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. 252881-74-6, name is tert-Butyl 3-(2-(2-(2-aminoethoxy)ethoxy)ethoxy)propanoate, A new synthetic method of this compound is introduced below., Computed Properties of C13H27NO5
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. 252881-74-6, name is tert-Butyl 3-(2-(2-(2-aminoethoxy)ethoxy)ethoxy)propanoate, A new synthetic method of this compound is introduced below., Computed Properties of C13H27NO5
To the solution of intermediate 20 (22 mg, 0.03 mmol) in DMSO (3.0 mL) were added NMM (10 mg, 0.09 mmol), tert-butyl 3-(2-(2-(2-aminoethoxy)ethoxy)ethoxy)propanoate (13 mg, 0.04 mmol), HOAt (6.4 mg, 0.05 mmol), and EDCI (46 mg, 0.05 mmol). The mixture was allowed to stir at room temperature overnight. The progress of the reaction was monitored by LC-MS. Upon completion, the mixture was concentrated under vacuum and purified by preparative HPLC to afford intermediate 21 (21 mg, 70%). The solution of intermediate 21 (21 mg, 0.02 mmol) in formic acid (5.0 mL) was stirred overnight at room temperature. The progress of the reaction was monitored by LC-MS. Upon completion, the reaction was concentrated under vacuum and the resulting residue was dissolved in DMSO (2.0 mL). To the resulting solution were added VHL-1 (13 mg, 0.03 mmol), NMM (14 mg, 0.14 mmol), HOAt (4.6 mg, 0.03 mmol), and EDCI (6.5 mg, 0.03 mmol). The reaction mixture was allowed to stir at room temperature overnight. The progress of the reaction was monitored by LC-MS. Upon completion, the mixture was concentrated under vacuum and purified by preparative HPLC to afford XY019-083 (4.5 mg, 16%) as solid. 1H NMR (600 MHz, CD3OD) delta 8.90 (s, 1H), 8.32 (s, 1H), 7.74 (s, 1H), 7.68 (s, 1H), 7.45 (d, J = 8.1 Hz, 2H), 7.39 (d, J = 8.0 Hz, 2H), 6.32 (d, J= 21.1 Hz, 1H), 6.13 (s, 1H), 5.06 – 4.99 (m, 1H), 4.64 (d, J = 8.9 Hz, 1H), 4.58 – 4.45 (m, 5H), 4.40 – 4.30 (m, 2H), 4.24 (s, 1H), 4.00 – 3.94 (m, 2H), 3.90 – 3.83 (m, 2H), 3.82 – 3.36 (m, 25H), 2.93 – 2.85 (m, 2H), 2.71 (d, J = 45.0 Hz, 2H), 2.59 -2.50 (m, 1H), 2.46 (s, 3H), 2.41 (s, 3H), 2.26 – 2.17 (m, 4H), 2.07 (d, J = 8.8 Hz, 1H), 1.54 (d, J = 6.5 Hz, 6H), 1.02 (s, 9H). MS (m/z) [M + H]+: 1240.2.
The synthetic route of 252881-74-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI; JIN, Jian; PARSONS, Ramon; STRATIKOPOULOS, Ilias; YANG, Xiaobao; (168 pag.)WO2018/81530; (2018); A1;,
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