- β-elimination of a phosphonate group from an alkoxy radical: An intramolecular acylation approach using an acylphosphonate as a carbonyl group acceptor
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On the basis of facile β-elimination of a phosphonate group from an alkoxy radical, intramolecular acylation reaction has been developed, in which an acylphosphonate is used as an excellent carbonyl group radical acceptor. Copyright
- Kim, Sunggak,Cho, Chang Ho,Lim, Chae Jo
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Read Online
- Synthesis and assignment of the absolute configuration of the anti-Helicobacter pylori agents CJ-12,954 and CJ-13,014
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The synthesis of the spiroacetal-containing anti-Helicobacter pylori agents (3S,2″S,5″S,7″S)-1a (ent-CJ-12,954) and (3S,2″S, 5″R,7″S)-2a (ent-CJ-13,014) has been carried out based on the convergent union of a 1: 1 mixture of heterocycle-activated spiroace
- Brimble, Margaret A.,Bryant, Christina J.
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Read Online
- New method for promoting photosensitive oxidation to remove 1, 2-mercaptoethanol acetal protecting group by utilizing visible light irradiation
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The invention discloses a new method for removing a 1, 2-mercaptoethanol acetal protecting group, and belongs to the field of organic synthetic chemistry. The method comprises the following steps of:under a room-temperature open system, adding a substrate 2-substituted-1, 3-oxo-thio-cyclopentane and a catalytic amount of a photosensitizer Eosin Y into a proper amount of acetonitrile; and performing irradiating with a blue LED lamp for 3 hours while stirring to obtain the corresponding aldehyde compound with favorable yield. The method has the advantages of mild operation conditions, greenness, environmental protection, no harsh water and oxygen removal operation and device, realization of the reaction at room temperature, high substrate conversion rate, simple and easy post-treatment, andprovides a good method for removing the 1, 2-mercaptoethanol acetal protecting group at present.
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Paragraph 0014-0016
(2021/01/30)
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- Copper-catalyzed enantioselective synthesis of bridged bicyclic ketals from 1,1-disubstituted-4-methylene-1,6-hexanediols and related alkenols
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Bridged bicyclic ketals display a range of bioactivities. Their catalytic enantioselective synthesis from acyclic 1,1-disubstituted alkene diols is disclosed. This reaction combines asymmetric catalysis with a distal radical migration. Alkynes and arenes
- Burde, Ameya S.,Karyakarte, Shuklendu D.,Sylvester, Eric D.,Chemler, Sherry R.
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p. 105 - 108
(2021/01/14)
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- Chemoenzymatic process for the preparation of (S)-7-((tert-butyldiphenylsilyl)oxy)hept-1-yn-4-ol in a continuous packed-bed reactor, a key intermediate for eribulin synthesis
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A practical chemoenzymatic process has been developed for the preparation of optically pure (S)-7-((tertbutyldiphenylsilyl) oxy)hept-1-yn-4-ol, (S)-4. This was prepared via enantioselective acylation of racemic homopropargylic alcohol (+/-)-4 catalyzed by
- Basetty, Shalini,Chandrasekhar, Srivari,Ghosh, Subhash,Krishna, Avula Shiva,Kumaraguru, Thenkrishnan,Mainkar, Prathama S.,Nasam, Rajesh,Pabbaraja, Srihari,Ralte, Samuel L.,Reddy, Chada Raji,Sudhakar, Gangarajula
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p. 2657 - 2664
(2020/12/29)
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- Visible light photoredox catalyzed deprotection of 1,3-oxathiolanes
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An efficient visible light photoredox catalyzed aerobic deprotection of 1,3-oxathiolanes using organic dye Eosin Y as a photocatalyst is disclosed. The deprotection procedure features the use of a metal-free catalyst, mild conditions, a broad range of substrate scope, and good functional group tolerance. 35 examples were tested under the standard conditions and most of them afforded the deprotected products in modest to high yields.
- Yang, Mingyang,Xing, Zhimin,Fang, Bowen,Xie, Xingang,She, Xuegong
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supporting information
p. 288 - 291
(2020/01/13)
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- FUSED TRICYCLIC HETEROCYCLE COMPOUNDS AND THERAPEUTIC USES THEREOF
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This application discloses a new class of fused tricyclic heterocycles of formula (I), preparation methods thereof, pharmaceutical compositions comprising these compounds, and pharmaceutically acceptable salts, solvates, or prodrugs thereof, and their use
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- TRICYCLIC COMPOUNDS AS STING AGONISTS, AND PREPARATION METHODS AND MEDICINAL USES THEREOF
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Compounds of formula (I) useful as agonists of stimulator of interferon genes (STING), the preparation method therefor, pharmaceutcal compositions comprising the compounds, and the pharmaceutical uses for the treatment of STING-mediated diseases or disord
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- Intermediate for preparing halichondrin compound and preparation method thereof
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The invention relates to an intermediate for preparing a halichondrin compound and a preparation method thereof. The invention particularly relates to an intermediate for preparing halichondrin, eribulin or analogues thereof, and a preparation method and application of the intermediate. The intermediate as well as the preparation method and application thereof are used for constructing C20-C26 structural fragments of the halichondrin compound. The initial raw materials of the synthesis route are cheap, easy to obtain, stable in source and reliable in quality; the structural characteristics ofreactants are fully utilized in the selection of a chiral center construction method, so that the synthesis efficiency is practically improved, and the difficulty and risk of product quality control are reduced; and the use of a high-toxicity and expensive organic tin catalyst is avoided, so that the cost and the environmental friendliness are remarkably improved.
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Paragraph 0132; 0160-161
(2020/07/07)
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- PYRROLIDINE DERIVATIVE
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The present invention aims to provide a novel compound which has CGRP receptor antagonist activity and which is useful for the treatment of various diseases mediated by CGRP receptors. That is, the present invention relates to the pyrrolidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. In the formulae, W is ring, X is a carbon atom or the like, Y1 to Y4 are carbon atoms or the like, and R1 to R7 is alkyl or the like. The compounds of the present invention or a pharmaceutically acceptable salt thereof have an excellent CGRP receptor antagonist activity, and thus are useful as agents for the treatment of various diseases mediated by CGRP receptors.
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- Chemoselective deoxygenation of ether-substituted alcohols and carbonyl compounds by B(C6F5)3-catalyzed reduction with (HMe2SiCH2)2
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B(C6F5)3-catalyzed deoxygenation of ether-substituted alcohols and carbonyl compounds has been developed using (HMe2SiCH2)2 as the reductant. This unique reagent shows distinct superiority over traditional one silicon-centered hydrosilanes, giving the corresponding alkanes in high yields with good tolerance of ethers, aryl halides and alkenes. The control experiments suggest that (HMe2SiCH2)2 might facilitate the approach in an intramolecular Si/O activation manner.
- Yang, Wenyu,Gao, Lu,Lu, Ji,Song, Zhenlei
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p. 4834 - 4837
(2018/05/23)
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- Tuning Regioselectivity of Wacker Oxidation in One Catalytic System: Small Change Makes Big Step
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A regioselectivity switchable aerobic Wacker-Tsuji oxidation has been developed using catalytic tert-butyl nitrite as a simple organic redox cocatalyst. By solely switching the solvent, either substituted aldehydes or ketones could be prepared under mild
- Hu, Kang-Fei,Ning, Xiao-Shan,Qu, Jian-Ping,Kang, Yan-Biao
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p. 11327 - 11332
(2018/09/06)
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- Iridium-Catalyzed Aerobic α,β-Dehydrogenation of γ,δ-Unsaturated Amides and Acids: Activation of Both α- And β-C-H bonds through an Allyl-Iridium Intermediate
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Direct aerobic α,β-dehydrogenation of γ, δ-unsaturated amides and acids using a simple iridium/copper relay catalysis system is described. We developed a new strategy that overcomes the challenging issue associated with the low α-acidity of amides and acids. Instead of α-C-H metalation, this reaction proceeds by β-C-H activation, which results in enhanced α-acidity. Conjugated dienamides and dienoic acids were synthesized in excellent yield with this reaction, which uses a simple reaction protocol. Mechanistic experiments suggest a catalyst resting state mechanism in which both α-C-H and β-C-H cleavage is accelerated.
- Wang, Zhen,He, Zhiqi,Zhang, Linrui,Huang, Yong
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p. 735 - 740
(2018/01/26)
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- Diastereoselective Synthesis of Highly Substituted Tetrahydrofurans by Pd-Catalyzed Tandem Oxidative Cyclization-Redox Relay Reactions Controlled by Intramolecular Hydrogen Bonding
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Palladium-catalyzed oxidative cyclization of alkenols provides a convenient entry into cyclic ethers but typically proceeds with little or no diastereoselectivity for cyclization of trisubstituted olefins to form tetrahydrofurans due to the similar energi
- Brooks, Joshua L.,Xu, Liping,Wiest, Olaf,Tan, Derek S.
