With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1062580-52-2,(3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride,as a common compound, the synthetic route is as follows.
The reaction flask is added to sodium hydroxide (10.0g, 250mmol), water and dissolved, make 10% of the solution, adding acetone to another reaction bottle 80g, the toluene sulfonyl chloride (38.13g, 200mmol), after stirring to dissolve, then adding 4-chloro pyrrolo pyrimidine (15.36g, 100mmol), stirring mixing, cooling to 0 C the following, dropping sodium hydroxide solution, the temperature is controlled at 5 C the following, completion of the dropping, heating, to control the temperature to 20-30 C stirring within the range of the reaction, to the reaction end after TLC monitoring, filtering, to get the product into the reaction bottle, adding water 200 ml, (3R, 4R)-cis-1-benzyl-4-methyl-3-methylamino-piperidine dihydrochloride (21.33g, 105mmol), stirring to dissolve, then adding potassium carbonate (82.93g, 600mmol), stirring, heating 95 C, TLC monitoring to the reaction end of the, cooling to 45-55C, by adding acetonitrile, preserving heat and stirring 1 hour, cooling to room temperature, crystallization, filtration, washing, the wet articles in added in the reaction bottle, adding dimethyl sulfoxide 250 ml, by adding 50% sodium hydroxide solution to 250 ml, stirring and heating 95 C, TLC monitoring to the reaction end rear, layered, water extraction once with dimethyl sulfoxide, merger dimethyl asian sulphone level, cooling to 75-85C, water slowly under stirring, the stirring cooling to room temperature, filtering, washing, 50% ethanol washing, filtering, drying, be [(3R, 4R) – 1 benzyl-4-methyl-piperidin-3-yl]-methyl-(7H-pyrrolo [2,3-d] pyrimidin-4-yl)-amine 25.83g, yield 77.0%, optical purity 99.8% (HPLC method).
1062580-52-2, 1062580-52-2 (3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride 45790119, apiperidines compound, is more and more widely used in various fields.
Reference：
Patent; Shandong Elohim Pharmaceutical Group Co., Ltd.; Liu, Xiaofeng; Sun, Yuanlong; Yang, Linlin; (12 pag.)CN105884781; (2016); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem