Application of 851386-40-8, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.851386-40-8, name is 4-Chloro-2,5-difluoropyridine, molecular formula is C5H2ClF2N, molecular weight is 149.53, as common compound, the synthetic route is as follows.
To a dry microwave vial under nitrogen was added (S)-isopropyl 2-(fert- butoxy)-2-(4-(4,4-dimethylpiperidin-l-yl)-2,6-dimemyl-5-(l,2,3,4-tetrahydroisoquinolin- 6-yl)pyridin-3-yl)acetate (46.8 mg, 0.090 mmol), 4-chloro-2,5-difluoropyridine (149.5 mg, 1.0 mmol), and acetonitrile (0.9 mL). The reaction was flushed briefly with nitrogen, treated with Hunig ‘s base (230 mu, 1.37 mmol), capped and heated in a microwave reactor at 85 – 95 C for 17h, followed by heating at 80 C for 36h in a sand bath. The crude reaction was purified via reverse phase Prep-HPLC to afford isopropyl (S)-2-(fert- butoxy)-2-(5-(2-(2,5-difluoropyridin-4-yl)-l,2,3,4-tetrahydroisoquinolin-6-yl)-4-(4,4- dimethylpiperidin-l-yl)-2,6-dimethylpyridin-3-yl)acetate, 42 mg (quant). LCMS (M+l) = 635.4.
The chemical industry reduces the impact on the environment during synthesis 851386-40-8, I believe this compound will play a more active role in future production and life.
Reference:
Patent; VIIV HEALTHCARE UK (NO.5) LIMITED; BOWSHER, Michael S.; DESKUS, Jeffrey; EASTMAN, Kyle J.; GILLIS, Eric P; FRENNESSON, David B; IWUAGWU, Christiana; NAIDU, B. Narasimhulu; PARCELLA, Kyle E.; PEESE, Kevin M; SAULNIER, Mark G; SIVAPRAKASAM, Prasanna; (220 pag.)WO2018/127801; (2018); A1;,
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