- Pd(II)-catalyzed one-pot, three-step route for the synthesis of unsymmetrical acridines
-
Unsymmetric acridines are synthesized via a one-pot amination/cyclization/ aromatization reaction for the first time. With Pd(OAc)2-X-Phos as the catalyst, a series of unsymmetric acridines are obtained in moderate to excellent yields (up to 99
- Guo, Hai-Ming,Mao, Run-Ze,Wang, Qiao-Tian,Niu, Hong-Ying,Xie, Ming-Sheng,Qu, Gui-Rong
-
-
Read Online
- 4-benzylaminobenzenesulfonamide derivative and preparation and application thereof
-
The invention provides a 4-benzylaminobenzenesulfonamide derivative represented by a formula (I) or a pharmaceutically acceptable salt, a solvate or a metabolite thereof. In the formula (I), R1, R2, R3, R4, R5 and R6 are defined in the specification. The
- -
-
Paragraph 0258-0261
(2020/08/30)
-
- Construction of spirofused tricyclic frameworks by NHC-catalyzed intramolecular stetter reaction of a benzaldehyde tether with a cyclic exsnone
-
Various benzaldehyde tethers with a cyclic enone were prepared from commercially available 2-hydroxybenzaldehydes via a three-step sequence involving triflate formation, Sonogashira cross-coupling, and regioselective hydrogenation. These substrates were t
- Hsu, Day-Shin,Cheng, Chiao-Yun
-
p. 10832 - 10842
(2019/09/30)
-
- Synthesis of macrocyclic bisbibenzyl derivatives and their anticancer effects as anti-tubulin agents
-
Based on the core skeleton of the total synthesized bisbibenzyl marchantin C, riccardin D and plagiochin E, a series of brominated and aminomethylated derivatives of above three bisbibenzyls have been synthesized and their cytotoxic activity against KB, M
- Jiang, Juan,Sun, Bin,Wang, Yan-Yan,Cui, Min,Zhang, Li,Cui, Chang-Zhi,Wang, Yan-Feng,Liu, Xi-Gong,Lou, Hong-Xiang
-
scheme or table
p. 2382 - 2391
(2012/05/05)
-
- Synthetic studies towards the core tricyclic ring system of pradimicin A
-
Pradimicins are structurally intriguing natural products that possess potent biological activity as antifungal and antiviral agents through a unique mode of action as carbohydrate binding agents. A preliminary synthetic approach towards pradimicin A has focused on a model study of the core tricyclic ring system. The route features an alkoxyallylboration/cycloisomerization/Diels-Alder cycloaddition sequence as the key steps. The alkoxyallylboration was critical for differentiating the hydroxy groups in the central cyclohexadienediol unit of pradimycins, which will ensure a regiocontrolled glycosylation. For the cycloisomerization reaction, various substrates and conditions were tested for a ring-closing enyne metathesis reaction. With enyne substrate 23, dimerization-prone bicyclic diene 24 was isolated as the major product under the conditions of both ruthenium-catalyzed metathesis and palladium-catalyzed cycloisomerization. In the end, the optimal route found for the synthesis of the model functionalized tricyclic ring system 31 features a one-pot sequential palladium-catalyzed cycloisomerization, Diels-Alder reaction, and oxidative aromatization. A model study towards the synthesis of the C-D-E tricyclic core of the carbohydrate binding agent, pradimicin A, is described. Alkoxyallylboration provided the differentially protected diol unit of the central ring. Optimization of a key enyne cycloisomerization reaction led to the synthesis of the tricycle by a one-pot Pd-catalyzed cycloisomerization/Diels- Alder cycloaddition/aromatization.
- Zilke, Laura,Hall, Dennis G.
-
scheme or table
p. 4153 - 4163
(2012/09/22)
-
- Syntheses of macrocyclic bis(bibenzyl) compounds derived from perrottetin e
-
Macrocyclic bis(bibenzyl) compounds are natural products from liverworts and are of growing interest due to recent reports on new isolated compounds and on their remarkable biological activities. We report here on a flexible and general approach to the to
- Speicher, Andreas,Groh, Matthias,Hennrich, Markus,Huynh, Anh-Minh
-
experimental part
p. 6760 - 6778
(2011/03/18)
-
- AMINOQUINOLINE COMPOUNDS
-
The present invention relates to a compound of Formula (1) or pharmaceutically acceptable salts thereof. The compound of Formula (1) is useful for treating a disease for which a MTP and/or APO B secretion inhibitor is indicated.
- -
-
Page/Page column 10; 32
(2010/04/03)
-
- A synthesis-driven structure revision of 'plagiochin E', a highly bioactive bisbibenzyl
-
Recently, a bisbibenzyl named plagiochin E showing remarkable antifungal and antitumor activities was isolated from Marchantia polymorpha, a liverwort. The total synthesis of the proposed structure for plagiochin E and of two structurally and biosynthetic
- Speicher, Andreas,Groh, Matthias,Zapp, Josef,Schauml?ffel, Anu,Knauer, Michael,Bringmann, Gerhard
-
scheme or table
p. 1852 - 1858
(2009/12/05)
-
- BORON-CONTAINING SMALL MOLECULES
-
This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
- -
-
Page/Page column 225-226
(2009/01/23)
-
- Preparation and Palladium-Catalyzed Cross-Coupling of Aryl Triethylammonium Bis(catechol) Silicates with Aryl Triflates
-
Pentavalent aryl and heteroaryl bis(catechol) silicates undergo palladium-catalyzed cross-coupling with aryl and heteroaryl triflates in the presence of a fluoride source in excellent yields. These solid, air-stable bis(catechol) silicates are prepared from a high-yielding displacement reaction between catechol and an aryl siloxane in the presence of an amine base. The cross-coupling reaction is tolerant of a wide range of electron-donating and electron-withdrawing groups. Several examples of di-ortho-substituted triflates are successfully coupled with these reagents.
