The origin of a common compound about (1-Aminocyclopropyl)methanol hydrochloride

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,115652-52-3, its application will become more common.

Related Products of 115652-52-3 ,Some common heterocyclic compound, 115652-52-3, molecular formula is C4H10ClNO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

To a mixture of 2- (5-amino-2- (furan-2-yl) -7H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yl) -2-phenylpropanoic acid (40 mg, 0.1 mmol) , (1-aminocyclopropyl) methanol hydrochloride (16 mg, 0.13 mmol) , DIPEA (60 mg, 0.46 mmol) in DMF (1 mL) was added HATU (50 mg, 0.13 mmol) at rt and the mixture was stirred at rt for 3 hrs. The mixture was diluted with 15 mL of EtOAc, washed with brine (5 mL x 3) , dried over Na 2SO 4, concentrated and the resulted oil was purified by prep-TLC (EtOAc: 100%) to give the title product (28.0 mg, yield: 61%) after lyophilization. 1H NMR (400 MHz, DMSO-d6) delta 8.22 (s, 1H) , 8.10 -7.82 (m, 3H) , 7.75 (s, 1H) , 7.35 -7.19 (m, 4H) , 7.11 (d, J = 8.0 Hz, 2H) , 6.79 -6.69 (m, 1H) , 4.55 (t, J = 5.6 Hz, 1H) , 3.59 (dd, J = 11.2, 6.0 Hz, 1H) , 3.41 (dd, J = 11.2, 5.6 Hz, 1H) , 2.25 (s, 3H) , 0.73 -0.50 (m, 4H) . MS: M/e 459 (M+1) +.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,115652-52-3, its application will become more common.

Reference:
Patent; BEIGENE, LTD.; ZHANG, Guoliang; ZHOU, Changyou; (152 pag.)WO2019/196803; (2019); A1;,
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