Reference of 918538-05-3, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 918538-05-3, name is 2,4-Dichloropyrrolo[2,1-f][1,2,4]triazine belongs to chlorides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.
To a solution of 2,4-dichloropyrrolo[1,2-f][1,2,4]triazine (4a) (83 mg, 0.44 mmol) in IPA (5 mL) was added (lR,3S,5R)-2-azabicyclo[3.1.0]hexan-3-ylmethanol TFA salt (325c) (100 mg, 0.44 mmol) and DIPEA (0.23 mL, 1.32 mmol). The resulting mixture was stirred for 3h at 60 C, cooled to RT and concentrated in vacuum. The residue obtained was purified by flash column chromatography [silica gel (12 g), eluting with 0-60% EtOAc/MeOH (9: 1) in hexane from 0-100%] to afford ((lR,3S,5R)-2-(2-chloropyrrolo[l,2-f][l,2,4]triazin-4-yl)-2- azabicyclo[3.1.0]hexan-3-yl)methanol (325d) (75 mg, 64 % yield) as a semi-solid. MR (300 MHz, DMSO-i) delta 7.73 (t, J = 2.0 Hz, 1H), 7.24 – 7.16 (m, 1H), 6.72 – 6.64 (m, 1H), 4.96 (t, J = 5.8 Hz, 1H, D20 exchangeable), 4.55 – 4.44 (m, 1H), 3.77 – 3.68 (m, 1H), 3.66 – 3.50 (m, 2H), 2.35 – 2.24 (m, 1H), 1.98 – 1.80 (m, 2H), 1.28 – 1.16 (m, 1H), 0.68 – 0.57 (m, 1H); MS (ES+): 265.2 (M+l); (ES-): 299.2, 301.2 (M+Cl).
The synthetic route of 2,4-Dichloropyrrolo[2,1-f][1,2,4]triazine has been constantly updated, and we look forward to future research findings.
Reference:
Patent; BIOCRYST PHARMACEUTICALS, INC.; KOTIAN, Pravin, L.; BABU, Yarlagadda, S.; KUMAR, V., Satish; ZHANG, Weihe; LU, Peng-Cheng; RAMAN, Krishnan; (747 pag.)WO2018/232094; (2018); A1;,
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