- Copper-catalyzed carboarylation of alkynes via vinyl cations
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Copper-catalyzed arylation of electron rich alkynes reveals stabilized trisubstituted vinyl cation equivalents that react with pendant arene nucleophiles to form all carbon tetrasubstituted alkenes. The new process streamlines the synthesis of important medicinally relevant molecules.
- Walkinshaw, Andrew J.,Xu, Wenshu,Suero, Marcos G.,Gaunt, Matthew J.
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supporting information
p. 12532 - 12535
(2013/09/23)
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- PROCESS FOR THE PREPARATION OF α-SUBSTITUTED KETONES AND THEIR APPLICATION IN SYNTHESIS OF PHARMACEUTICALLY ACTIVE COMPOUNDS
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The present invention relates to a novel one step preparation of 6-methoxy-2-phenyl-tetralone starting from 6-methoxy-tetralone and its use as an intermediate in the synthesis of pharmaceutically active compounds.
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- Process for the preparation of alfa-substituted ketones and their application in synthesis of pharmaceutically active compounds
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The present invention relates to a novel one step preparation of 6-methoxy-2-phenyl-tetralone starting from 6-methoxy-tetralone and its use as an intermediate in the synthesis of pharmaceutically active compounds.
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Page/Page column 14
(2012/12/13)
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- A PROCESS FOR THE PREPARATION OF LASOFOXIFENE TARTRATE
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The present invention relates to solid state chemistry of 1-(2-[4-(6-methoxy-3,4-dihydronaphthalene-1-yl) phenoxy]ethyl)pyrrolidine, a process for its preparation and its use as an intermediate in the synthesis of lasofoxifene.
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Page/Page column 20; 21
(2010/11/17)
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- Synthesis of lasofoxifene, nafoxidine and their positional isomers via the novel three-component coupling reaction
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A Lewis acid-mediated three-component coupling reaction was successfully applied for the synthesis of lasofoxifene (1), nafoxidine (2), and their positional isomers, inv-lasofoxifene (3) and inv-nafoxidine (4). In the presence of HfCl4, the des
- Nakata, Kenya,Sano, Yoshiyuki,Shiina, Isamu
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experimental part
p. 6773 - 6794
(2011/02/22)
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- PROCESS FOR PRODUCTION OF LASOFOXIFENE OR ANALOGUE THEREOF
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Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue the
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Page/Page column 20-21; 30
(2008/12/04)
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- An expeditious synthesis of lasofoxifene and nafoxidine via the novel three-component coupling reaction
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The simple and efficient synthesis of lasofoxifene (4), a possible candidate for alleviating osteoporosis, via the novel three-component coupling reaction among 4-pivaloyloxybenzaldehyde (5), cinnamyltrimethylsilane (6), and anisole in the presence of HfCl4 is illustrated. The successive cationic cyclization of the coupling product, olefin formation, and migration of the double-bond are performed to afford the common synthetic intermediate of lasofoxifene (4) and nafoxidine (3) via a very concise procedure. Copyright
- Sano, Yoshiyuki,Nakata, Kenya,Otoyama, Takafumi,Umeda, Sei,Shiina, Isamu
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