Reference of 52378-63-9, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.52378-63-9, name is (3-Aminopyridin-2-yl)methanol, molecular formula is C6H8N2O, molecular weight is 124.14, as common compound, the synthetic route is as follows.
Neat (3-aminopyridin-2-yl)methanol (may be prepared as described in Description 80; 68 mg, 0.55 mmol) was added in one charge to a stirred suspension of 2- [(phenylmethyl)oxy]-5-(4-pyridinyl)benzoic acid (may be prepared as described in Description 79;120 mg, 0.393 mmol), EDC (151 mg, 0.786 mmoi), HOBT (120 mg, 0.79 mmol) and triethylamine (0.11 ml, 0.79 mmol) in N,N-dimethylformamide (1.5 ml) in air at 15 C. The reaction mixture was stirred at 15 C overnight. Water (30 ml) was added and the reaction mixture extracted with ethyl acetate (30 ml x 3). The organic phases were dried with Na2S04 and concentrated. The residue was purified by pre-HPLC(instrument: Gilson-281 , Column: WATERS XBRIDGE 30-100MM SUM, Mobile Phase : A: 0.04%NH3H2O B:CH3CN, Flow rate: 30.0ml/L, Gradient: 0-10min, B = 30-38% RT= P1 : 7.0min; P2: 9.5min) to yield the title compound as a white solid. 20 mg,HNMR (400MHz, D SO-d6); 10.82 (s, 1 H), 8.57-8.63 (m, 3H), 8.35-8.36 (m, H), 8.27- 8.29 (m, 1 H), 7.95-7.97 (m, 1 H), 7.70-7.71 (m, 2H), 7.53-7.55 (m, 2H), 7.32-7.41 (m, 5H), 5,54 (s, 2H), 4.65 (s, 2H).MS (electrospray): m/z [M+H]+ = 412
Statistics shows that 52378-63-9 is playing an increasingly important role. we look forward to future research findings about (3-Aminopyridin-2-yl)methanol.
Reference:
Patent; GLAXO GROUP LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; NICHOLS, Paula Louise; EATHERTON, Andrew John; BAMBOROUGH, Paul; JANDU, Karamjit Singh; PHILPS, Oliver James; ANDREOTTI, Daniele; WO2011/38572; (2011); A1;,
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