848498-20-4

Upstream product

• 610-72-0 2,5-dimethylbenzoic acid 
• 13730-55-7 methyl 2,5-dimethylbenzoate 
• 72985-20-7 2-bromomethyl-5-methylbenzoic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 

Downstream Products

• 1022984-27-5 6-methyl-2-(4-dimethylaminophenyl)-2,3-dihydroisoindol-1-one 
• 1022984-33-3 6-methyl-2-(4-dimethylamino-3-methoxyphenyl)-2,3-dihydroisoindol-1-one 
• 72985-23-0 6-methylisobenzofuran-1(3H)-one 
• 72985-22-9 2-(hydroxymethyl)-5-methylbenzoic acid 
• 150867-03-1 2-formyl-5-methylbenzoic acid 
• 1352835-84-7 2-((3-(1-carbamoyl-7-(2-methoxyethoxy)-9H-pyrido[3,4-b]indol-4-yl)-2-fluorophenylamino)methyl)-5-methylbenzoic acid 
• 1416990-04-9 3-(6-methyl-1-oxoisoindolin-2-yl)piperidine-2,6-dione 

Relevant academic research and scientific papers

Copper-promoted direct amidation of isoindolinone scaffolds by sodium persulfate

Isoindolinones are ubiquitous structural motifs in natural products and pharmaceuticals. Establishing an efficient method for structural modification of isoindolinones could significantly facilitate new drug development. Herein, we describe copper-promoted direct amidation of isoindolinone scaffolds mediated by sodium persulfate. The method exhibits mild reaction conditions and high site-selectivity, and enables the structural modification of the drug indobufen ester with various amides with yields of 49 to 98%. It is also gram-scalable. Additionally, the reaction mechanism appears to involve a radical and a carbocationic pathway.

Isosteric analogs of lenalidomide and pomalidomide: Synthesis and biological activity

A series of analogs of the immunomodulary drugs lenalidomide (1) and pomalidomide (2), in which the amino group is replaced with various isosteres, was prepared and assayed for immunomodulatory activity and activity against cancer cell lines. The 4-methyl and 4-chloro analogs 4 and 15, respectively, displayed potent inhibition of tumor necrosis factor-α (TNF-α) in LPS-stimulated hPBMC, potent stimulation of IL-2 in a human T cell co-stimulation assay, and anti-proliferative activity against the Namalwa lymphoma cell line. Both of these analogs displayed oral bioavailability in rat.

CARBOLINE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.

Isoindol-1,3-dione and isoindol-1-one derivatives with high binding affinity to β-amyloid fibrils

Based on the structural features of Indoprofen and PIB, a series of isoindol-1,3-diones 1a-k and isoindol-1-ones 2a-l were designed and synthesized. These 23 compounds were evaluated by competitive binding assay against aggregated Aβ42 fibrils using [125I]TZDM. All the isoindolone derivatives showed very good binding affinities with Ki values in the subnanomolar range (0.42-0.94 nM). Among them, isoindol-1,3-diones 1i and 1k and isoindol-1-ones 2c and 2i exhibited excellent binding affinities (Ki = 0.42-0.44 and 0.46-0.49 nM) than those of Indoprofen (Ki = 0.52 nM) and PIB (Ki = 0.70 nM). These results suggest that isoindolones could be served as a scaffold for potential AD diagnostic probes to monitor Aβ fibrils.

DIPEPTIDYL PEPTIDASE IV INHIBITOR

A compound of the formula [I] wherein each symbol is as defined in the specification, or a stereoisomer thereof, a pharmaceutically acceptable salt thereof or a solvate thereof show a DPP-IV inhibitory activity and are novel compounds effective for the treatment of type II diabetes, obesity and the like.