As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 68327-04-8, name is (1S,2S)-2-Aminocyclopentanol hydrochloride, molecular formula is C5H12ClNO, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. name: (1S,2S)-2-Aminocyclopentanol hydrochloride
A solution of 75 mg intermediate 6-[6-(d ifluoromethyl)pyrid in-3-yl]-3-oxo-2-(pyrid in-3-yl)-2,3-dihydropyridazine-4-carboxylic acid, 60 mg (1 S,2S)-2-aminocyclopentanol hydrochloride (1:1),166 mg HATU, 0.15 mL ethyldiisopropylamine and 1 mg 4-dimethylaminopyridine in 2 mL ofDMF was stirred at rt for 14 hours. Then the reaction mixture was filtered and subjected toRP-HPLC (instrument: Labomatic HD-3000 HPLC gradient pump, Labomatic Labocol Vario2000 fraction collector; column: Chromatorex 0-18 125 mm x 30 mm, eluent A: 0.lvol% formic acid in water, eluent B: acetonitrile; gradient: A 85% I B 15% – A 45% I B 55%; flow: 150 mLlmin; UV-detection: 254 nm) to yield 54 mg 6-[6-(difluoromethyl)pyridin-3-yl]-N-[(1S,2S)-2- hydroxycyclopentyl]-3-oxo-2-(pyridin-3-yl)-2,3-d ihyd ropyridazine-4-carboxamide.1H NMR (400 MHz, DMSO-d6) 6 [ppm] = 1.39- 1.56 (m, 2 H), 1.58- 1.67 (m, 1 H), 1.67- 1.76(m, 1 H), 1.77- 1.87 (m, 1 H), 2.03-2.15 (m, 1 H), 3.94 (quin, 1 H), 3.98-4.07 (m, 1 H), 4.95(d, 1 H), 7.06 (t, 1 H), 7.62 – 7.67 (m, 1 H), 7.84 (d, 1 H), 8.19 (ddd, 1 H), 8.58 (dd, 1 H), 8.70(dd, 1 H), 8.76 (s, 1 H), 8.94 (d, 1 H), 9.24 – 9.29 (m, 2 H).
With the rapid development of chemical substances, we look forward to future research findings about 68327-04-8.
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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