Synthetic Procedure Optimization Of (+)PD128907

In recent years, the dopamine D3 receptor (D3R) functions had gained a lot of attention in drug dependence. Pharmacological experiments proved that (D3R) receptors are involved reinforcement and reward of drug dependence. The dopamine D3 receptor mainly existed in the mesolimbic channel, and the change of this area was the important neural basis of central nervous system's drug dependence. Researches showed that the selectivity of (+) PD 128907 for D3 receptor has better which 1000 times for D2 receptors and 10000 times for D4 receptor. (+) PD 128907 can reduce the behavior of rats to find cocaine when it's in drug addiction. (+) PD 128907 can't make people addicted, and it can be used in the treatment of drug addiction.To meet needs of market demand, we successfully optimized the synthesis route of (+)PD 128907.4-Methoxyphenol was selected as the starting material, after 13 steps reactions, the final product was obtained. we have optimized the reaction time, temperature, ratio of reactants, varieties of catalysis and other parameters that may influence the reaction yield and product quality. We also improved the work up procedure after reaction, and optimized the separation and purification method. This paper was aimed at improving the yield, reducing the cost and the use of dangerous chemicals, which make the amplification process feasible, and the target compound can be obtained in kilogram scale.