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supporting information
p. 57 - 75
(2017/04/26)
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- Tert-Butyl Nitrite: Organic Redox Cocatalyst for Aerobic Aldehyde-Selective Wacker-Tsuji Oxidation
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An aldehyde-selective aerobic Wacker-Tsuji oxidation is developed. Using tert-butyl nitrite as a simple organic redox cocatalyst instead of copper or silver salts, a variety of aldehydes were achieved as major products in up to 30/1 regioselectivity as well as good to high yields at room temperature.
- Ning, Xiao-Shan,Wang, Mei-Mei,Yao, Chuan-Zhi,Chen, Xian-Min,Kang, Yan-Biao
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p. 2700 - 2703
(2016/06/15)
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- Synthesis of long-chain fatty acid derivatives as a novel anti-Alzheimer's agent
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In order to develop new drugs for Alzheimer's disease, we prepared 17 fatty acid derivatives with different chain lengths and different numbers and positions of double bonds by using Wittig reaction and stereospecific hydrogenation of triple bonds as key reactions. Among them, (4Z,15Z)- octadecadienoic acid (10) and (23Z,34Z)-heptatriacontadienoic acid (16) showed the most potent neurite outgrowth activities on Aβ(25-35)-treated rat cortical neurons, which activities were comparable to that of a positive control, NGF. Both fatty acids 10 and 16 possess two (Z)-double bonds at the n-3 and n-14 positions, which might be important for the neurite outgrowth activity.
- Zhang, Hong-Yan,Yamakawa, Yu-Ichiro,Matsuya, Yuji,Toyooka, Naoki,Tohda, Chihiro,Awale, Suresh,Li, Feng,Kadota, Shigetoshi,Tezuka, Yasuhiro
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p. 604 - 608
(2014/01/23)
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- One-pot sequential 1,4- and 1,2-reductions of α,β-unsaturated δ-lactones to the corresponding δ-lactols with CuCl and NaBH 4 in methanol
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An efficient, one-pot method for the highly chemoselective synthesis of δ-lactols from α,β-unsaturated δ-lactones using CuCl and NaBH4 in methanol was developed. Georg Thieme Verlag Stuttgart. New York.
- Matsumoto, Yasunobu,Yonaga, Masahiro
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p. 1764 - 1768
(2014/08/05)
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- Boronic acid catalysis as a mild and versatile strategy for direct carbo- and heterocyclizations of free allylic alcohols
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BAC to the future: Boronic acid catalysis (BAC) was applied to the direct activation of alcohols leading to the preparation of carbocycles (see scheme), benzofurans, tetrahydrofurans, pyrrolidines, pyrans, piperidines, and various polycyclic compounds. The reactions proceed under mild conditions that circumvent the use of reactive leaving groups like halides. Copyright
- Zheng, Hongchao,Ghanbari, Sina,Nakamura, Shinji,Hall, Dennis G.
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p. 6187 - 6190
(2012/08/13)
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- Synthesis of antineoplastic analogs of aplysiatoxin with various side chain structures
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We have recently developed a simplified analog of aplysiatoxin with anti-proliferative activity (1). To investigate the structure-activity relationship of its side chain, an alternative synthetic route of 1 has been established. Via the key intermediate 6
- Shu, Yuki,Yanagita, Ryo C.,Tokuda, Harukuni,Suzuki, Nobutaka,Irie, Kazuhiro
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p. 281 - 303
(2013/08/23)
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- Zwitterionic aza-Claisen rearrangements controlled by pyrrolidine auxiliaries-useful key steps in convergent enantioselective syntheses
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Chiral pyrrolidine substituents served as efficient auxiliaries in diastereoselective zwitterionic ketene aza-Claisen rearrangements. Palladium-catalysed N-allylation starting from optically active proline and prolinol derivatives, as well as from (2S,5S)-2,5-dimethoxymethylpyrrolidine, gave various allylamines bearing trisubstituted olefin moieties. Treatment with complex carboxylic acid fluorides in the presence of trimethylaluminium induced activated ketene addition to the nitrogen and subsequent [3,3] sigmatropic rearrangement to give γ,δ-unsaturated amides with excellent simple diastereoselectivities and up to 11:1 auxiliary-induced diastereomeric ratios. Cleavage of the pyrrolidine amide was achieved through iodolactonization, with the option for recovery of the auxiliary pyrrolidine. The stereochemical outcomes of the rearrangements and the iodocyclizations were established by X-ray and NOEDS analyses of suitable amides and lactones. Overall, both enantiomers were accessible selectively. The optically active amides and lactones of defined configurations formed in this way should be useful as key intermediates in convergent steroidal natural and pharmaceutically important product synthesis. Enantiopure N-allylpyrrolidines and 4-arylbut-3-enoyl fluorides underwent zwitterionic aza-Claisen rearrangements in high yields, as well as with high simple and up to 11:1 auxiliary-induced diastereoselectivities. After selective olefin hydrogenation, iodocyclization and pyrrolidine removal enabled synthesis of the lactones. Both enantiomers of target molecules could be achieved selectively.
- Friedemann, Nora M.,Haerter, Alice,Brandes, Sebastian,Gross, Steffen,Gerlach, Dorothea,Muench, Winfried,Schollmeyer, Dieter,Nubbemeyer, Udo
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supporting information; experimental part
p. 2346 - 2358
(2012/05/20)
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- A formal synthesis of vinigrol
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Two key reactions in a rapid assembly of the tricyclic core of vinigrol are a stereoselective Claisen rearrangement and an intramolecular Diels-Alder reaction. The method paves the way for a total synthesis of this synthetically challenging and biologically interesting natural product. Copyright
- Poulin, Jason,Grise-Bard, Christiane M.,Barriault, Louis
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supporting information; experimental part
p. 2111 - 2114
(2012/04/10)
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- Total synthesis of iso- and bongkrekic acids: Natural antibiotics displaying potent antiapoptotic properties
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For over five decades, owing to their antiapoptotic activities, bongkrekic and isobongkrekic acids have generated interest from the scientific community. Here, we disclose full details of our investigation into the synthesis of isobongkrekic acid, which culminated in its first preparation and features various palladium-catalysed cross-couplings and Takai olefination reactions. Access to bongkrekic acid is also reported by this route. These syntheses involve the preparation and use of new general building blocks which could find wider applications. Iso-bong: A versatile first synthesis of isobongkrekic acid (IBA) has been developed. Key steps include three different palladium cross-couplings and an asymmetric homopropargylation. In-depth synthetic studies reveal the challenges faced in generating the right geometry of each diene.
- Francais, Antoine,Leyva-Perez, Antonio,Etxebarria-Jardi, Gorka,Pena, Javier,Ley, Steven V.
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p. 329 - 343
(2011/03/21)
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- Synthesis of a platform to access bistramides and their analogues
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The platform C14-C40, which can be used to prepare bistramide C and 39-oxobistramide K, was synthesized in 19 steps with an overall yield of 6.2%. Furthermore, the chemoselective reduction of the ketone at C-39 was performed giving an easy access to bistramides A, B, D, K, and L. Finally, the versatility of the synthesis of the C14-C40 fragment can allow the preparation of a large variety of stereoisomers to produce bistramide analogues.
- Commandeur, Malgorzata,Commandeur, Claude,Cossy, Janine
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p. 6018 - 6021
(2011/12/16)
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- Tandem cycloaddition reactions of allenyl diazo compounds forming triquinanes via trimethylenemethane diyls
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A tandem reaction strategy for forming triquinanes from linear allenyl diazo compounds through an intramolecular 1,3-dipolar cycloaddition reaction of an allenyl diazo group that generates a trimethylenemethane (TMM) diyl followed by an intramolecular [2
- Kang, Taek,Kim, Won-Yeob,Yoon, Yeokwon,Kim, Byung Gyu,Lee, Hee-Yoon
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p. 18050 - 18053
(2011/12/13)
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- Synthesis of disubstituted 1,2-dioxolanes, 1,2-dioxanes, and 1,2-dioxepanes
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A route to cyclic peroxides containing 1,2-dioxolane, 1,2-dioxane or 1,2-dioxepane rings is described. These compounds present simpler structures related to the bicyclic core of stolonoxides, metabolites with marked cytotoxicity against several mammalian
- Guerra, Francisco M.,Zubía, Eva,Ortega, María J.,Moreno-Dorado, F. Javier,Massanet, Guillermo M.
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scheme or table
p. 157 - 163
(2010/03/01)
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- Hydroxamic acid derivatives of 4-phenyl 4-hydroxy, 4-phenyl 4-alkoxy and 4-phenyl 4-arylalkoxy butyric acid useful as therapeutic agents for treating anthrax poisoning
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Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of 4-phenyl-4-hydroxy-butyric acid and capable of inhibiting the lethal effects of infection by anthrax bacteria and are usefu
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(2010/12/29)
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- Synthesis of the C1-C12 acid fragment of amphidinolide T marine macrolides via SmI2-mediated enantioselective reductive coupling of aldehydes with a chiral crotonate
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A new strategy for enantioselective assembly of the trisubstituted tetrahydrofuran ring has been established for synthesis of the C1-C12 acid fragment of amphidinolide T series marine macrolides. The key steps involve the SmI2-mediated highly e
- Luo, Jialu,Li, Huoming,Wu, Jinlong,Xing, Xinglong,Dai, Wei-Min
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experimental part
p. 6828 - 6833
(2009/12/06)
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- Concise asymmetric synthesis of antimalarial alkaloid (+)-febrifugine
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An asymmetric total synthesis of antimalarial alkaloid (+)-febrifugine is accomplished in 23% overall yield over 14 steps from readily available starting materials. The synthesis features a SmI2-mediated reductive cross-coupling of chiral N-ter
- Wang, Rui,Fang, Kai,Sun, Bing-Feng,Xu, Ming-Hua,Lin, Guo-Qiang
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body text
p. 2301 - 2304
(2009/12/08)
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- Synthetic studies toward neovibsanins A and B: construction of the neovibsanin core utilizing palladium(0)-catalyzed carbonylative cyclization with carbon monoxide
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The core A-ring of neovibsanins A (1) and B (2), which are potent neurotrophic agents isolated from the leaves of Viburnum awabuki, have been effectively constructed by the intramolecular palladium(0)-catalyzed carbonylative cyclization of alkenyl iodide
- Esumi, Tomoyuki,Zhao, Ming,Kawakami, Taishi,Fukumoto, Mayuna,Toyota, Masao,Fukuyama, Yoshiyasu
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p. 2692 - 2696
(2008/09/19)
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- Synthesis of 3-(carboxyarylalkyl)imidazo[2,1-f][1,2,4]triazines as potential inhibitors of AMP deaminase
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C-Ribosyl 1,2,4-triazolo[1,2,4]triazines which are able to undergo covalent hydration are of interest as potential inhibitors of AMP deaminase. In a search for compounds with improved bioavailability we have synthesized compounds in which the sugar has been replaced by carboxyarylalkyl based ribose phosphate mimics. The target carboxyarylalkyl imidazotriazines 11 and 12 were synthesized using a linear seven step sequence starting from simple benzoate derivatives. Alternatively, the hydroxyethyl imidazotriazine 39 is available in five steps and this synthon was used to prepare the imidazotriazines 34 and 48 in a short convergent manner.
- Kirkman, Joseph K.,Lindell, Stephen D.,Maechling, Simon,Slawin, Alexandra M. Z.,Moody, Christopher J.
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supporting information; experimental part
p. 4452 - 4459
(2009/02/07)
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- Organocatalysis in a synthetic receptor with an inwardly directed carboxylic acid
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A cavitand functionalized with a Kemp-s triacid derivative was used to catalyze the epoxide ring-opening cyclizations of 1,5-epoxyalcohols. A deep, cylindrical cavity containing electron-rich aromatic walls and an inwardly directed carboxylic acid displayed the necessary characteristics to bind different 1,5-epoxyalcohols and initiate their cyclization reactions. The reactions inside this synthetic receptor occurred in a catalytic and regioselective manner. These results highlight that the arrangement of functionality and unique solvation provided by the structured interiors of natural enzymes can be incorporated into synthetic systems having useful physical and chemical properties. Copyright
- Shenoy, Siddhartha R.,Pinacho Crisostomo, Fernando R.,Iwasawa, Tetsuo,Rebek Jr., Julius
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p. 5658 - 5659
(2008/12/21)
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- Improved synthesis of the polyhydroxylated central part of phoslactomycin B
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A new approach to the C(7)-C(13) intermediate for the synthesis of phoslactomycin B was investigated. Asymmetric dihydroxylation of the β,γ-unsaturated ester proceeded cleanly to afford the β-hydroxyl-γ-lactone with 97.6% ee, which upon protection as the
- Nonaka, Hisato,Maeda, Noriaki,Kobayashi, Yuichi
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p. 5601 - 5604
(2008/03/11)
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- A catalytic asymmetric vinylogous mukaiyama aldol reaction
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A vinylogous Mukaiyama aldol reaction, conducted using 10 mol % of a BITIP catalyst and B(OMe)3 as an additive, effects an enantioselective four-carbon chain extension to give versatile Eαβ-unsaturated thiol esters.
