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News


Feb. 2, 2018

Dr. Naoya Kumagai won MBLA 2017.

Dec. 14, 2017

Dr. Takumi Watanabe won The Pharmaceutical Society of Japan Award for Divisional Scientific Promotion '18.

Dec. 11, 2017

Our dioxaazatriborinane (B3NO2) was nominated for "Molecules of the year (C&EN)".

Feb. 1, 2017

Our recent research results on the novel catalyst for amidation were described in C&EN (Jan. 30th, 2017) , Mainichi Shimbun (Jan. 31st, 2017), and Nikkei Sangyo Shimbun (Jan. 31st, 2017).

Jun. 1, 2015

Our lab moved to the new building.


TOP


Recent publication

"A C4N4 Diaminopyrimidine Fluorophore"
Noda, H.; Asada, Y.; Maruyama, T.; Takizawa, N.; Noda, N. N.; Shibasaki, M.; Kumagai, N.
Chem. Eur. J. 2019, Early View.


"Catalytic Asymmetric Synthesis of syn Aldols with Methyl Ketone Functionality and anti Aldols with a Thioamide Group"
Ota, Y.; Li, Z.; Kumagai, N.; Shibasaki, M.
Synlett 2019, eFirst.


"Direct Catalytic Asymmetric Aldol Reaction of α‐Alkoxyamides to α‐Fluorinated Ketones"
Pluta, R.; Kumagai, N.; Shibasaki, M.
Angew. Chem. Int. Ed. 2019, 58, 2459.



"Neighboring Protonation Unveils Lewis Acidity in the B3NO2 Heterocycle"
Noda, H.; Asada, Y.; Shibasaki, M.; Kumagai, N.
J. Am. Chem. Soc. 2019, 141, 1546.


"Direct Catalytic Asymmetric Mannich-Type Reaction of an α-CF3 Amide to Isatin Imines"
Yu, J.-S.; Noda, H.; Kumagai, N.; Shibasaki, M.
Synlett 2019, 30, 488.



"Achiral Trisubstituted Thioureas as Secondary Ligands to Cu(I) Catalysts: Direct Catalytic Asymmetric Addition of α‐Fluoronitriles to Imines"
Balaji, P. V.; Brewitz, L.; Kumagai, N.; Shibasaki, M.
Angew. Chem. Int. Ed. 2018, 58, 2644. Selected as inside back cover.


"A fluorogenic C4N4 probe for azide-based labelling"
Noda, H.; Asada, Y.; Shibasaki, M.; Kumagai, N.
Org. Biomol. Chem. 2019, 17, 1813.


"7-Azaindoline Auxiliary: A Versatile Attachment Facilitating Enantioselective C-C Bond-Forming Catalysis"
Kumagai, N.; Shibasaki, M.
Synthesis 2019, 51, 185.


"Exploiting β‐Amino Acid Enolates in Direct Catalytic Diastereo‐ and Enantioselective C‐C Bond Forming Reactions"
Yu, J.-S.; Noda, H.; Shibasaki, M.
Chem. Eur. J. 2018, 24, 15796.


"anti-Selective Catalytic Asymmetric Nitroaldol Reaction of α-Keto Esters; Intriguing Solvent Effect, Flow Reaction, and Synthesis of APIs"
Karasawa, T.; Oriez, R.; Kumagai, N.; Shibasaki, M.
J. Am. Chem. Soc. 2018, 140, 12290.


"Structure-activity relationship study of leucinostatin A, a modulator of tumor−stroma interaction"
Abe, H.; Kawada, M.; Sakashita, C.; Watanabe, T.; Shibasaki, M.
Tetrahedron 2018, 74, 5129.


"Direct Catalytic Asymmetric 1,6-Conjugate Addition of Amides to p-Quinone Methides"
Sun, Z.; Sun, B.; Kumagai, N.; Shibasaki, M.
Org. Lett. 2018, 20, 3070.


"Direct Catalytic Asymmetric Aldol Reaction of α-Vinyl Acetamide"
Takeuchi, T.; Kumagai, N.; Shibasaki, M.
J. Org. Chem. 2018, 83, 5851.