- Seganish, W. Michael,DeShong, Philip
-
p. 1137 - 1143
(2007/10/03)
-
- Benzazine derivatives as phosphodiesterase 4 inhibitors
-
Compounds of formula I: wherein A is a heterocycle containing a nitrogen atom and optionally saturated or unsaturated and optionally further substituted by an oxo group (═O); R is: hydrogen, cyano, (C1-4)alkoxycarbonyl, carbamoyl; optionally substituted (C4-7)-cycloalkyl, aryl or heterocycle; (C1-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl optionally branched and/or substituted by (C4-7) cycloalkyl, aryl or heterocycle; aryloxy, heterocyclyloxy, aryl(C1-4)alkoxy, heterocyclyl(C1-4)alkoxy, amino substituted by one or two (C1-4)alkyl group(s), aryl-amino, heterocyclyl-amino, aryl(C1-4)alkyl-amino, or heterocyclyl(C1-4)alkylamino; Y is methylene or ethylene; W is an optionally substituted aryl or heterocycle; R1is hydrogen, (C4-7)cycloalkyl or a (C2-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl group optionally substituted by hydroxy, oxo, (C4-7)cycloalkyl, aryl or heterocycle, and optionally interrupted by one or more heteroatom(s) or heterogroup(s); R2is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; the N→O derivatives of the compounds of formula I and the pharmaceutically acceptable salts thereof. The compounds of formula (I) are PDE 4 inhibitors and may be used in compositions and methods involving PDE 4 inhibition.
- -
-
-
- Fast Synthesis of Aryl Triflates with Controlled Microwave Heating
-
matrix presented Synthesis of aryl triflates from phenols using N-phenyltriflimide requires only 6 min for completion when conducted with controlled microwave heating. The methodology was applied to both solution- and solid-phase conditions. Ten different
- Bengtson, Anna,Hallberg, Anders,Larhed, Mats
-
p. 1231 - 1233
(2007/10/03)
-
- Triaromatic compounds and pharmaceutical/cosmetic compositions comprised thereof
-
Novel pharmaceutically/cosmetically-active triaromatic compounds have the structural formula (I): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
- -
-
-
- Biaryl diacid inhibitors of human s-PLA2 with anti-inflammatory activity
-
Twenty-four hydrophobic dicarboxylic acids are described which were evaluated as inhibitors of 14 kDa human platelet phospholipase A2 (HP- PLA2). In general, biarylacetic acid derivatives were found to be more active than biaryl acids or biarylpropanoic acids. More potent inhibitors were obtained when hydrophobic groups were attached to the biaryl acid nucleus using an olefin linkage as compared to an ether linkage. Compounds with larger hydrophobic groups were usually more potent inhibitors of HP- PLA2. Five of the compounds disclosed in this report (2, 4, 28, 36b and 36i) were found to possess significant anti-inflammatory activity in a phorbol ester induced mouse ear edema model of chronic inflammation. (C) 2000 Elsevier Science Ltd.
- Springer, Dane M.,Luh, Bing-Yu,Bronson, Joanne J.,McElhone, Katharine E.,Mansuri, Muzammil M.,Gregor, Kurt R.,Nettleton, David O.,Stanley, Paul L.,Tramposch, Kenneth M.
-
p. 1087 - 1109
(2007/10/03)
-
- A Novel Palladium-Mediated Cascade Reaction Triggered by Strain Release of the Cyclobutane System. A New General Route to Benzo- and Naphthohydrindans
-
A novel palladium-mediated cascade reaction was reported.By this procedure, the olefinic cyclobutanols 17, 24, and 31; 41; 37; and 45 afforded the benzo- and naphthohydrindans (46-49, 50-53, 54-57, and 58-61) respectively in one operation in the ratios depending on the mediators and solvents employed.This provides a novel and efficient synthesis of biologically important A-nor and C11-alkylated steroids.
- Nemoto, Hideo,Miyata, Junji,Yoshida, Masahiro,Raku, Naomi,Fukumoto, Keiichiro
-
p. 7850 - 7857
(2007/10/03)
-
- BIARYL PHOSPHOLIPASE A2 INHIBITORS
-
Certain novel biaryl compounds are effective phospholipase A2 (PLA2) inhibitors.
- -
-
-
- Palladium-Catalyzed Cross-Coupling Reactions of Highly Hindered, Electron-Rich Phenol Triflates and Organostannanes
-
The palladium-catalyzed cross-coupling reaction of highly hindered, electron-rich phenol triflates and organostannanes (Stille reaction) has been studied in a systematic manner.The following are its salient features: (1) electron-rich phenol triflates require triphenylphosphine to undergo palladium-catalyzed cross-couplings; (2) in general, efficient reactions take place only when larger-than-usual amounts (10-15percent) of palladium are employed.On the reagent side, alkyl- (methyl only), allyl-, vinyl- and alkinylstannanes undergo efficient cross-couplings with the titlesubstrates.However, some limitations to this novel entry to 2-substituted resorcinols exist in regard to both substrates and reagents.Thus, conformationally rigid (hexasubstituted) aryl triflates behave poorly, demethylation being an important side reaction.Moreover, alkyl groups other than methyl cannot be introduced because β elimination occurs more rapidly.The potentially powerful synthesis of hindered biaryls has also been studied briefly.In the present conditions, the reaction appears to be limited by the presence of ortho substituents on the arylstannane moiety.
- Saa, Jose M.,Martorell, Gabriel,Garcia-Raso, Angel
-
p. 678 - 685
(2007/10/02)
-