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Akademický článek

Asymmetric Synthesis of the Carbon-14-Labeled Selective Glucocorticoid Receptor Modulator using Cinchona Alkaloid Catalyzed Addition of 6-Bromoindole to Ethyl Trifluoropyruvate

Autor: Norie Tsuboya, Masanori Tobe, Tomoko Nakajima, Kazumi Niidome, Masato Sakamoto, Kengo Tojo, Daisuke Urabe, Takaaki Sumiyoshi

Publikováno v: Molecules, Vol 17, Iss 6, Pp 6507-6518 (2012)

We describe in this study the asymmetric synthesis of radioisotope (RI)-labeled selective glucocorticoid receptor modulator. This synthesis is based on optimization of the cinchona alkaloid catalyzed addition of 6-bromoindole to ethyl trifluoropyruva

Externí odkaz: https://doaj.org/article/79f7caab5cf24be3b16326e0a5063007

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Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M1 and M4 muscarinic acetylcholine receptors agonists

Autor: Atsushi Kitamura, Atsushi Suwa, Mutsuko Sakai, Takeshi Enomoto, Harumi Matsuda, Yasuko Konishi, Kentaro Takai, Kengo Tojo, Yoshiharu Uruno, Tomokazu Nakako, Takaaki Sumiyoshi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:5357-5361

We designed and synthesized a series of dihydroquinazolinone derivatives as selective M1 and M4 muscarinic acetylcholine receptors agonists. Introduction of the N-carbethoxy piperidine unit into a HTS hit compound followed by optimization of the amin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1df5c0ef018e6536fa0ef8cfeb47011
https://doi.org/10.1016/j.bmcl.2015.09.032

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Discovery of Novel N-Substituted Oxindoles as Selective M1 and M4 Muscarinic Acetylcholine Receptors Partial Agonists

Autor: Yoko Takahashi, Yasuaki Uematsu, Mutsuko Sakai, Atsushi Kitamura, Harumi Matsuda, Kentaro Takai, Akihiko Kiyoshi, Takaaki Sumiyoshi, Yasuko Konishi, Tomokazu Nakako, Kengo Tojo, Atsushi Suwa, Yoshiharu Uruno, Takeshi Enomoto

Publikováno v: ACS Medicinal Chemistry Letters. 4:244-248

Activation of the M1 and M4 muscarinic acetylcholine receptors is thought to play an important role in improving the symptoms of schizophrenia. However, discovery of selective agonists for these receptors has been a challenge, considering the high se

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0b9ee88415a41c72fc7cd07dd6da120
https://doi.org/10.1021/ml300372f

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Asymmetric synthesis of the 6-cyanoindole derivatives as non-steroidal glucocorticoid receptor modulators using (+)- and (−)-tert-butyl 6-cyano-3-[3-ethoxy-1,1,1-trifluoro-2-hydroxy-3-oxopropan-2-yl]-1H-indole-1-carboxylate

Autor: Daisuke Urabe, Masanori Tobe, Kengo Tojo, Takaaki Sumiyoshi

Publikováno v: Tetrahedron: Asymmetry. 22:153-160

We have successfully synthesized enantiomerically pure (+)- and (−)- tert -butyl 6-cyano-3-[3-ethoxy-1,1,1-trifluoro-2-hydroxy-3-oxopropan-2-yl]-1 H -indole-1-carboxylate (+)- 1 and (−)- 1 , which are key intermediates of non-steroidal glucocorti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f37e42d197e4d7f19bc867f65ac23556
https://doi.org/10.1016/j.tetasy.2011.01.020

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Stereoselective Total Synthesis of (+)-Scyphostatin via a π-Facially Selective Diels−Alder Reaction

Autor: Ryukichi Takagi, Wataru Miyanaga, Kengo Tojo, Shinjiro Tsuyumine, Katsuo Ohkata

Publikováno v: The Journal of Organic Chemistry. 72:4117-4125

A stereoselective total synthesis of scyphostatin is described. The hydrophilic moiety was stereoselectively synthesized via (i) a highly pi-facially selective Diels-Alder reaction of a spirolactone generated from L-tyrosine and (ii) a hydroxy group

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b11969c4ae8bc12619039c2eade00402
https://doi.org/10.1021/jo070337k

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Asymmetric Synthesis of the Carbon-14-Labeled Selective Glucocorticoid Receptor Modulator using Cinchona Alkaloid Catalyzed Addition of 6-Bromoindole to Ethyl Trifluoropyruvate

Autor: Takaaki Sumiyoshi, Kengo Tojo, Masato Sakamoto, Daisuke Urabe, Masanori Tobe, Norie Tsuboya, Kazumi Niidome, Tomoko Nakajima

Publikováno v: Molecules; Volume 17; Issue 6; Pages: 6507-6518
Molecules
Molecules, Vol 17, Iss 6, Pp 6507-6518 (2012)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2b7c9404934ed143961089031c56400

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Synthesis of a 4,5-epoxy-2-cyclohexen-1-one derivative via epoxide ring opening, 1,3-carbonyl transposition and epoxide ring regeneration: a synthetic study on a scyphostatin analogue

Autor: Ryukichi Takagi, Katsuo Ohkata, Kengo Tojo, Masato Iwata

Publikováno v: Organicbiomolecular chemistry. 3(10)

A 6-alkyl-4,5-epoxy-6-hydroxy-2-cyclohexen-1-one derivative, a model compound for the hydrophilic moiety of scyphostatin, was stereoselectively synthesized from the Diels–Alder adduct. The key steps were the reductive cleavage of the 4,5-epoxide ri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e64ba6eaad71bd7f13f6402d96cdcb3
https://pubmed.ncbi.nlm.nih.gov/15889188

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