17 Sep 2021 News Analyzing the synthesis route of 1-Benzoylpiperazine

The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13754-38-6,1-Benzoylpiperazine,as a common compound, the synthetic route is as follows.

13754-38-6, Example 18 N-{[1-(2-(4-benzoylpiperazine-1-yl)propane-1-yl)-pyrrolidine-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide 400 mg (1 . 07 mmol) N-{[1-(2-hydroxypropyl)-pyrrolidine-(3R)-yl-carbamoyl]-methyl}-3-trifluoromethylbenzamide and 0.18 ml (1.29=01, 1.2 eq.) triethylamine described at manufacturing example 6 were dissolved to 20 ml dichloromethane and cooled to 3 C. under argon gas. 135 mg (1.18 mmol, 1.1 eq.) methansulfonyl chloride was slowly added to reaction solution and was stirred at same temperature for 30 min. 20 ml purified water was added and then organic layer was separated and concentrated with decompression. After 10 ml acetonitrile were added to obtained residues and dissolved them, 444 mg (3.21 mmol) potassium carbonate and 202 mg (1.06 mmol) 1-benzoylpiperazine were added. After stirring for 2 hours at room temperature, 15 ml saturated sodium chloride aqueous solution was added to reaction solution and was extracted twice with 15 ml ethylacetate. After organic layer was collected and dried with anhydrous magnesium sulfate, it was concentrated with decompression. 30 mg (51%) target compound as light-yellow solid was yielded by purifying obtained residues with chromatography using silicagel (mobile phase:dichloromethane/methanol=5:1 and 1:1). 1H NMR (400 MHz, DMSO-d6) 1.05 (3H, s), 1.55-1.65 (1H, m), 2.00-2.10 (1H, m), 2.15-2.25 (1H, m), 2.28-2.55 (9H, m), 2.70-2.85 (2H, m), 3.17 (1H, d), 3.54-3.65 (2H, m), 3.87 (2H, d), 4.10-4.20 (1H, m), 7.35-7.40 (2H, m), 7.40-7.47 (3H, m), 7.74 (1H, t), 7.92 (1H, d), 8.14 (1H, s), 8.18 (1H, d), 8.23 (1H, s), 9.01 (1H, t) MS (M)+ 545.6

The synthetic route of 13754-38-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; YANG JI CHEMICAL CO., LTD.; US2012/190689; (2012); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics