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Microwave-assisted synthesis of 3-aminobenzo[b]thiophene scaffolds for the preparation of kinase inhibitors.
- Source :
-
Organic & biomolecular chemistry [Org Biomol Chem] 2015 Jun 28; Vol. 13 (24), pp. 6814-24. - Publication Year :
- 2015
-
Abstract
- Microwave irradiation of 2-halobenzonitriles and methyl thioglycolate in the presence of triethylamine in DMSO at 130 °C provides rapid access to 3-aminobenzo[b]thiophenes in 58-96% yield. This transformation has been applied in the synthesis of the thieno[2,3-b]pyridine core motif of LIMK1 inhibitors, the benzo[4,5]thieno[3,2-e][1,4]diazepin-5(2H)-one scaffold of MK2 inhibitors and a benzo[4,5]thieno[3,2-d]pyrimidin-4-one inhibitor of the PIM kinases.
- Subjects :
- Amination
Humans
Lim Kinases antagonists & inhibitors
MAP Kinase Kinase 2 antagonists & inhibitors
Microwaves
Protein Kinase Inhibitors chemistry
Proto-Oncogene Proteins c-pim-1 antagonists & inhibitors
Thiophenes chemistry
Protein Kinase Inhibitors chemical synthesis
Thiophenes chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1477-0539
- Volume :
- 13
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Organic & biomolecular chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26013834
- Full Text :
- https://doi.org/10.1039/c5ob00819k