- Chemoselective One-Pot Synthesis of Functionalized Amino-azaheterocycles Enabled by COware
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Functionalized bicyclic amino-azaheterocycles are rapidly accessed in a one-pot cross-coupling/reduction sequence enabled by the use of COware. Incompatible reagents are physically separated in a single reaction vessel to effect two chemoselective transformations - Suzuki-Miyaura cross-coupling and heteroarene reduction. The developed method allows access to novel heterocyclic templates, including semisaturated Hedgehog and dual PI3K/mTOR inhibitors, which show enhanced physicochemical properties compared to their unsaturated counterparts.
- Clohessy, Thomas A.,Roberts, Alastair,Manas, Eric S.,Patel, Vipulkumar K.,Anderson, Niall A.,Watson, Allan J. B.
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supporting information
p. 6368 - 6371
(2017/12/08)
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- INDOLOACRIDINE-CONTAINING DERIVATIVE, PREPARATION PROCESS AND USE THEREOF, AND ORGANIC LUMINESCENT DEVICE
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The disclosure provides an indoloacridine-containing derivative represented by formula (I), wherein A is a group represented by formula (II), and wherein X, Y, Z and W represent a carbon atom or a nitrogen atom, and at least one of W, X, Y and Z represent a nitrogen atom; R represents a phenyl group, a biphenylyl group, a naphthyl group or a phenanthryl group. The disclosure further provides a process for preparing the compound. The disclosure further provides an organic electroluminescent device comprising the compound. This compound can be used as a phosphorescence host material, a hole-injecting material or a hole-transporting material in an organic electroluminescent device.
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Paragraph 0113-0114
(2016/03/22)
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- Convenient synthesis of 2,4-disubstituted pyrido[2,3-d]pyrimidines via regioselective palladium-catalyzed reactions
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A novel and effective route for the synthesis of 2,4-disubstituted pyrido[2,3-d]pyrimidines III is reported starting from the corresponding 2,4-dichloropyridopyrimidine 1 through regioselective functionalization palladium-catalyzed C-C coupling reactions, by two successive palladium-catalyzed reactions involving an original regioselective chlorine discrimination. Alternatively, type III compounds were elaborated from 2 by C-2 chlorine further displacement of the C-4 isopropylsulfanyl group, which acted as a temporary C-4 protecting group. Further Suzuki-Miyaura cross-coupling reactions led to C-2 and C-4 disubstituted compounds.
- Riadi, Yassine,Massip, Stephane,Leger, Jean-Michel,Jarry, Christian,Lazar, Sa?d,Guillaumet, Gérald
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supporting information; experimental part
p. 5018 - 5024
(2012/08/07)
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- INHIBITORS OF THE HEDGEHOG PATHWAY
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The present invention is directed to a compound of Formula (I) or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula (I) to treat cancer.
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