With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.17402-83-4,Benzo[b]thiophen-4-amine,as a common compound, the synthetic route is as follows.
Example 8 N2-(1 ,1-dioxido-1-benzothien-4-yl)-N4-(5-fluoro-1 H-indazol-3-yl)-2,4-pyrimidinediamineA solution of N-(2-chloro-4-pyrimidinyl)-5-fluoro-1 H-indazol-3-amine (25.00 mg, 0.095 mmol) and 1-benzothien-4-ylamine (14.15 mg, 0.095 mmol) in N-Methyl-2-pyrrolidone (NMP) (474 pi) was treated with 2 drops of 2N HCI in Et20 and stirred at 100 ¡ãC for 20 hours. Solid NaHC03 was added followed by oxone (58.3 mg, 0.095 mmol), and a few drops of water. The reaction was stirred at rt for 20 hours. The reaction mixture was filtered through a 0.2 muetaeta ptfe frit and diluted with MeOH then purified via prep HPLC using a Sunfire 5 pm, 30×150 mm, C18 column eluting with 25-65percent MeCN/water (with 0.1 percent TFA) to give the title compound as the TFA salt. 1H NMR (DMSO-d6) delta : 12.97 (s, 1 H), 9.32 (s, 1 H), 9.18 (s, 1 H), 8.18 (s, 1 H), 7.68 (d, J = 5.6 Hz, 1 H), 7.59 (dd, J = 9.0, 4.2 Hz, 1 H), 7.55 (d, J = 5.6 Hz, 1 H), 7.42 (d, J = 7.8 Hz, 1 H), 7.25 – 7.37 (m, 3H), 6.57 (t, J = 8.0 Hz, 1 H).; MS (m/z) 409 (M+H+).
17402-83-4, 17402-83-4 Benzo[b]thiophen-4-amine 298484, abenzothiophene compound, is more and more widely used in various fields.
Reference£º
Patent; GLAXO GROUP LIMITED; CASILLAS, Linda, N.; CHAKRAVORTY, Subhas, J.; CHARNLEY, Adam, Kenneth; EIDAM, Patrick; HAILE, Pamela, A.; HUGHES, Terry, Vincent; JEONG, Jae, U.; KANG, Jianxing; LAKDAWALA SHAH, Ami; LEISTER, Lara, Kathryn; MARQUIS, Robert, W.; MILLER, Nathan, Andrew; PRICE, Daniel, J.; SEHON, Clark, L.; WANG, Gren, Z.; ZHANG, Daohua; WO2011/120025; (2011); A1;,
Benzothiophene – Wikipedia
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