With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.877265-23-1,6-Bromobenzo[d]isothiazole,as a common compound, the synthetic route is as follows.
877265-23-1, 6-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]isothiazole. To a mixture of 6-bromobenzo[d]isothiazole (0.86 g, 4.0 mmol)(prepared as described in WO 2008/036308), potassium acetate (0.38 mL, 6.0 mmol), bis(pinacolato)diboron (1.3 g, 5.2 mmol), tris(dibenzylideneacetone)dipalladium (0) (0.18 g, 0.20 mmol), and tricyclohexylphosphine (0.12 g, 0.44 mmol) was added dioxane (5 mL). The resulting mixture was sealed and heated at 1 10C for 30 minutes under microwave irradiation. The mixture was cooled and passed through a short path of Celite, washing with DCM (3 x 10 mL). The combined organic phases were concentrated to give a residue that was purified by chromatography on silica gel (hexanes – 50 % EtOAc in hexanes) and triturat on with hexanes provided the product as a white powder (0.59 g, 56 %). LCMS (API-ES) m/z (%): 230.2 (100 %, M+H+); 1H NMR (400 MHz, CDCl3) delta ppm 8.95 (s, 1 H) 8.58 (s, 1 H) 7.91 – 8.02 (m, 2 H) 1.41 (s, 12 H).
The synthetic route of 877265-23-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; AMGEN INC.; WO2009/11871; (2009); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com