Catalytic Decarboxylative Cross-Coupling of Aryl Chlorides and Benzoates without Activating ortho Substituents
The restriction of decarboxylative cross-coupling reactions to ortho-substituted or heterocyclic carboxylate substrates was overcome by holistic optimization of a bimetallic Cu/Pd catalyst system. The combination of a CuI/Me4phen decarboxylation catalyst and a [(MeCN)4Pd](OTf)2/XPhos cross-coupling catalyst enables the synthesis of biaryls from inexpensive aryl chlorides and potassium benzoates regardless of their substitution pattern. Lifting the restriction: A combination of a CuI/Me4phen decarboxylation catalyst and a [(MeCN)4Pd](OTf)2/XPhos cross-coupling catalyst enables the synthesis of biaryls from inexpensive aryl chlorides and potassium benzoates regardless of their substitution pattern (see scheme; FG=functional group). This approach lifts the restriction of decarboxylative cross-coupling reactions to ortho-substituted or heterocyclic carboxylate substrates.
The present invention provides novel diarylurea derivatives (compounds of formula (I)) and their uses. The compounds of the present invention are demonstrated to be allosteric modulators of the CB1 receptor, and therefore useful for the treatment of diseases and conditions mediated by CB1.
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Paragraph 69; 72; 92
(2018/12/02)
Remarkably effective phosphanes simply with a PPh2 moiety: Application to Pd-Catalysed cross-coupling reactions for tetra-ortho-substituted biaryl syntheses
Chemical equation presented Expanding the horizons of ArPPh2: New applications of triarylphosphane ligands are presented. The Pd-L1 and Pd-L2 complexes offer exceptionally high activity in Suzuki-Miyaura cross-couplings of aryl chlorides. The extremely congested synthesis of tetraortho-substituted biaryl compounds is achieved for the first time by simply using triarylphosphane ligands.