With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.18480-53-0,3,4-Dichloroisothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.
3,4-Dichloroisothiazole-5-carboxylic acid (CAS 18480-53-0, 34.8 mg, 0.18 mmol) was dissolved in DMF (200 iL). HBTU (83 mg, 0.22 mmol) and TEA (61.1 iL, 0.44 mmol) were added. The solution was stirred for 6 mm and then 4-(2-amino-3-methylbutanoyl)benzonitrile hydrochloride (Example 49b, 35 mg, 0.15 mmol) in DMF (400 iL) and TEA (61.1 iL, 0.44 mmol) was added. The reaction mixture was stirred at rt for 1 h and then purified by preparative HPLC to give 3,4-dichloro-N-(1-(4-cyanophenyl)-3-methyl-1-oxobutan-2-yl)isothiazole-5-carboxamid (15 mg, 28percent).1H NMR (500 MHz, CDCI3) 5 ppm 0.87 (d, 3 H) 1.12 (d, 3 H) 2.26 – 2.36 (m, 1 H) 5.75 (dd, 1 H)7.74 (d, 1 H) 7.86 (d, 2 H) 8.12 (d, 2 H).MS (ESI) m/z 379.7 [M-H], 18480-53-0
As the paragraph descriping shows that 18480-53-0 is playing an increasingly important role.
Reference£º
Patent; ACTURUM LIFE SCIENCE AB; LINDE, Christian Erik; PAULSEN, Kim; SOHN, Daniel; SVENSSON, Mats A; VALLIN, Karl S A; WEIGELT, Dirk; MINIDIS, Alexander; WO2014/184235; (2014); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com