These common heterocyclic compound, 939412-86-9, name is (3-Chloropyrazin-2-yl)methanamine hydrochloride, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Recommanded Product: (3-Chloropyrazin-2-yl)methanamine hydrochloride
To a solution of(3S,6S)-l-((benzyloxy)carbonyl)-6-(hydroxymethyl)piperidine- 3-carboxylic acid (0.78 g, 2.66 mmol) in 20 mL of DMF was added HATU (1.21 g, 3.2 mmol). After stiring for 30 min under N2, (3-Chloro-pyrazin-2-yl) methanamine hydrochloride (0.48 g, 2.66 mol) and Et3N (0.8 g, 7.98 mmol) was added. The reaction mixture was stirred at room temperature for 12 hours under N2. The mixture was partitioned between EA and water. The organic layer was washed with 1 N HC1 and water, dried over sodium sulfate, filtered and concentrated in vacuo. The residue was purified by silica gel column chromatography to afford (2S,5R)-benzyl 5-(((3- chloropyrazin-2-yl)methyl)carbamoyl)-2-(hydroxymethyl)piperidine-l -carboxylate (0.7 g, 63.0% yield). 1HNMR (400 MHz, CD3OD): delta= 8.50 ~ 8.54 (m, 1 H), 8.35 (d, / = 2.4 Hz, 1 H), 7.31 ~ 7.41 (m, 5 H), 5.16 (s, 2 H), 4.63 (s, 2 H), 4.34 ~ 4.38 (m, 1 H), 4.21 ~ 4.25 (m, 1 H), 3.72 ~ 3.77 (m, 1 H), 3.63 ~ 3.67 (m, 1 H), 3.01 ~ 3.07 (m, 1 H), 2.46 ~ 2.54 (m, 1 H), 1.80 ~ 1.93 (m, 3 H), 1.61 ~ 1.71 (m, 1 H). MS (ESI): M/Z (M+l): 419.1
The synthetic route of (3-Chloropyrazin-2-yl)methanamine hydrochloride has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MERCK SHARP & DOHME CORP.; WU, Hao; KIM, Ronald M.; LIU, Jian; GAO, Xiaolei; BOGA, Sobhana Babu; GUIADEEN, Deodialsingh; KOZLOWSKI, Joseph; YU, Wensheng; ANAND, Rajan; YU, Younong; SELYUTIN, Oleg B.; GAO, Ying-Duo; LIU, Shilan; YANG, Chundao; WANG, Hongjian; WO2014/114185; (2014); A1;,
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