Downstream synthetic route of 300543-56-0

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.300543-56-0,(R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

Example 2a) [2- [4- [ (4-chlorophenyl)phenylmethyl] -1-piperazinil] ethoxy] – acetonitrile dihydrochlorideCharge 2400 mL of acetonitrile to the reaction vessel, add 400 g of (-) -1- [ (4-chlorophenyl) phenylmethyl ] -4-piperazine, 300 g Na2CO3, 20 g KI and 300 g of 2- (2-chloroethoxy) acetonitrile in turn under stirring.Stir and gradually raise the temperature to 110-115 0C. Keep the temperature for 20 hours, after the reaction is completed, cool the mixture to 80-90 0C and add 25 g of activated carbon and stir for 20 minutes. Filter off carbon and wash cake with appropriate amount of acetonitrile. Into combined filtrate in? troduce dry HCl gas until pH value reaches 0.5-1. Continue to stir the slurry for 20 minutes and filter. Wash the cake with appropriate amount of ethanol and dry at 50-550C for 10 hours to obtain 520 g of the title product.The yield 95%, HPLC (area) 95 %. The obtained [2- [4- [(4- chlorophenyl) phenylmethyl] -1-piperazinyl] ethoxy] -acetonitrile dihydrochloride has in the X-ray powder diffractogram the peaks at about: 8.5; 18.5; 19.1; 22.7; 24.9; 25.7; 25.9 in 28.7 +/- 0.2 2Theta.b) Maceration of a crude [2- [4- [ (4-chlorophenyl)phenylmethyl] – 1-piperazinyl] ethoxy] -acetonitrile dihydrochloride10 g of [2- [4- [ (4-chlorophenyl) phenylmethyl] -1-piperazinyl] ethoxy] -acetonitrile dihydrochloride were suspended in 30 mL of methanol. The suspension was heated to the boiling tempera? ture and stirred at this temperature for at least 20 minutes. Thereafter the suspension was cooled to 0 0C and stirred at this temperature for one hour. The precipitate was filtered, washed with cold methanol and dried. HPLC (area) 98 %., 300543-56-0

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

Reference£º
Patent; KRKA, TOVARNA ZDRAVIL, D.D., NOVO MESTO; WO2008/110586; (2008); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics