With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1750-42-1,Isoxazol-3-amine,as a common compound, the synthetic route is as follows.
A 40-mL vial was charged with imidazole (922 mg, 13.6 mmol) and 3-aminoisoxazole (320 |xL, 4.34 mmol) then purged with nitrogen. CH2C12 (10 mL) was introduced and the reaction mixture was cooled to -78 C in a dry ice-acetone bath. Sulfuryl chloride (352.0 |xL, 4.32 mmol) was added dropwise via syringe to the reaction mixture. Following addition, the cold bath was removed and the resultant mixture was allowed to warm to ambient temperature. After 30 minutes, (Rac)-1 -(4-bromo-5 -fluoro-2-methoxyphenyl)-5,6,7,8-tetrahydro-l,6-naphthyridin-2(lH)-one (See Preparation 8a, step 1, 957 mg, 2.71 mmol) was introduced in a single portion followed by CH2C12 (10.0 mL). The vial was sealed with a PTFE lined cap and the reaction mixture was warmed to 80 C. After 30 min, the reaction mixture was cooled to ambient temperature and diluted with an aqueous solution of citric acid (1.0 M, 25 mL), brine (25 mL) and EtOAc (50 mL). The layers were separated and the aqueous layer was extracted with EtOAc (3 x 25 mL). The combined organic layers were dried over anhydrous magnesium sulfate, filtered, and concentrated under reduced pressure and purified (100-g silica gel SNAP Ultra column, 0 to 50% 3:1 EtOAc/EtOH in heptane with DCM as a 10% additive) to afford (rac)-1-(4-bromo-5-fluoro-2-methoxyphenyl)-N-(isoxazol-3-yl)-2-oxo-1,2,7,8-tetrahydro-1,6-naphthyridine-6(5H)-sulfonamide (1.01 g, 2.023 mmol, 74.7 % yield) as a yellow solid.
1750-42-1, The synthetic route of 1750-42-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; USA Anjin Corporation; M .weisi; B .C.miergelamu; T .dining; J .siteerwogen; A .gusiman-peileisi; A .beiqiao; I .E.makesi; (177 pag.)CN107531705; (2018); A;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem