109492-91-3Relevant academic research and scientific papers
Cobalt-Catalyzed Desymmetric Isomerization of Exocyclic Olefins
Lan, Yu,Liu, Qiang,Liu, Shihan,Liu, Xufang,Rong, Xianle
supporting information, p. 20633 - 20639 (2021/12/17)
Chiral cyclic olefins, 1-methylcyclohexenes, are versatile building blocks for the synthesis of pharmaceuticals and natural products. Despite the prevalence of these structural motifs, the development of efficient synthetic methods remains an unmet challenge. Herein we report a novel desymmetric isomerization of exocyclic olefins using a series of newly designed chiral cobalt catalysts, which enables a straightforward construction of chiral 1-methylcyclohexenes with diversified functionalities. The synthetic utility of this methodology is highlighted by a concise and enantioselective synthesis of a natural product, β-bisabolene. The versatility of the reaction products is further demonstrated by multifarious derivatizations.
Discovery of novel S1P2 antagonists, part 3: Improving the oral bioavailability of a series of 1,3-bis(aryloxy)benzene derivatives
Kusumi, Kensuke,Shinozaki, Koji,Yamaura, Yoshiyuki,Hashimoto, Ai,Kurata, Haruto,Naganawa, Atsushi,Otsuki, Kazuhiro,Matsushita, Takeshi,Sekiguchi, Tetsuya,Kakuuchi, Akito,Yamamoto, Hiroshi,Seko, Takuya
, p. 1209 - 1213 (2016/02/23)
The structure of the S1P2 antagonist 1 has been modified with the aim of improving its oral bioavailability. The chemical modification of the alkyl chain and carboxylic acid moieties of 1 led to significant improvements in the oral exposure of compounds belonging to this series. The optimization of the ring size of the urea portion of these molecules also led to remarkable improvements in the oral exposure. Based on these changes, the pyrrolidine derivative 16 was identified as a suitable candidate compound and showed excellent pharmacokinetic profiles in rat and dog, while maintaining high levels of potency and selective antagonistic activity toward S1P2.
PHENYL DERIVATIVE
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Paragraph 0121, (2014/08/19)
The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.
Compounds that modulate PPAR activity and methods of preparation
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, (2008/06/13)
This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia and hypercholesteremia in a mammal. The present invention also discloses methods for making the disclosed compounds.
Studies on the Synthesis of Aphidicolin. Preparation of Aromatic Precursors for Spirocyclic Dienone Formation
Bell, Vivien L.,Giddings, Peter J.,Holmes, Andrew B.,Mock, Graham A.,Raphael, Ralph A.
, p. 1515 - 1522 (2007/10/02)
Novel syntheses of the alkanediones (12; R=Me, or CH2Ph) and the corresponding epoxides (13) are described.Attempts to cyclise these compounds to the spirocyclic dienone (4) were unsuccessful.Model studies on the phenolic keto cyano toluene-p-sulphonate (24) showed that the cyclopropane(25) was formed preferentially.A variety of related model compounds (29), (31), (32), and (37) were prepared and studied, but none could be cyclised to spirocyclic dienones.