- Heumann, Lars V.,Keck, Gary E.
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p. 4275 - 4278
(2008/02/13)
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- Fully reagent-controlled asymmetric synthesis of (-)-Spongidepsin via the Zr-catalyzed asymmetric carboalumination of alkenes (ZACA reaction)
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The ZACA reaction has been shown to proceed satisfactorily with internally OH-substituted 1-alkenes, provided that the OH group is unprotected and non-allylic. This reaction was used for reagent-controlled asymmetric construction of 3. Allylic alcohol was
- Zhu, Gangguo,Negishi, Ei-Ichi
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p. 2771 - 2774
(2008/02/07)
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- Diaryl substituted pyrazoles as potent CCR2 receptor antagonists
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We have identified and synthesized a series of diaryl substituted pyrazoles as potent antagonists of the chemokine receptor subtype 2. Structure-activity relationship studies directed toward improving the potency led to the discovery of 23 (IC50/sub
- Pinkerton, Anthony B.,Huang, Dehua,Cube, Rowena V.,Hutchinson, John H.,Struthers, Mary,Ayala, Julia M.,Vicario, Pasquale P.,Patel, Sima R.,Wisniewski, Thomas,DeMartino, Julie A.,Vernier, Jean-Michel
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p. 807 - 813
(2007/10/03)
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- Stereoselective synthesis of the C(53)-C(67) polyene fragment of amphidinol 3
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A stereoselective synthesis of the polyene fragment C(53)-C(67) of amphidinol 3 is described using a sequence of reduction, benzoylation, and reductive elimination for the stereospecific preparation of the polyene motif as key steps starting from acetylen
- Colobert, Fran?oise,Kreuzer, Thomas,Cossy, Janine,Reymond, Sébastien,Tsuchiya, Tomoki,Ferrié, Laurent,Marko, Istvan E.,Jourdain, Pierre
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p. 2351 - 2354
(2008/03/12)
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- BETA-GLUCURONIDE-LINKER DRUG CONJUGATES
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Ligand Drug conjugate compounds comprising a β-glucuronide-based linker and methods of using such compounds are provided.
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Page/Page column 96
(2010/11/25)
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- SYNTHESIS OF CHLORINS AND PHORBINES WITH ENHANCED RED SPECTRAL FEATURES
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The present invention provides compounds of the general Formula DI: along with methods of making such compounds, formulations containing the same, and methods of using the same (e.g., in photodynamic therapy, for the production of solar cells, etc.).
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Page/Page column 124-125
(2008/06/13)
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- Mild organocatalytic α-methylenation of aldehydes
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A rapid and extremely convenient method for α-methylenation of aldehydes with aqueous formaldehyde is described. Two optimal catalytic systems are presented that allow short reaction times and afford the functionalized products in good to excellent yields (up to 99%) and chemoselectivity.
- Erkkil?, Anniina,Pihko, Petri M.
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p. 2538 - 2541
(2007/10/03)
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- Dipeptide-based highly potent doxorubicin antibody conjugates
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Highly potent and novel derivatives of doxorubicin were linked to monoclonal antibodies (mAbs) for site-specific drug delivery. Drug linker 5 consisted of a dipeptide linker attached directly to the daunosamine nitrogen of the n-butyldiacetate doxorubicin
- Jeffrey, Scott C.,Nguyen, Minh T.,Andreyka, Jamie B.,Meyer, Damon L.,Doronina, Svetlana O.,Senter, Peter D.
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p. 358 - 362
(2007/10/03)
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- SUBSTITUTED PYRAZOLES AS MODULATORS OF CHEMOKINE RECEPTORS
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Substituted pyrazole compounds such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including al
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Page/Page column 31-32
(2008/06/13)
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- BASIC AMINE COMPOUND AND USE THEREOF
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Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A 1 and A 2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH 2 , C(=O), NR 11 , or CHR 35 and D represents a group represented by the following formula (6): where Q represents a single bond, NR 12 , or a group represented by the formula (13): and Y represents a group represented by the following formula (7) : where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents -NR 25 R 26 ; and R 1 to R 26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.
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Page/Page column 30
(2010/11/24)
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- β elimination of a phosphonate group from an alkoxyl radical - Intramolecular acylation using acylphosphonate derivatives as carbonyl group acceptors
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The possibility of β elimination of a phosphonate group in radical reactions was studied. The facile β elimination of the phosphonate group from an alkoxyl radical was observed for the first time, whereas the β elimination of the phosphonate group from an
- Cho, Chang Ho,Kim, Sunggak
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p. 917 - 921
(2007/10/03)
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- AMINE COMPOUNDS AND USE THEREOF
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It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1):In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(=O) or NR11; and D is a group represented by the following general formula (4) or (6).-Q-Y-BIn the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl.
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Page/Page column 115
(2010/02/12)
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- Stereoselective syntheses of rolliniastatin 1, rollimembrin, and membranacin
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A radical cyclization of β-alkoxyvinyl sulfoxides-Pummerer rearrangement-allylation protocol was successfully applied to the synthesis of the threol cis/threol cis/erythro bis-oxolane moiety in rolliniastatin 1 (1), rollimembrin (2), and membranacin (3).
- Keum, Gyochang,Hwang, Cheol Hee,Kang, Soon Bang,Kim, Youseung,Lee, Eun
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p. 10396 - 10399
(2007/10/03)
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- NOVEL HETEROCYCLIC COMPOUNDS AS HSP90-INHIBITORS
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Novel heterocyclic compounds are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agent. Method of synthesis and use of such compounds are also described.
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Page/Page column 268-269
(2008/06/13)
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- PYRIDIN-4-YLAMINE COMPOUNDS USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN
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The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorde
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Page/Page column 30
(2010/02/11)
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- Synthetic study on Pandanus Alkaloids: from Norpandamarilactonines to Pandamarilactonines, a Proof of their Configurational Instability
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The ethyl carbamate of norpandamarilactonine-A was prepared in an enantiomerically pure form starting from (S)-prolinol. Deprotection of the amine functionality rendered both diastereomeric norpandamarilactonines as racemates, which were used as synthetic precursors of pandamarilolactonine-A and -B.
- Blanco, Pilar,Busque, Felix,March, Pedro de,Figueredo, Marta,Font, Josep,Sanfeliu, Elena
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- Asymmetric total synthesis of (-)-callystatin A and (-)-20-epi-callystatin A employing chemical and biological methods
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An efficient asymmetric total synthesis of the potent cytotoxic marine natural product (-)-callystatin A and its 20-epi analogue has been achieved. The synthetic pathway involved the preparation of three fragments to be coupled with each other at the end of the route. The first fragment 3 was obtained using a biocatalytic enantioselective reduction of a 3,5-dioxocarboxylate as the key step. For the second intermediate 4 the asymmetric α-alkylation of an O-protected derivative of 4-hydroxybutanal was performed exploiting the SAMP/ RAMP hydrazone alkylation methodology, and followed by a highly Z-selective Homer-Wadsworth-Emmons reaction under modified conditions. For the synthesis of the polypropionate fragment 5 a diastereoselective syn-aldol reaction was employed between a chiral ethyl ketone and an α-substituted chiral aldehyde, both prepared in enantiopure form again by means of the asymmetric alkylation of their corresponding RAMP hydrazones. Finally, these three building blocks were coupled using highly E-selective Wittig reactions via allyltributylphosphonium ylides to afford the target compounds after a final oxidation/deprotection sequence.
- Enders, Dieter,Vicario, Jose L.,Job, Andreas,Wolberg, Michael,Mueller, Michael
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p. 4272 - 4284
(2007/10/03)
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- Total synthesis of four Pandanus alkaloids: Pandamarilactonine-A and -B and their chemical precursors norpandamarilactonine-A and -B
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Norpandamarilactonine-A and -B are prepared from (S)-prolinol and converted into pandamarilactonine-A and -B.
- Busqué, Félix,De March, Pedro,Figueredo, Marta,Font, Josep,Sanfeliu, Elena
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p. 5583 - 5585
(2007/10/03)
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