| Publication No: | IN202411009640 [India] | Application No: | IN202411009640 |
| Title: | A process for thepreparation (un)substituted quinolone and isoquinolone compounds | ||
| Publication Date: | 22-08-2025 | File Date: | 12-02-2024 |
| Inventor(s): | Santosh Baburao Mhaske; Sachin Dhanraj Mahale | ||
| IPC Classification: | C07D498/04, A61K31/5365, C07D498/14, C07D498/20, C07F17/02, C07D471/04 | ||
| Abstract: | The present invention discloses a functionalized isoquinolone and quinolone compounds and an efficient transition-metal-free approach for the synthesis of the same. The invention provides a highly functionalized isoquinolones from the reaction of dimethyl-2-((phenylamino)methylene) malonate with aryne precursors under mild. The reaction proceeds through insertion of aryne into the C-C s-bond, which offers a novel and practical entry to access a wide range of isoquinolones with enhanced yields. The substrate scope is broad as the process can stands a variety of functional groups and the application of the developed process has been demonstrated in the total synthesis of antimalarial agent SJ000101247. Also, the highly functionalized quinolones are also useful in the synthesis of floxacins based compounds and derivatives e.g. ciprofloxacin, norfloxacin, G003967, etc. or Formula I Formula IV |
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