Hydrochloric Acid → HCID 66580548, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 4-(methoxymethyl)-3-(morpholin-4-ylcarbonyl)-1-phenyl-1,4-dihydropyrazolo[4,3-c][1,2]benzothiazine 5,5-dioxide (85 mg; 0.19 mmol; 1.00 eq.) in 1,4-dioxane (3 mL) is added HCl (0.75 mL; 1 M; 0.75 mmol; 4.00 eq.) after which reaction mixture is stirred at 100° C. for 90 min under microwave irradiation (*2). DCM is added to the reaction mixture that is neutralized to pH 6 with NaHCO3, extracted with DCM, dried over MgSO4 and purified by MD-Autoprep to give 8 mg (10%) of the title compound as an off white solid. 1H NMR (300 MHz, DMSO-d6): δ 10.94 (s, 1H), 8.00-7.91 (m, 1H), 7.71-7.50 (m, 7H), 6.99-6.86 (m, 1H), 3.83-3.55 (m, 8H). HPLC (max plot) 97.4%; Rt 3.27 min. MS (ESI+) 411.2.

Provenance & Evidence