Adding a certain compound to certain chemical reactions, such as: 1014645-87-4, name is Methyl 4-(1-aminocyclopropyl)benzoate hydrochloride, belongs to esters-buliding-blocks compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 1014645-87-4, Recommanded Product: Methyl 4-(1-aminocyclopropyl)benzoate hydrochloride
To a solution of 26 g (95.4 mmol) of 4-(trifluoromethyl) benzyl)-D-proline and N- hydroxybenzotriazole hydrate (17.6 g, 114 mmol) dissolved in 600 ml of DCM, 80 ml of TEA (570 mmol) and 20 g (105 mmol) of EDCI were added under nitrogen stream. The reaction mixture was left under stirring for about 6 hours, then 24 g (105 mmol) of methyl-4-(1 -aminocyclopropyl) benzoate hydrochloride were added and then left to react always under stirring for a further 24 hours at room temperature. When the reaction was complete, water (500 ml_) was added and the two phases stirred for about 10 minutes. The organic phase was separated from the aqueous phase and washed sequentially with a saturated solution of NaHC03 (400 ml), and finally with 400 ml_ of water. The organic phase was dried with Na2S04 and concentrated to obtain a solid cream colour. This solid was suspended in 1 liter of methyl-terbutyl-ether, heated to boiling, filtered hot and the clear solution thus obtained was concentrated under vacuum to dryness to obtain a white solid which was then dried at 50C for 24 hours to obtain the desired compound (32.5 g; yield: 75%). (Intermediate P3). MS: (ES/+) m/z: 447 1H NMR (400 MHz, CHLOROFORM-d) d ppm 7.80 – 8.01 (3 H, m), 7.62 (2 H, d), 7.41 (2 H, d), 7.12 -7.24 (2 H, m), 3.86 (4 H, s), 3.66 (1H, d), 3.27 (1H, dd), 3.07 – 3.18 (1H, m), 2.46 (1H, td), 2.21 – 2.38(1H, m), 1.70 – 2.03 (3 H, m), 1.05 – 1.44 (4 H, m).
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Reference:
Patent; ROTTAPHARM BIOTECH S.R.L.; PUCCI, Sabrina; ROVATI, Lucio Claudio; (0 pag.)WO2020/12305; (2020); A1;,
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