- NITROGEN-CONTAINING 6-MEMBERED CYCLIC COMPOUND
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A novel compound represented by the following general formula (1), or a salt thereof, which has a superior EP4 receptor agonist activity, and a medicament containing the compound or a salt thereof as an active ingredient, which can be used for promotion of osteogenesis, therapeutic treatment and/or promotion of healing of fracture and the like.
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Paragraph 0253-0256
(2020/12/01)
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- Ambient Decarboxylative Arylation of Malonate Half-Esters via Oxidative Catalysis
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We report decarboxylative carbonyl α-arylation by coupling of arylboron nucleophiles with malonic acid derivatives. This process is enabled by the merger of aerobic oxidative Cu catalysis with decarboxylative enolate interception reminiscent of malonyl-CoA reactivity in polyketide biosynthesis. This method enables the synthesis of monoaryl acetate derivatives containing electrophilic functional groups that are incompatible with existing α-arylation reactivity paradigms. The utility of the reaction is demonstrated in drug intermediate synthesis and late-stage functionalization.
- Moon, Patrick J.,Yin, Shengkang,Lundgren, Rylan J.
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supporting information
p. 13826 - 13829
(2016/11/06)
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- Synthesis and evaluation of γ-lactam analogs of PGE2 as EP4 and EP2/EP4 agonists
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To identify topically effective EP4 agonists and EP2/EP4 dual agonists with excellent subtype selectivity, further optimization of the 16-phenyl ω-chain moiety of the γ-lactam 5-thia prostaglandin E analog and the 2-mercaptothiazole-4-carboxylic acid anal
- Kambe, Tohru,Maruyama, Toru,Nakai, Yoshihiko,Oida, Hiroji,Maruyama, Takayuki,Abe, Nobutaka,Nishiura, Akio,Nakai, Hisao,Toda, Masaaki
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experimental part
p. 3502 - 3522
(2012/07/30)
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- Discovery of novel prostaglandin analogs as potent and selective EP2/EP4 dual agonists
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To identify potent EP2/EP4 dual agonists with excellent subtype selectivity, a series of γ-lactam prostaglandin E analogs bearing a 16-phenyl ω-chain were synthesized and evaluated. Structural hybridization of 1 and 2, followed by more detailed chemical m
- Kambe, Tohru,Maruyama, Toru,Nakai, Yoshihiko,Yoshida, Hideyuki,Oida, Hiroji,Maruyama, Takayuki,Abe, Nobutaka,Nishiura, Akio,Nakai, Hisao,Toda, Masaaki
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experimental part
p. 2235 - 2251
(2012/05/20)
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- Copper(II)-catalyzed meta-selective direct arylation of α-aryl carbonyl compounds
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Strong competition: A method for the meta-selective arylation of the highly versatile α-aryl carbonyl motif using diaryliodonium salts is described. In this CuII-catalyzed process the remote carbonyl group is capable of overpowering even strongly para-directing functionalities to form the elusive meta-products (see scheme). Remarkably, the arylation process can also operate under metal-free conditions.
- Duong, Hung A.,Gilligan, Ruth E.,Cooke, Michael L.,Phipps, Robert J.,Gaunt, Matthew J.
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supporting information; experimental part
p. 463 - 466
(2011/03/16)
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- Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists
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Replacement of the hydroxy cyclopentanone ring in PGE2 with chemically more stable heterocyclic rings and substitution of the unsaturated α-alkenyl chain with a metabolically more stable phenethyl chain led to the development of potent and selective analogs of PGE2. Compound 10f showed the highest potency and selectivity for EP4 the receptor.
- Zhao, Zhong,Araldi, Gian Luca,Xiao, Yufang,Reddy, Adulla P.,Liao, Yihua,Karra, Srinivasa,Brugger, Nadia,Fischer, David,Palmer, Elizabeth
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p. 6572 - 6575
(2008/09/16)
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- The diazo route to diazonamide A. Studies on the indole bis-oxazole fragment
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Various approaches to the indole bis-oxazole fragment of the marine secondary metabolite diazonamide A are described, all of which feature dirhodium(II)-catalyzed reactions of diazocarbonyl compounds in key steps. Thus, 3-bromophenylacetaldehyde is conver
- Davies, James R.,Kane, Peter D.,Moody, Christopher J.
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p. 7305 - 7316
(2007/10/03)
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