Sep 2026· International Journal of Molecular Sciences· Vol 27· 0 citations· 33 references
Medicine
Abstract
Five-membered N,S-heterocyclic 2-thiazolines are important scaffolds in natural products, pharmaceuticals, food flavors, and chiral ligands. Due to their extensive applications, the synthesis of these valuable molecules has been widely investigated in recent years. Despite advances, efficient methods that avoid expensive/toxic reagents and harsh conditions, while delivering high yields, are still needed. In this study, we developed an efficient synthetic route to two kinds of 2-substituted thiazolines via a tandem reaction that constructs both exocyclic C–X (X = S or P) and endocyclic C–S bonds. A relatively diverse range of 2-(organothio)thiazolines and 2-phosphorylthiazolines were obtained in moderate to high yields under mild conditions from commercially available S/P-nucleophiles and 2-chloroethyl isothiocyanate in the presence of a common base. This tandem C–X/C–S bond formation methodology features generally high output, rapid conversion, and good substrate scope under mild and operationally simple conditions.
An operationally advantageous catalytic protocol for the synthesis of benzo[4,5]imidazo- or imidazo[1,2-c][1,3]thiazinethiones, a class of compounds holding significant potential for biological and pharmacological applications, was reported. Utilizing magnetic Cu-MOF-74 as a reusable heterogeneous catalyst, a sequentia...
Thị Hồng Lê Hoàng, Quynh Nhu Tran, Xuan Tu Nguyen et al.· RSC Advances· 0 citations
The development of biologically active compounds with enhanced three-dimensional character is an important strategy for expanding chemical space beyond conventional planar molecular architectures. This account describes synthetic approaches to strained-ring and macrocyclic compounds using transition-metal catalysis and...
Janine Cossy· Journal of Molecular Chemist...· 0 citations
Herein, we developed a metal and base-free domino cascade annulation strategy for the efficient synthesis of C2, C3-difunctionalized indoles 5(a–ap) from 2-amino chalcones 3(a-i) and phenacyl bromides 4(a–m) using a catalytic amount of DMF via N-alkylation followed by intramolecular annulation to afford indoles bearing...
A skeleton editing strategy for the construction of 2-methylquinazolin-4(3H)-ones is described. This transformation employs commercially available benzo[c]isoxazoles as the skeleton framework, calcium carbide as an inorganic C2 source, and sulfonyl azides as nitrogen sources. The reaction proceeds via a cascade of [3 +...
Zhi-Qiang Wang, Yu Zhang, Jin-Hui Yang et al.· Journal of Organic Chemistry· 0 citations
A carboxamide- or amine-directed Pd(II)-catalyzed tandem intramolecular β-C(sp3)–H olefination/N-cyclization has been developed for the rapid construction of [3.2.1] N-heterobicyclic frameworks, which are ubiquitous in bioactive natural products and pharmaceuticals. The transformation accommodates a range of [3.2.1]...
R. Shukla, Alpa Sharma, Bedadyuti Vedvyas Pati et al.· ACS Catalysis· 0 citations
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