866270-03-3Relevant academic research and scientific papers
NITROGEN-CONTAINING 6-MEMBERED CYCLIC COMPOUND
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Paragraph 0253-0256, (2020/12/01)
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.
Ambient Decarboxylative Arylation of Malonate Half-Esters via Oxidative Catalysis
Moon, Patrick J.,Yin, Shengkang,Lundgren, Rylan J.
supporting information, p. 13826 - 13829 (2016/11/06)
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.
Synthesis and evaluation of γ-lactam analogs of PGE2 as EP4 and EP2/EP4 agonists
Kambe, Tohru,Maruyama, Toru,Nakai, Yoshihiko,Oida, Hiroji,Maruyama, Takayuki,Abe, Nobutaka,Nishiura, Akio,Nakai, Hisao,Toda, Masaaki
experimental part, p. 3502 - 3522 (2012/07/30)
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
Discovery of novel prostaglandin analogs as potent and selective EP2/EP4 dual agonists
Kambe, Tohru,Maruyama, Toru,Nakai, Yoshihiko,Yoshida, Hideyuki,Oida, Hiroji,Maruyama, Takayuki,Abe, Nobutaka,Nishiura, Akio,Nakai, Hisao,Toda, Masaaki
experimental part, p. 2235 - 2251 (2012/05/20)
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
Copper(II)-catalyzed meta-selective direct arylation of α-aryl carbonyl compounds
Duong, Hung A.,Gilligan, Ruth E.,Cooke, Michael L.,Phipps, Robert J.,Gaunt, Matthew J.
supporting information; experimental part, p. 463 - 466 (2011/03/16)
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.
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists
Zhao, Zhong,Araldi, Gian Luca,Xiao, Yufang,Reddy, Adulla P.,Liao, Yihua,Karra, Srinivasa,Brugger, Nadia,Fischer, David,Palmer, Elizabeth
, p. 6572 - 6575 (2008/09/16)
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.
The diazo route to diazonamide A. Studies on the indole bis-oxazole fragment
Davies, James R.,Kane, Peter D.,Moody, Christopher J.
, p. 7305 - 7316 (2007/10/03)
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
