Reference of 86873-60-1, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 86873-60-1, name is 5-Chloro-2-picolinic acid. This compound has unique chemical properties. The synthetic route is as follows.
5-Chloropicolinic acid (75.6 mg, 480 muetaiotaomicron) was suspended in dichloromethane (6 mL), the suspension was cooled to 0-5C (ice bath) and oxalyl chloride (85.2 mg, 58.8 mu, 672 mupiiotaomicron) as well as dimethylformamide (0.137 M in toluene, 87.6 mu^, 12 mupiiotaomicron) were added. The mixture was stirred for 17 h at room temperature. Then, it was concentrated in vacuo (40C, 5 mbar) to afford 5-chloropicolinoyl chloride as yellow oil (88.8 mg, quant.). After that, tert-butyl ((4aR,5R,9R)-5-(6-amino-3-fluoropyridin-2-yl)-3,3-difluoro-5,8,8-trimethyl-9-oxido- 2,3,4,4a,5,8-hexahydro-[l,4]thiazino[2, l-f][l,2]thiazin-7-yl)carbamate (Int-51AAp, 80 mg, 168 muiotaetaomicron) was dissolved in dichloromethane (5 mL), the solution cooled to 0-5C (ice bath) and N,N-diisopropylethylamine (82.6 mg, 111.6 muL, 640 muiotaetaomicron) was added, followed by a solution of 5-chloropicolinoyl chloride (vide supra, 88.8 mg, 480 muiotaetaomicron) in dichloromethane (6 mL). The reaction mixture was stirred for 15 min at 0-5C, followed by 3 h at room temperature. Then, an aqueous solution of sodium carbonate (10%, 15 mL) was added, the mixture was stirred for 10 min at room temperature. After phase separation, the aqueous layer was extracted the dichloromethane (2 x 10 mL), the combined organics were dried (sodium sulfate) and concentrated in vacuo. The crude was purified by column chromatography (silica gel, 12 g, eluting with ethyl acetate / n-heptane, gradient 10:90 to 40:60) to yield, after drying in vacuo (40C, 5 mbar), the title compound as an off-white solid (110 mg), that was used in the next step without further purification. HPLC (method LCMS_gradient) tR = 3.6 min. MS (ES+) m/z 615.1 [M+H].
While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 86873-60-1, 5-Chloro-2-picolinic acid.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; BARTELS, Bjoern; CUENI, Philipp; DOLENTE, Cosimo; GUBA, Wolfgang; HAAP, Wolfgang; KUGLSTATTER, Andreas; OBST SANDER, Ulrike; PETERS, Jens-Uwe; ROGERS-EVANS, Mark; VIFIAN, Walter; WOLTERING, Thomas; (231 pag.)WO2016/55496; (2016); A1;,
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