- Nickel-Catalyzed Desymmetrizing Cross-Electrophile Coupling of Cyclic Meso-Anhydrides
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A Ni-catalyzed desymmetrizing cross-electrophile coupling of cyclic meso-anhydrides with aryl triflates has been successfully demonstrated. This is the only example using cyclic meso-anhydrides in cross-electrophile coupling reactions. A diverse array of valuable γ-keto acid building blocks can be generated under these conditions with excellent functional group tolerance and stereochemical fidelity.
- Lin, Tingzhi,Mi, Jianjun,Song, Lichao,Gan, Jiamin,Luo, Pan,Mao, Jianyou,Walsh, Patrick J.
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supporting information
p. 1191 - 1194
(2018/02/22)
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- Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones
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A series of 4-aryl-substituted cis-4a,5,8,8a-tetra- and cis-4a,5,6,7,8,8a-hexahydro-2H-phthalazin-1-ones with high inhibitory activity toward cAMP-specific phosphodiesterase (PDE4) was synthesized. To study structure-activity relationships various substituents were introduced to the 2-, 3-, and 4-positions of the 4-phenyl ring. Substitution at the 4-position of the phenyl ring was restricted to a methoxy group, probably due to unfavorable steric interactions of larger groups with the binding site. The introduction of many alkoxy substituents including distinct ring systems and functional groups was allowed to the 3-position. It was found that in general the cis-4a,5,8,8a-tetrahydro-2H-phthalazin-1-ones are more potent than their hexahydrophthalic counterparts, the best activity residing in (4-imidazol-1-yl-phenoxy)butoxy analogue 16o (pIC50 = 9.7).
- Van der Mey,Hatzelmann,Van Klink,Van der Laan,Sterk,Thibaut,Ulrich,Timmerman
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p. 2523 - 2535
(2007/10/03)
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- An efficient and general method for ester hydrolysis on the surface of silica gel catalyzed by indium triiodide under microwave irradiation
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Carboxylic esters are hydrolyzed to the corresponding carboxylic acids in high yields through a simple microwave assisted operation on the surface of silica gel moistened with few drops of water in presence of indium triiodide.
- Ranu,Dutta,Sarkar
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p. 4167 - 4171
(2007/10/03)
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- A New Redundant Rearrangement of Aromatic Ring Fused Cyclic α-Hydroxydithiane Derivatives. Synthesis of Aromatic Ring Fused Cyclic 1,2-Diketones with One-Carbon Ring Expansion
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A new reaction involving rearrangement of aromatic ring fused cyclic dithiane alcohol by N-chlorosuccinimide in CH2Cl2-H2O to the corresponding one-carbon ring expanded 1,2-diketone has been developed. A wide range of structurally varied dithiane alcohols have been found to undergo this rearrangement in high yields. The general criteria and reaction mechanism for this rearrangement have also been worked out.
- Ranu, Brindaban C.,Jana, Umasish
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p. 6380 - 6386
(2007/10/03)
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