Electric Literature of 1056162-06-1, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 1056162-06-1, name is (2-(Trifluoromethyl)pyridin-3-yl)methanamine, molecular formula is C7H7F3N2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
A mixture of 4-chloro-N-isopropyl-1 ,8-naphthyridin-2-amine (150 mg, 676.6 umol, 1 eq) and [2-(trifluoromethyl)-3-pyridyl]methanamine (1.2 g, 6.8 mmol, 10 eq) was stirred at 180C for 0.5 hour under microwave and N2. TLC (EtOAc) showed that 4~chloro- N-isopropyl-1 ,8-naphthyridin-2-amine was consumed completely and several new spots. LCMS showed that several peaks and 20% of desired product. To the mixture was added water (40 mL) and extracted with EtOAc (40 mL*2). The organic layers were washed with brine (40 mL), dried over NaaSCU and concentrated. The residue was purified by prep-TLC (EtOAc). Then the crude product was further purified by prep-HPLC (Column: Phenomenex Synergi C18 150*30mm*4um; Condition: water(0.225%FA)-ACN). The salt product was basified by strong basic anion exchange resin. Then the residue was purified by prep-TLC (Dichloromethane: Methanol 10: 1) to obtain N2-isopropyi-N4-[[2-(trifluoromethyi)-3- pyridyl]methyl]-1 ,8-naphthyridine-2,4-diamine (5.4 mg, 15 umo, 2% yield) as a light yellow solid.
According to the analysis of related databases, 1056162-06-1, the application of this compound in the production field has become more and more popular.
Reference:
Patent; LIVERPOOL SCHOOL OF TROPICAL MEDICINE; THE UNIVERSITY OF LIVERPOOL; EISAI R&D MANAGEMENT CO., LTD.; WARD, Stephen A.; TAYLOR, Mark J.; O’NEILL, Paul M.; HONG, Weiqian David; BENAYOUD, Farid; (300 pag.)WO2018/134685; (2018); A2;,
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