While continuous chemical processes have attracted both academic and industrial interest, virtually all active pharmaceutical ingredients (APIs) are still produced by using multiple distinct batch processes. To date, methods for the divergent multistep continuous production of customizable small molecules are not available. A chemical assembly system was developed, in which flow-reaction modules are linked together in an interchangeable fashion to give access to a wide breadth of chemical space. Control at three different levels--choice of starting material, reagent, or order of reaction modules--enables the synthesis of five APIs that represent three different structural classes (γ-amino acids, γ-lactams, β-amino acids), including the blockbuster drugs Lyrica and Gabapentin, in good overall yields (49-75%).
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http://dx.doi.org/10.1002/anie.201409765 | DOI Listing |
Chem Sci
January 2025
College of Chemistry and Chemical Engineering, Key (Guangdong-Hong Kong Joint) Laboratory for Preparation and Application of Ordered Structural Materials of Guangdong Province, Shantou University Shantou 515063 P. R. China
In the past few years, the direct activation of organohalides by ligated boryl radicals has emerged as a potential synthetic tool for cross-coupling reactions. In most existing methods, ligated boryl radicals are accessed from NHC-boranes or amine-boranes. In this work, we report a new photocatalytic platform by modular assembly of readily available amines and diboron esters to access a library of ligated boryl radicals for reaction screening, thus enabling the cross-coupling of organohalides and alkenes including both activated and unactivated ones for C(sp)-C(sp) bond formation by using the assembly of DABCO A1 and BNepB1.
View Article and Find Full Text PDFMater Today Bio
February 2025
Biobank of Tumors from Plateau of Gansu Province, Lanzhou University Second Hospital, Lanzhou, 730030, China.
Pancreatic cancer (PC) is a highly lethal malignancy with rapid progression and poor prognosis. Despite the widespread use of gemcitabine (Gem)-based chemotherapy as the first-line treatment for PC, its efficacy is often compromised by significant drug resistance. 1,2,3,4,6-Pentagaloyl glucose (PGG), a natural polyphenol, has demonstrated potential in sensitizing PC cells to Gem.
View Article and Find Full Text PDFSmall
January 2025
Department of Chemistry, National Taiwan University, Taipei, 10617, Taiwan.
Addressing the challenges of the efficiency and stability of red perovskite nanocrystals is imperative for the successful deployment of these materials in displays and lighting applications. the structural dynamic changes of red perovskite quantum dots (PQDs) are explored using a flow chemistry system to solve the above hurdles. First, the ultrabright red-emitting PQDs of CsPb(Br,I) are achieved by adjusting ligand distribution (oleic acid and oleyamine) in combination with different flow rates and equivalence ratios.
View Article and Find Full Text PDFSmall Methods
January 2025
College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang, 050018, P. R. China.
Asymmetric carbon-based materials (ACBMs) have received significant attention in scientific research due to their unique structures and properties. Through the introduction of heterogeneous atoms and the construction of asymmetric ordered/disordered structures, ACBMs are optimized in terms of electrical conductivity, pore structure, and chemical composition and exhibit multiple properties such as hydrophilicity, hydrophobicity, optical characteristics, and magnetic behavior. Here, the recent research progress of ACBMs is reviewed, focusing on the potential of these materials for electrochemical, catalysis, and biomedical applications and their unique advantages over conventional symmetric carbon-based materials.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
Fudan University, Department of Macromolecular Science, 2205 Songhu Rd, 200438, Shanghai, CHINA.
Nitrogen heterocyclic carbenes (NHCs) are emerging as effective substitutes for conventional thiol ligands in surface functionalization of nanoparticles (NPs), offering exceptional stability to NPs under harsh conditions. However, the highly reactive feature of NHCs limits their use in introducing chemically active groups onto the NP surface. Herein, we develop a general yet robust strategy for the efficient surface functionalization of NPs with copolymer ligands bearing various functional groups.
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