With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.822-82-2,Isothiazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.,822-82-2
To a solution of l-[4-[propyl(tetrahydropyran-4-yl)amino]-5-oxido-6,7-dihydro- thieno[3,2-d]pyrimidin-5-ium-2-yl]azetidin-3-ol (5.0 mg, 14 muiotatauiotaomicronIota) in DCE (0.2 mL) was added solutions of 4-isothiazolecarboxylic acid (2.6 mg in 0.2 mL DCE, 20 muiotatauiotaomicronIota), DMAP (0.5 mg in 0.1 mL DCE, 4.1 muiotatauiotaomicronIota) and EDAC (3.9 mg in 0.2 mL DCE, 20 muiotatauiotaomicronIota). The mixture was shaken at room temperature overnight before it was concentrated in vacuo. Prep HPLC purification (basic) afforded the title compound as colorless oil. 1H NMR (DMSO-d6) delta: 9.81 (s, 1H), 9.00 (s, 1H), 5.49 (tt, J = 6.6, 3.9 Hz, 1H), 4.88 – 4.65 (m, 1H), 4.54 – 4.39 (m, 2H), 4.13 (dd, 2H), 3.96 (td, J = 11.3, 4.3 Hz, 2H), 3.54 – 3.35 (m, 5H), 3.25 – 3.16 (m, 1H), 3.07 – 2.97 (m, 2H), 1.95 – 1.82 (m, 2H), 1.74 (d, 1H), 1.65 – 1.54 (m, 3H), 0.90 (t, J = 7.3 Hz, 3H). HPLC-Retention time (XE Metode 7 CM) : 2.03 minutes. Detected “M + l”-mass: 478.15.
As the paragraph descriping shows that 822-82-2 is playing an increasingly important role.
Reference£º
Patent; LEO PHARMA A/S; LARSEN, Jens; (110 pag.)WO2019/57806; (2019); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com