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. 1014645-87-4, name is Methyl 4-(1-aminocyclopropyl)benzoate hydrochloride, A new synthetic method of this compound is introduced below., Quality Control of Methyl 4-(1-aminocyclopropyl)benzoate hydrochloride
Description 142: methyl 4-(1-(5-chloro-2-(2-phenylpyrrolidin-1- yl)nicotinamido)cyclopropyl)benzoate (D142)A solution of 5-chloro-2-(2-phenylpyrrolidin-1 -yl)nicotinic acid (D98) (150 mg, 0.5 mmol), methyl 4-(1 -aminocyclopropyl)benzoate hydrochloride (D7) (1 14 mg, 0.5 mmol) and N,N-Diisopropylethylamine (194 mg, 1 .5 mmol) in dimethylformamide (10ml) was stirred 1 h at room temperature, then benzotriazol-1 -yl- oxytripyrrolidinophosphonium hexafluorophosphate (PyBOP) (312 mg, 0.6 mmol) was added. The mixture was stirred at room temperature overnight, then poured into ice-water (20ml) and extracted with ethyl acetate (2x20ml). The organic solution was washed with brine (40ml), dried over Na2S04 and concentrated to obtain a residue which was purified by flash chromatography on silica gel eluting with a mixture petroleum ether/ethyl acetate (4:1 ). Collected fractions after solvent evaporation afforded the title compound (D142) (189 mg) as a yellow solid.1 H NMR (400MHz ,CHLOROFORM-d) delta (ppm): 8.10 (1 H, d, J = 2.4 Hz) 8.03 – 8.00 (2H, m) 7.74 (1 H, d, J = 2.4 Hz) 7.67 (1 H, s) 7.41 (2H, d, J = 8.0 Hz) 7.28 – 7.18 (5H, m) 5.36 – 5.32 (1 H, m) 3.91 (3H, s) 3.69 – 3.63 (1 H, m) 3.16 – 3.1 1 (1 H, m) 2.43 – 2.37 (1 H, m) 1 .97 – 1 .87 (3H, m) 1 .49 – 1 .39 (4H, m)
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
Reference:
Patent; ROTTAPHARM S.P.A.; BORRIELLO, Manuela; ROVATI, Lucio; STASI, Luigi Piero; BUZZI, Benedetta; COLACE, Fabrizio; WO2012/76063; (2012); A1;,
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