Downstream synthetic route of 22065-85-6

22065-85-6 1-Benzylpiperidine-4-carbaldehyde 89584, apiperidines compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.22065-85-6,1-Benzylpiperidine-4-carbaldehyde,as a common compound, the synthetic route is as follows.

Example 11 Production of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methylpiperidine using a mixed solvent of 2-propanol and toluene and sodium methoxide and adopting method A Into a 50-mL four-necked flask were charged 2.0 g (10.4 mmol) of 5,6-dimethoxy-1-indanone, 2.5 g (12.3 mmol, 1.2 equivalents) of 1-benzyl-4-formylpiperidine and 24 mL of a mixed solvent (2-propanol: toluene = 16: 14). After the air in the system was replaced with nitrogen, 2.4 g (12.4 mmol, 1.2 equivalents) of a 28%-sodium methoxide/methanol solution was poured into the reaction solution with refluxing (83C). After completion of the pouring, stirring was continued with refluxing for 1 hour and 2 minutes to complete the reaction. Then, the reaction solution was cooled to 7C (cooling rate: 33C/hour). Crystals began to be precipitated at 42C. The crystals were collected by filtration, washed with water (30 ml) and 6 mL of methanol and then dried at 50C (drying time: 1 hour and 20 minutes) to obtain 2.87 g of the crystals of the title compound (yield: 73.1%). 1H-NMR data of these crystals agreed with those obtained in Example 1.

22065-85-6 1-Benzylpiperidine-4-carbaldehyde 89584, apiperidines compound, is more and more widely used in various.

Reference£º
Patent; Eisai R&D Management Co., Ltd.; EP1911745; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Brief introduction of 22065-85-6

The synthetic route of 22065-85-6 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.22065-85-6,1-Benzylpiperidine-4-carbaldehyde,as a common compound, the synthetic route is as follows.

To a cooled solution of 1-benzyl-4-piperidinecarboxaldehyde (407 mg, 2.0 mmol) and propargylamine (165 mg, 3.0 mmol) in MeOH (6 mL) at 0 C, a small amount of CF3CO2H (5 drops) was added. After being stirred for 1 h, NaBH3CN (189 mg, 2.9 mmol) was added to the solution portionwsise. The mixture was stirred at rt overnight and then quenched with aqueous saturated NaHCO3. The mixture was concentrated in vacuo and then extracted with AcOEt.

The synthetic route of 22065-85-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Universitat Autonoma de Barcelona; Consejo Superior de Investigaciones Cientificas (CSIC); National University Corporation Okayama University; Universidad de Alcala; Esteban, Gerard; Unzeta, Mercedes; Inokuchi, Tsutomu; Marco-Contelles, Jose Luis; Samadi, Abdelouahid; Iriepa, Isabel; Ojima, Masaki; Li, Wang; EP2727916; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem