Synthetic Route of 16133-25-8, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 16133-25-8 as follows.
Example 64Pyridine-3-sulfonic acid [3-(4,4-dimethyl-6-trifluoromethyl-l,2,3,4-tetrahydro- quinolin-2-yl)-phenyl]-amideTo a stirred solution of 3-(4,4-dimethyl-6-trifluoromethyl-l,2,3,4-tetrahydro-quinolin-2-yl)- phenylamine (150 mg, 0.47 mmol) in pyridine (0.74 mg, 0.94 mmol) and dichloromethane (3 mL) at 0¡ãC was added dropwise a solution of pyridine-3-sulfonyl chloride (100 mg, 0.56 mmol) in dichloromethane (1 mL). The mixture was stired at room temperature overnight. Thin layer chomatography and LC-MS indicated that 3-(4,4,6-trimethyl-l,2,3,4-tetrahydro- quinolin-2-yl)-phenylamine was consumed completely. The mixture was quenched with water (5 mL) and extracted with dichloromethane (5 mL x 2). The combined organic layers were dried over anhydrous sodium sulfate and evaporated. The residue was purified by column chomatography on silica gel to afford pyridine-3 -sulfonic acid [3-(4,4-dimethyl-6- trifluoromethyl-l,2,3,4-tetrahydro-quinolin-2-yl)-phenyl]-amide (170 mg, 78.7percent) as a white solid. MS (ESI+APCI) M+l=442.3.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,16133-25-8, its application will become more common.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; FENG, Lichun; HUANG, Mengwei; LIU, Yongfu; WU, Guolong; ZHOU, Mingwei; WO2012/52372; (2012); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem