- Total Synthesis of Asparenydiol by Two Sonogashira Cross-Coupling Reactions Promoted by Supported Pd and Cu Catalysts
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Asparenydiol, which is an important natural compound with potential pharmacological activities, was synthesized through two Sonogashira cross-coupling reactions catalyzed by supported Pd and Cu catalysts and by a Mitsunobu etherification. The optimization
- Angelici, Gaetano,Carpita, Adriano,Casotti, Gianluca,Evangelisti, Claudio,Ferreri, Matteo,Fusini, Graziano,Pardini, Luca Fidia
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p. 1795 - 1803
(2020/06/08)
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- Efficient synthesis of 3-benzoyl Benzo[b]thiophenes and raloxifene via Mercury(II)-Catalyzed cyclization of 2-alkynylphenyl alkyl sulfoxides
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The unique selective estrogen receptor modulator, Raloxifene (1), and antitubulin agent 2 were synthesized through the key intermediate, 4-methoxybenzyl 2-bromo-4-methoxyphenyl sulfoxide (6), respectively. It was found that compared with the o-sulfanyl aryl bromides, the sulfinyl group at ortho position accelerated the Sonogashira coupling reaction of aryl bromides. Thus, compound 6 was coupled with 3,4,5-trimethoxyphenyl acetylene, followed by mercury-catalyzed cyclization reaction afford compound 2 in 79% overall yield. Raloxifene (1) was prepared from compound 6 in four steps and 33% overall yield via coupling reaction with 1-trimethylsily-2-(4-tert-butyldimethylsiloxy)phenylethyne, mercury-catalyzed cyclization reaction, alkylation and demethylation.
- Wen, Shi-Ming,Lin, Cheng-Han,Chen, Chin-Chau,Wu, Ming-Jung
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p. 2493 - 2499
(2018/04/16)
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- AN ISOXAZOLE DERIVATIVES AS NUCLEAR RECEPTOR AGONISTS AND USED THEREOF
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The present invention relates to isoxazole derivatives, including pharmaceutical compositions and for the preparation of isoxazole derivatives. And more particularly the present invention provided a pharmaceutical composition of isoxazole derivatives for activation of Farnesoid X receptor(FXR, NR1H4).
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- Sulfoxide compound and method of producing benzothiophene derivatives using the same
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A sulfoxide compound and method of producing benzothiophene derivatives using the same are provided. The sulfoxide compound is represented by formula (I), wherein R1 and R2 are individually and independently benzoyl group; alkyl, acyl or silyl group of C1-C6 straight chain or branched chain; or alkenyl group of C3-C6 straight chain or branched chain; and X is halogen atom. The sulfoxide compound reacts with alkynyl compound, and then the synthesis efficiency of benzothiophene derivatives can be effectively increased.
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Page/Page column 12; 13
(2017/09/26)
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- A p-[18F]fluoroethoxyphenyl bicyclic nucleoside analogue as a potential positron emission tomography imaging agent for varicella-zoster virus thymidine kinase gene expression
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We recently reported a new positron emission tomography (PET) reporter gene, namely, varicella-zoster virus thymidine kinase (VZV-tk) in combination, with carbon-11 or fluorine-18 labeled m-alkoxyphenyl bicyclic nucleoside analogues (BCNAs) as PET reporte
- Chitneni, Satish K.,Deroose, Christophe M.,Balzarini, Jan,Gijsbers, Rik,Celen, Sofie,Debyser, Zeger,Mortelmans, Luc,Verbruggen, Alfons M.,Bormans, Guy M.
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p. 6627 - 6637
(2008/09/17)
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- Photo-cross-coupling reaction of electron-rich aryl chlorides and aryl esters with alkynes: A metal-free alkynylation
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(Chemical Equation Presented) Photoheterolysis of aryl halides substituted with electron-donating groups (EDGs) or aryl esters in 2,2,2-trifluoroethanol (TFE) leads to phenyl cations, which can add to alkynes (see scheme, Tf = trifluoromethanesulfonyl). This reaction is an appealing metal-free alternative to the (sila)-Sonogashira reaction.
- Protti, Stefano,Fagnoni, Maurizio,Albini, Angelo
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p. 5675 - 5678
(2007/10/03)
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- Silver(I)-catalysed protiodesilylation of 1-(Trimethylsilyl)-1-alkynes
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A procedure for protiodesilylation of 1-(trimethylsilyl)-1-alkynes that involves the use of catalytic amounts of AgNO3 and does not require the employment of KCN is described. This procedure allows for chemoselective deprotection of 1-(trimethylsilyl)-1-alkynes containing α-(trimethylsilyl) benzyl moieties, tert-butyldiphenylsilyl alkyl ethers or tert-butyldimethylsilyl aryl ether groups. However, it causes complete desilylation of l-(trimethylsilyl)-1-alkynes characterised by a primary alcoholic group protected as a tert-butyldimethylsilyl ether. Interestingly, compounds that contain this last functional group can also furnish the corresponding alcohols by treatment with a catalytic amount of aqueous HNO3. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.
- Carpita, Adriano,Mannocci, Luca,Rossi, Renzo
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p. 1859 - 1864
(2007/10/03)
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