Drug Discovery and Synthesis Highlights
@TotalSyntheses
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Highlight Total Synthesis, Organometallic Chemistry, Heterocycles Synthesis, Biosynthesis, Medicinal Chemistry, Electrochemistry and Photochemistry.
United States
Joined December 2016
Concise Synthesis of (−)-GA18 Methyl Ester @MingjiDai @LifeAtPurdue @EmoryChem @EmoryUniversity @TotalSyntheses @TotalSynthesis #Synthesis #2plus2 #Transhydrindane #Gibberellins
pubs.acs.org
Gibberellins (GAs) are important plant hormones, but some of their family members are in extremely limited natural supply including GA18. Herein, we report a concise synthesis of (−)-GA18 methyl...
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Excited-State Copper-Catalyzed [4 + 1] Annulation Reaction Enables Modular Synthesis of α,β-Unsaturated-γ-Lactams @SUNY @TotalSyntheses #Cu #ExcitedState #Annulation #Modular #Lactams #Enamides
pubs.acs.org
Synthesis of α,β-unsaturated-γ-lactams continue to attract attention due to the importance of this structural motif in organic chemistry. Herein, we report the development of a visible-light-induced...
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Check out our recent syntheses of bufospirostenin A and ophiopogonol A in only seven steps from inexpensive starting materials just out in @J_A_C_S . Great collaboration with Hong group from Zhejiang University for computational studies:
pubs.acs.org
Controlling the conformation of medium-sized rings is challenging because of their flexibility and ring strain effects. Herein, we report non-Curtin–Hammett conditions for the precise control of the...
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JACS online： #Symmetry-Driven Total #Synthesis of #Myrioneurinol
@J_A_C_S @isciverse @CHNSci @UTSWNews
@TotalSynthesis @TotalSyntheses #Chemistry #Science #Catalysis #technology
https://t.co/s3jwDqQL9d
pubs.acs.org
We report a total synthesis of the Myrioneuron alkaloid myrioneurinol enabled by the recognition of hidden symmetry within its polycyclic structure. Our approach traces myrioneurinol’s complex...
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Synthesis of Pleuromutilin @UCIChemistry @UCIrvine @TotalSynthesis @TotalSyntheses #Pleuromutilin #Total #Synthesis
pubs.acs.org
Synthesis of a potent inhibitor of bacterial protein synthesis, pleuromutilin, is described. Assembly of the critical cyclooctane fragment relies on an oxidative ring-expansion, and complete stereo...
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JACS online: Asymmetric Total #Syntheses of #Cephalotane-Type #Diterpenoids #Cephanolides A–D @J_A_C_S @isciverse @CHNSci @PKU1898
@TJU1895 @TotalSynthesis @TotalSyntheses
#Chemistry #Science #Catalysis #technology
https://t.co/9fvm2Hq3dj
pubs.acs.org
Cephanolides A–D are cephalotane-type diterpenoids featuring a novel 6/6/6/5 tetracyclic core embedded with a bridged δ-lactone. The asymmetric and divergent total syntheses of cephanolides A–D have...
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Introducing the Catalytic Amination of Silanes via Nitrene Insertion @PedroJPerez65 @CIQSO_UHU @MaserasGroup @ICIQchem @_BIST #Catalytic #Amination #Silanes #Nitrene @TotalSyntheses
pubs.acs.org
The direct functionalization of Si–H bonds by the nitrene insertion methodology is described. A copper(I) complex bearing a trispyrazolylborate ligand catalyzes the transfer of a nitrene group from...
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Organocatalytic Asymmetric Synthesis of Si-Stereogenic Silyl Ethers @ListLaboratory @ben_list @ICReDDconnect #Organocatalysis @TotalSyntheses #Silyl #Stereogenic #Silylethers
pubs.acs.org
Functionalized enantiopure organosilanes are important building blocks with applications in various fields of chemistry; nevertheless, asymmetric synthetic methods for their preparation are rare....
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Happy to report a practical bottom-up synthesis of aminoglycoside antibiotic ribostamycin!!! Collaborative efforts with @pengliu_group. Novel asymmetric catalytic desymmetrization of ⌬ (♡!), mechanism, com. studies, and more! https://t.co/gBqgyxefBN
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Ever wondered about directly turning the indole skeleton of a bioactive compound into a quinazoline or quinoxaline by "just" inserting a N atom? Check this MS @ChemRxiv from Julia, @origree1, @HappyFranchino, @PDFinkelstein. https://t.co/SiX0lByQEN
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Cu-Mediated Ullmann-Type Cross-Coupling and Industrial Applications in Route Design, Process Development, and Scale-up of Pharmaceutical and Agrochemical Processes
pubs.acs.org
Cu-mediated Ullmann-type cross-coupling has experienced significant advances over the last century since the seminal publication by Ullmann in 1901. These advances have significantly expanded the...
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Two-Stage Syntheses of Clionastatins A and B @CHNSci @TotalSynthesis @TotalSyntheses #Synthesis #Clionastatins #Chlorination
pubs.acs.org
A concise and divergent synthesis of the polychlorinated marine steroids clionastatin A and B from inexpensive testosterone has been achieved through a unique two-stage chlorination–oxidation...
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Synthesis of Dimeric Securinega Alkaloid Flueggeacosine B: From Pd-Catalyzed Cross-Coupling to Cu-Catalyzed Cross-Dehydrogenative Coupling @KAIST #TotalSynthesis @TotalSynthesis @TotalSyntheses #Alkaloid #Pd #CrossCoupling #Cu #Dehydrogenative
pubs.acs.org
We completed the synthesis of dimeric high-oxidation-state securinega alkaloid flueggeacosine B via two synthetic routes from allosecurinine. The first-generation synthesis (seven overall steps)...
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Versatile Palladium-Catalyzed Approach to Acyl Fluorides and Carbonylations by Combining Visible Light- and Ligand-Driven Operations @mcgillu @TotalSyntheses #Palladium #Fluorides #Light
pubs.acs.org
We describe the development of a general palladium-catalyzed carbonylative method to synthesize acyl fluorides from aryl, heteroaryl, alkyl, and functionalized organic halides. Mechanistic analysis...
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Design of an Organocatalytic Asymmetric (4 + 3) Cycloaddition of 2-Indolylalcohols with Dienolsilanes @ben_list @ListLaboratory @MPI @TotalSyntheses #Organocatalysis #Asymmetric #indole #Cycloaddition #Dienolsilanes
pubs.acs.org
Here we present the design of a highly enantioselective, catalytic (4 + 3) cycloaddition of gem-dialkyl 2-indolyl alcohols and dienolsilanes, enabled by strong and confined IDPi Lewis acids. The...
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A Unified Approach to Decarboxylative Halogenation of (Hetero)aryl Carboxylic Acids @dmac68 @MacMillan_Lab @PrincetonChem @TotalSyntheses @pfizer_news @NCState @NCStateChem @CastellanoGroup @FNCastellano #decarboxylative #Halogenation #Hetaranes
pubs.acs.org
Aryl halides are a fundamental motif in synthetic chemistry, playing a critical role in metal-mediated cross-coupling reactions and serving as important scaffolds in drug discovery. Although thermal...
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Breaking news courtesy of Kevin Campos and Dave MacMillan, from Sally Evans. Dave passed away last night. This pic that they included is how Dave looked during my days in his group. Circa 1985-87
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