2010/07/04)
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- Palladium-Catalyzed highly diastereoselective oxidative cascade cyclization reactions
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Isoquinoline and quinoline have been discovered as novel ligands for palladium-catalyzed oxidative cascade cyclization reactions. With our new catalyst systems (Pd(OAc)2/isoquinoline or quinoline), unsaturated anilides cyclize under an oxygen atmosphere (1 atm) to furnish structurally versatile indoline derivatives in good yields. One C-N bond and two C-C bonds are formed in a single step with excellent diastereoselectivities (dr> 24:1).
- Yip, Kai-Tai,Zhu, Nian-Yong,Yang, Dan
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supporting information; experimental part
p. 1911 - 1914
(2009/09/25)
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- First intramolecular geminal acylation: Synthesis of bridged bicyclic diketones
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Bicyclic diketones have been produced by Lewis acid-promoted geminal acylations involving cyclic acyloins tethered to an acetal. This intramolecular process must proceed via a mode of reaction which, due to steric hindrance, is not seen in the intermolecu
- Blanchard, Angela N,Burnell
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p. 4779 - 4781
(2007/10/03)
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- Effects of Olefin Substitution on the Ring-Closing Metathesis of Dienes
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Ruthenium alkylidene 1 and molybdenum alkylidene 2 have been utilized in the ring-closing metathesis (RCM) of dienes containing gem-disubstituted olefins to yield tri- and tetrasubstituted cyclic olefins. Dienes with sterically demanding and/or electron-withdrawing substituents such as Ph, CO2Me, and tBu were cyclized successfully with 2, but did not cyclize with 1. Tetrasubstituted cyclic olefins could be formed with 2, but not using alkylidene 1. Dienes with allylic functional groups yielded functionalized cyclic olefins when treated with 1.
- Kirkland, Thomas A.,Grubbs, Robert H.
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p. 7310 - 7318
(2007/10/03)
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- Liquid crystals
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Compounds of the formula STR1 wherein n stands for the number 0 or 1; the rings A1, A2 and A3 represent 1,4-phenylene, 2-fluoro-1,4-phenylene or trans-1,4-cyclohexylene or one of these rings also represents a 2,5-disubstituted pyrimidine ring or a trans-2,5-disubstituted m-dioxane ring; X1 represents a single covalent bond, --COO--, --OOC--, --CH2 CH2 --, p--C6 H4 --, --CH2 CH2 --p-- C6 H4 --, --CH2 CH2 --p--C6 H4 --CH2 CH2 -- or, insofar as the rings A1 and A2 represent 1,4-phenylene, also --NON--; R2 represents 1E-alkenyl, 2Z-alkenyl, 3E-alkenyl, 4-alkenyl or alkenyloxy, with the proviso that the oxygen atom in alkenyloxy is linked with a saturated carbon atom; and R1 signifies 1E-alkenyl, 2Z-alkenyl, 3E-alkenyl, 4-alkenyl or, insofar as R2 represents alkenyloxy, also alkyl, their manufacture, as well as liquid crystalline mixtures and the use for electro-optical purposes.
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- Thromboxane Receptor Antagonism Combined with Thromboxane Synthase Inhibition. 3. Pyridinylalkyl-Substituted 8-octanoic Acids
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A series of 8-octanoic acids substituted with a pyridinylalkyl group along the chain were synthesized and tested in vitro for their ability to both antagonize the binding of thromboxane A2 to its receptors and to inhibit th
- Main, Alan J.,Bhagwat, Shripad S.,Boswell, Clay,Goldstein, Robert,Gude, Candido,et al.
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p. 4366 - 4372
(2007/10/02)
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- CERTAIN (ARYLSULFONAMIDO- AND IMIDAZOLYL-)-SUBSTITUTED CARBOXYLIC ACIDS AND DERIVATIVES THEREOF AND USE FOR SUPPRESSING THROMBOXANE ACTIVITY
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The present invention is concerned with compounds of formula I STR1 wherein A, B, M, R, Ar and Het are as defined in the specification, pharmaceutically acceptable ester and amide derivatives thereof; N-oxides thereof, tetrazole derivatives thereof, and s
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- (Arylsulfonamido- and pyridyl-)-substituted carboxylic acids and derivatives thereof and use for suppressing thromboxane activity
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Disclosed are the compounds of formula STR1 wherein A represents lower alkylene; B represents oxygen, sulfur, lower alkylene, lower alkylene interrupted by oxygen, sulfur, sulfinyl or sulfonyl, (oxy-, sulfinyl-, sulfonyl- or thio)-lower alkylene, lower al
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- Novel liquid crystal mixtures
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Liquid crystalline mixtures containing compounds of the formula STR1 wherein n stands for the number 0 or 1; X1 and X2 denote single covalent bonds or one of the symbols X1 and X2 also denotes --COO--, --OOC-- or --CH2 CH2 --; the rings A1, A2 and A3 represent 1,4-phenylene, 2-fluoro-1,4-phenylene or trans-1,4-cyclohexylene or one of these rings also represents a 2,5-disubstituted pyrimidine ring or a trans-2,5-disubstituted m-dioxane ring; R1 signifies 4-alkenyl or on a cyclohexyl ring also 2Z-alkenyl; and R2 denotes alkyl, alkoxy, --CN or --NCS, as well as the manufacture of these compounds and the use for electro-optical purposes are described.
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- Urazole analogs of prostaglandins
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Compounds of formula (I) STR1 wherein: n is 1 to 5 Y is --CH2 --CH2 or --CH=CH--; R1 is hydrogen or CO2 R1 represents an ester group in which the R1 moiety contains from 1-12 carbon atoms; R2 is hydrogen, C1-4 alkyl, or phenyl; R3 is hydroxy or protected hydroxy; R4 is hydrogen, C1-9 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl-C1-6 alkyl, phenyl, phenyl --C1-6 alkyl, naphthyl, naphthyl C1-6 alkyl, any of which phenyl moieties or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C1-6 alkyl, hydroxy, C1-6 alkoxy, phenyl C1-6 alkoxy or nitro groups; R5 is hydrogen, C1-6 alkyl, C5-8 cycloalkyl, phenyl, phenyl-C1-6 alkyl or phenyl C3-6 cycloalkyl, any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy or nitro groups; or R2 and R4 taken with the carbon atom to which they are joined represent a C5-8 cycloalkyl group; and salts thereof are useful for their prostaglandin-like activity.
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- COPPER (I) CATALYSIS OF OLEFIN PHOTOREACTIONS -9. PHOTOBICYCLIZATION OF alpha -, beta -, AND gamma -ALKENYLALLYL ALCOHOLS.
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Cyclobutylcarbinyl alcohols of the bicyclo left bracket 3. 2. 0 right bracket heptane ring system are produced by UV irradiation of alpha -, beta -, and gamma -alkenylallyl alcohols in the presence of copper (I) trifluoromethanesulfonate (CuOTf). endo-2-Hydroxy epimers of bicyclo left bracket 3. 2. 0 right bracket heptan-2-ols are generated stereoselectively. This result as well as the effect of CuOTf on the **1H NMR spectrum of 4,4-dimethyl-1,6-heptadien-3-ol suggests that coordination of two C equals C bonds and the hydroxyl group with a single copper (I) is important. The derived bicyclo left bracket 3. 2. 0 right bracket heptan 2-ones fragment cleanly at 580 degree C to afford cyclopent-2-en-1-ones. Geometric isomerization competes with photobicyclization of (E)- and (Z)-octa-2,7-dien-1-ols.
- Salomon,Coughlin,Ghosh,Zagorski
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p. 998 - 1007
(2007/10/14)
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