Continuously updated synthesis method about (3-Chloropyrazin-2-yl)methanamine hydrochloride

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 939412-86-9, name is (3-Chloropyrazin-2-yl)methanamine hydrochloride, A new synthetic method of this compound is introduced below., COA of Formula: C5H7Cl2N3

To a solution of (3-chloropyrazin-2-yl)methanamine hydrochloride 22 1 a (3.1 g, 21.7 mmol), 23 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate (7.1 g, 22 mmol) and 24 N,N-diisopropylethylamine (9.3 g, 72 mmol) in 25 dichloromethane (100 mL) at room temperature, 26 (S)-1-((benzyloxy)carbonyl)pyrrolidine-3-carboxylic acid (4.5 g, 18 mmol) was added in several batches. The resulting mixture was stirred at room temperature for 16 h. The reaction was quenched with 27 water (30 mL) and the organic phase was separated. The aqueous phase was extracted with dichloromethane (50 mL¡Á2), the combined organic phase was washed with saturated brine (50 mL¡Á2), dried over anhydrous sodium sulfate and filtered. The filtrate was concentrated under vacuum and the residue was purified by flash column chromatography (dichloromethane/methanol 20:1) to provide 28 benzyl-(S)-3-(((3-chloropyrazin-2-yl)methyl)carbamoyl) pyrrolidine-1-carboxylate 1b(4.85 g, 13.0 mmol, yellow oil). Yield: 72%1H NMR (400 MHz, CDCl3) delta8.43 (d, J=2.4 Hz, 1H), 8.34 (d, J=2.4 Hz, 1H), 7.37-7.26 (m, 5H), 6.92-6.85 (bs, 1H), 5.14 (s, 2H), 4.71 (d, J=4.4 Hz, 2H), 3.88-3.51 (m, 3H), 3.22-3.05 (m, 2H), 2.31-2.07 (m, 2H).

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; GUANGZHOU INNOCARE PHARMA TECH CO., LTD.; KONG, Norman Xianglong; ZHOU, Chao; CHEN, Xiangyang; US2019/177333; (2019); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem