Some common heterocyclic compound, 68774-77-6, name is 8-Chloro[1,2,4]triazolo[4,3-a]pyrazine, molecular formula is C5H3ClN4, 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. Application In Synthesis of 8-Chloro[1,2,4]triazolo[4,3-a]pyrazine
A stirred mixture of (-)-R-tert-butyl 4-(aminomethyl)-3,3-difluoropiperidine-1-carboxylate (230mg, 0.92 mmol), 8-chloro-[1,2,4]triazolo[4,3-a]pyrazine (127 mg, 0.83 mmol) and DIPEA (0.30 mL, 1.8 mmol) in n-BuOH (5 mL) was heated to 95C under nitrogen for 13 hr. The reaction mixture was allowed to cool to room temperature and concentrated in vacuo. The residue was purified by column chromatography over silica gel (ethyl acetate/hexane = 1/1) to afford the title compound as a white powder (210 mg, 62%). MS (ESI) calcd for C16H22F2N602: 368.2; found: 369.1 [M+H]. 1H NMR (400 MHz, CDCI3) 6 8.72 (s, 1H), 7.41 (d, J = 4.8 Hz, 1H), 7.35 (d, J = 4.8 Hz, 1H), 6.50-6.45 (m, 1H), 4.47-4.09 (m, 2H), 4.02-3.96 (m, 1H), 3.79-3.72 (m, 1H), 3.09-2.69 (m, 2H), 2.45-2.29 (m, 1H), 1.92-1.87 (m, 1H), 1.68-1.58 (m, 1H), 1.47 (s, 9H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 68774-77-6, its application will become more common.
Reference:
Patent; RUGEN HOLDINGS (CAYMAN) LIMITED; SHAPIRO, Gideon; (246 pag.)WO2016/196513; (2016); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem