Review:The importance of synthetic chemistry in the pharmaceutical industry
ScienceThe importance of synthetic chemistry in the pharmaceutical industryBY KEVIN R. CAMPOS, PAUL J. COLEMAN, JUAN C. ALVAREZ, SPENCER D. DREHER, ROBERT M. GARBACCIO, NICHOLAS K. TERRETT, RICHARD D. TILLYER, MATTHEW D. TRUPPO, EMMA R. PARMEEChemical synthesis plays a key role in pharmaceutical research and development. Campos et al. review some of the advantages that have come from recent innovations in synthetic methods. In particular, they highlight small-molecule catalysts stimulated by visible light, enzymes engineered for versatility beyond their intrinsic funct...
Source: Organometallic Current - January 18, 2019 Category: Chemistry Tags: Drug discovery Reviews Source Type: blogs
Concise total syntheses of ( –)-jorunnamycin A and (–)-jorumycin enabled by asymmetric catalysis
ScienceConcise total syntheses of ( –)-jorunnamycin A and (–)-jorumycin enabled by asymmetric catalysisBY ERIC R. WELIN, AURAPAT NGAMNITHIPORN, MAX KLATTE, GUILLAUME LAPOINTE, GERIT M. POTOTSCHNIG, MARTINA S. J. MCDERMOTT, DYLAN CONKLIN, CHRISTOPHER D. GILMORE, PAMELA M. TADROSS, CHRISTOPHER K. HALEY, KENJI NEGORO, EMIL GLIBSTRUP, CHRISTIAN U. GR ÜNANGER, KEVIN M. ALLAN, SCOTT C. VIRGIL, DENNIS J. SLAMON, BRIAN M. STOLTZSCIENCE18 JAN 2019 : 270-275 A route to two marine natural products distinct from the biosynthesis enables...
Source: Organometallic Current - January 18, 2019 Category: Chemistry Tags: Asymmetric Total synthesis Source Type: blogs
Divergent Synthesis of Natural Derivatives of (+) ‐Saxitoxin Including 11‐Saxitoxinethanoic Acid
AngewchemDivergent Synthesis of Natural Derivatives of (+) ‐Saxitoxin Including 11‐Saxitoxinethanoic Acid Dr. James R. Walker, Dr. Jeffrey E. Merit, Dr. Rhiannon Thomas ‐Tran, Doris T. Y. Tang, Prof. J. Du Bois[2,3]=4 toxins: A synthetic strategy that enables access to four naturally occurring guanidinium toxins, namely saxitoxin, decarbamoyl saxitoxin, C13 ‐acetoxy saxitoxin, and C11‐saxitoxinethanoic acid, is detailed. Highlights of this work include an unusual Mislow–Evans rearrangement and a late‐stage Stille ketene acetal cross‐coupling reaction. (Source: Organometallic Current)
Source: Organometallic Current - January 10, 2019 Category: Chemistry Tags: Total synthesis Source Type: blogs
Ynamide ‐Mediated Thiopeptide Synthesis
AngewchemYnamide ‐Mediated Thiopeptide SynthesisJinhua Yang, Changliu Wang, Silin Xu, Prof. Dr. Junfeng Zhao Effective to the backbone: In an ynamide ‐mediated two‐step procedure for thiopeptide bond formation, readily available monothiocarboxylic acids served as thioacyl donors. The appropriate balance between the activity and stability of α‐thioacyloxyenamide intermediates formed by the addition of the monothiocarboxylic acid to the ynamide enabled them to act as effective thioacylating reagents. (Source: Organometallic Current)
Source: Organometallic Current - January 10, 2019 Category: Chemistry Tags: Peptide Modification Source Type: blogs
Palladium ‐Catalyzed Intermolecular [4+1] Spiroannulation by C(sp3)−H Activation and Naphthol Dearomatization
AngewchemPalladium ‐Catalyzed Intermolecular [4+1] Spiroannulation by C(sp3)−H Activation and Naphthol DearomatizationBojun Tan, Lu Bai, Pin Ding, Jingjing Liu, Yaoyu Wang, Prof. Dr. Xinjun LuanTwo types of halides: A palladium ‐catalyzed [4+1] spiroannulation of two types of aryl halides has been developed for the rapid construction of a new class of spirocycles. This intermolecular domino process was realized through a sequence of C(sp3) −H cleavage, unsymmetrical biaryl coupling, and naphthol dearomatization. (Source: Organometallic Current)
Source: Organometallic Current - January 10, 2019 Category: Chemistry Tags: Dearomatization Pd Catalyzed sp3 C-H Activation Spirocycles Source Type: blogs
Carbonylation of Alkyl Radicals Derived from Organosilicates through Visible ‐Light Photoredox Catalysis
AngewchemCarbonylation of Alkyl Radicals Derived from Organosilicates through Visible ‐Light Photoredox CatalysisAlex Cartier, Etienne Levernier, Dr. Vincent Corc é, Prof. Takahide Fukuyama, Dr. Anne‐Lise Dhimane, Dr. Cyril Ollivier, Prof. Ilhyong Ryu, Prof. Louis Fensterbank Advocating a regime change: Primary, secondary, and tertiary alkyl radicals, formed by the photocatalyzed oxidation of organosilicates, underwent three ‐component reactions with carbon monoxide (CO) and radical acceptors to provide unsymmetrical ketones (see scheme). The concept of radical carbonylation under a photooxidative regime and me...
Source: Organometallic Current - January 10, 2019 Category: Chemistry Tags: Carbonylation Photoredox Catalysis Visible light Source Type: blogs
Oxidative Addition to Palladium(0) Made Easy through Photoexcited ‐State Metal Catalysis: Experiment and Computation
AngewchemOxidative Addition to Palladium(0) Made Easy through Photoexcited ‐State Metal Catalysis: Experiment and ComputationDr. Rajesh Kancherla, Dr. Krishnamoorthy Muralirajan, Dr. Bholanath Maity, Chen Zhu, Patricia E. Krach, Prof. Dr. Luigi Cavallo, Prof. Dr. Magnus Rueping Excited ‐state palladium catalyzed decarboxylative alkylation of α,β‐unsaturated acids is achieved by a barrierless approach under visible light irradiation at room temperature with good stereoselectivity. Detailed DFT calculations with experimental evidence suggests a neutral decarboxylative pathway. (Source: Organometallic Current)
Source: Organometallic Current - January 10, 2019 Category: Chemistry Tags: Pd Catalyzed Photocatalysis Source Type: blogs