"Direct enolization chemistry of 7-azaindoline amides: A case study of bis(tetrahydrophosphole)-type ligands"
Li, Z.; Noda, H.; Kumagai, N.; Shibasaki, M.
Tetrahedron 2018, 74, 3301.


"Catalytic Asymmetric Synthesis of α-Trifluoromethylated Carbinols: A Case Study of Tertiary Propargylic Alcohols"
Noda, H.; Kumagai, N.; Shibasaki, M.
Asian J. Org. Chem. 2018, 7, 599.


"Conquering amide planarity: structural distortion and its hidden reactivity"
Adachi, S.; Kumagai, N.; Shibasaki, M.
Tetrahedron Lett. 2018, 59, 1147.


"Catalytic Oligopeptide Synthesis"
Liu, Z.; Noda, H.; Shibasaki, M.; Kumagai, N.
Org. Lett. 2018, 20, 612.


"Direct Catalytic Asymmetric Mannich-Type Reaction en Route to α-Hydroxy-β-amino Acid Derivatives"
Sun, B.; Pluta, R.; Kumagai, N.; Shibasaki, M.
Org. Lett. 2018, 20, 526.


"Direct Catalytic Asymmetric Aldol Reaction of Thioamide with an α-Vinyl Appendage"
Cui, J.; Ohtsuki, A.; Watanabe, T.; Kumagai, N.; Shibasaki, M.
Chem. Eur. J. 2018, 24, 2598.


"Heterogeneous Heterobimetallic Catalysis Enabling Expeditious Access to CF3-Containing vic-Amino Alcohols"
Karasawa, T.; Kumagai, N.; Shibasaki, M.
Org. Lett. 2018, 20, 308.


"Quaternary β2,2-Amino Acids: Catalytic Asymmetric Synthesis and Incorporation into Peptides by Fmoc-Based Solid-Phase Peptide Synthesis"
Yu, J.-S.; Noda, H.; Shibasaki, M.
Angew. Chem. Int. Ed. 2018, 57, 818.



"Structural and Computational Investigation of Intramolecular N...H Interactions in α- and β-Fluorinated 7-Azaindoline Amides"
Brewitz, L.; Noda, H.; Kumagai, N.; Shibasaki, M.
Eur. J. Org. Chem. 2018, 714. Selected as a front cover.


"Bis(2-pyridyl)amides as Readily Cleavable Amides Under Catalytic, Neutral, and Room-Temperature Conditions"
Adachi, S.; Kumagai, N.; Shibasaki, M.
Synlett 2018, 29, 301.


"Catalytic enantioselective addition of diethyl phosphite to N-thiophosphinoyl ketimines: preparation of (R)-diethyl(1-amino-1-phenylethyl)phosphonate"
Lin, S.; Otsuka, Y.; Yin, L.; Kumagai, N.; Shibasaki, M.
Org. Synth. 2017, 94, 313.



"α,β-Unsaturated Amides as Dipolarophiles: Catalytic Asymmetric exo-Selective 1,3-Dipolar Cycloaddition with Nitrones"
Zhang, M.; Kumagai, N.; Shibasaki, M.
Chem. Eur. J. 2017, 23, 12450. Selected as Cover Picture and Cover Profile.


Synthetic studies of viridiofungins, broad-spectrum antifungal agents and serine palmitoyl transferase inhibitors
Kumagai, N.; Shibasaki, M.
J. Antibiot. 2018, 71, 53.


Catalytic Asymmetric Total Synthesis and Stereochemical Revision of Leucinostatin A: A Modulator of Tumor-Stroma Interaction
Abe, H.; Ouchi, H.; Sakashita, C.; Kawada, M.; Watanabe, T.; Shibasaki, M.
Chem. Eur. J. 2017, 23, 11792.


Direct Catalytic Asymmetric Aldol Addition of an α-CF3 Amide to Arylglyoxal Hydrates
Matsuzawa, A.; Noda, H.; Kumagai, N.; Shibasaki, M.
J. Org. Chem. 2017, 82, 8304.


Photocatalytic α-Acylation of Ethers
Sun, Z.; Kumagai, N.; Shibasaki, M.
Org. Lett. 2017, 19, 3727.



"Direct N-acylation of sulfoximines with carboxylic acids catalyzed by the B3NO2 heterocycle"
Noda, H.; Asada, Y.; Shibasaki, M.; Kumagai, N.
Chem. Commun. 2017, 53, 7447. Selected as a front cover.


"α-Halo Amides as Competent Latent Enolates: Direct Catalytic Asymmetric Mannich-Type Reaction"
Sun, B.; Balaji, P. V.; Kumagai, N.; Shibasaki, M.
J. Am. Chem. Soc. 2017, 139, 8295.


"Leptolyngbyolides, Cytotoxic Macrolides from the Marine Cyanobacterium Leptolyngbya sp.: Isolation, Biological Activity, and Catalytic Asymmetric Total Synthesis"
Cui, J.; Morita, M.; Ohno, O.; Kimura, T.; Teruya, T.; Watanabe, T.; Suenaga, K.; Shibasaki, M.
Chem. Eur. J. 2017, 23, 8500.


"Cu/Pd Synergistic Dual Catalysis: Asymmetric α-Allylation of an α-CF3 Amide"
Saito, A.; Kumagai, N.; Shibasaki, M.
Angew. Chem. Int. Ed. 2017, 56, 5551. Highlighted in Synfacts 2017, 13, 715.


"Catalytic asymmetric synthesis of CF3-substituted tertiary propargylic alcohols via direct aldol reaction of α-N3 amide"
Noda, H.; Amemiya, F.; Weidner, K.; Kumagai, N.; Shibasaki, M.
Chem. Sci. 2017, 8, 3260.


"Reversible Stereoselective Folding/Unfolding Fueled by the Interplay of Photoisomerism and Hydrogen Bonding"
Opie, C. R.; Kumagai, N.; Shibasaki, M.
Angew. Chem. Int. Ed. 2017, 56, 3349.


"Unique Physicochemical and Catalytic Properties Dictated by the B3NO2 Ring System"
Noda, H.; Furutachi, M.; Asada, Y.; Shibasaki, M.; Kumagai, N.
Nature Chem. 2017, 9, 571. Highlighted in C&EN (January 30, 2017); Mainichi Shimbun (Jan. 31st, 2017); Nikkei Sangyo Shimbun (Jan. 31st, 2017); Synform 2017, 10, A165.


"Asymmetric flow catalysis: Mix-and-go solid-phase Nd/Na catalyst for expeditious enantioselective access to a key intermediate of AZD7594"
Nonoyama, A.; Kumagai, N.; Shibasaki, M.
Tetrahedron 2017, 73, 1517. Highlighted in Synfacts 2017, 13, 462; Synfacts 2017, 13, 559.


"Direct Catalytic Asymmetric Aldol Reaction of α-Alkylamides"
Liu, Z.; Takeuchi, T.; Pluta, R.; Arteaga, F. A.; Kumagai, N.; Shibasaki, M.
Org. Lett. 2017, 19, 710.


"Catalytic Asymmetric Synthesis of 2,3,3,3-Tetrafluoro-2-Methyl-1-Arylpropan-1-Amines as Useful Building Blocks for SAR-Studies"
Brewitz, L.; Kumagai, N.; Shibasaki, M.
J. Fluor. Chem. 2017, 194, 1.



"Pyramidalization/Twisting of the Amide Functional Group via Remote Steric Congestion Triggered by Metal Coordination"
Adachi, S.; Kumagai, N.; Shibasaki, M.
Chem. Sci. 2017, 8, 85. Selected as inside front cover


"Strategic Immobilization of Molecular Catalysts onto Carbon Nanotubes via Noncovalent Interaction for Catalytic Organic Transformations"
Kumagai, N.; Shibasaki, M.
Isr. J. Chem. 2017, 57, 270.


"Catalytic Asymmetric Synthesis of the C1-C15 Segment of Spirastrellolide A"
Sahara, Y.; Cui, J.; Furutachi, M.; Chen, J.; Watanabe, T.; Shibasaki, M.
Synthesis 2017, 49, 69.