17247-58-4, name is (Bromomethyl)cyclobutane, belongs to bromides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Safety of (Bromomethyl)cyclobutane
[4~NitiO-3-(2,2,2~trifluoro-ethoxy)-phenyl]-a.cetic acid methyl ester (33 g, 94.5 mmol) and (bromomethyl)cyclobutane (17 g, 1 14.1 mmol) were mixed in DMSO (50 mL) and KOH (6.4 g, 14,1 mmol) was added in portions over 15 min. The reaction mixture was stirred for 16 h and water (100 mL) was added. The reaction mixture was extracted with EtOAc (3 x 50 mL). The combined organic phases were dried over MgS04and evaporated to give a crude yellow oil, which was purified by silica gel gradient column chromatography using Heptane-EtOAc (9: 1 – 4: 1) to give 15 g (40%) of the product as a. yellow oil. (The synthesis was repeated with temperature kept at 40 C over 16 h to give the product in quantitative yield).JH NMR (300 MHz, CDC /TMS): delta 7.86 (d, ./ 8.0 Hz, IH), 7.12-7.09 (m, 2H), 4.50 (q, J – 7.7 Hz, 2H), 3.68 (s, 3H), 3.55 (t, J = 7.3 Hz, I H ). 2.22,-2.10 (m, 2H), 2.03-1.75 (m, 5H), 1.70-1.55 (m, 2H).13C NMR (75 MHz, CDC TMS): 5 172.9, 150.5, 146.4, 139.4, 126.0, 122.7, 122.6 (d, VCF= 277.6 Hz), 1 16.0, 67.5 (q,CF36.7 Hz), 52.3, 49.6, 40.7, 33.9, 28.2, 27.9, 18.4.
The synthetic route of 17247-58-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ENVIVO PHARMACEUTICALS, INC.; KOENIG, Gerhard; BLAIN, Jean-francois; WO2013/106328; (2013); A1;,
Bromide – Wikipedia,
bromide – Wiktionary