Reference of 180205-28-1, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 180205-28-1, name is 1-(Aminomethyl)cyclobutanol. A new synthetic method of this compound is introduced below.
3-Oxo-2-(pyridin-3-yl)-6-[4-(trifluoromethyl)phenyl]-2 ,3-di hydropyridazi ne-4-carboxylic acid(100 mg, 0.28 mmol) was dissolved in anhydrous DMF (2.0 mL). 1-(Aminomethyl)cyclobutanol(59.0 mg, 0.55 mmol), N-ethyl-N-isopropylpropan-2-amine (217 pL, 1.25 mmol), and propanephosphonic acid anhydride (T3P, 243 pL, 50% in DMF, 416 pmol) were successively added. Itwas stirred for 3 h at rt. The reaction mixture was concentrated under vacuum and purified by RP-HPLC (column: X-Bridge 018 5pm lOOx3Omm, mobile phase: (water + 0.2 vol% aqueous ammonia (32%)) acetonitrile, gradient) yielding 81 mg (66%) of the title compound.1H-NMR (400MHz, DMSO-d6): 6 [ppm] = 1.44-1.57 (m, 1H), 1.59-1.68 (m, 1H), 1.92 -2.00 (m, 4H), 3.49 (d, 2H), 5.41 (s, 1H), 7.64 (ddd, 1H), 7.89 (d, 2H), 8.16-8.24 (m, 3H), 8.70 (dd, 1H), 8.76 (s, 1H), 8.92 (d, 1H), 9.49 (t, 1H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,180205-28-1, its application will become more common.
Reference:
Patent; BAYER AKTIENGESELLSCHAFT; BAYER PHARMA AKTIENGESELLSCHAFT; DEUTSCHES KREBSFORSCHUNGSZENTRUM; GUTCHER, Ilona; ROeHN, Ulrike; SCHMEES, Norbert; ZORN, Ludwig; ROeSE, Lars; BADER, Benjamin; KOBER, Christina; CARRETERO, Rafael; STOeCKIGT, Detlef; IRLBACHER, Horst; PLATTEN, Michael; (397 pag.)WO2018/146010; (2018); A1;,
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