Cu-catalyzed synthetic process for acetaminophen from dihalobenzenes

Abstract

Up to now, various kind of non-opioid analgesic drugs have been developed and their developments have been progressed to the improvement or the complement of weak point of the former analgesics at each time. In these days, one of them, acetaminophen (1) is known for the most widely used analgesics in the world on the account of the many advantages in terms of the medicinal application and few adverse effects in comparison with other analgesics. However, the former synthetic process of acetaminophen (1) have many problems such as, generation of undesired isomer and use of strong, toxic acid and so on. These problems accompany additional purification steps and recycle of waste acids, finally, bring about the additional cost that affect the production cost of acetaminophen (1). In this paper, we are going to discuss our efforts to develop both an efficient and an economic process for acetaminophen (1) using Cu-catalyzed reaction from dihallobenzenes. We could not only improve the drawbacks of the former synthetic process, but also could make the synthetic process more eco-friendly under mild reaction conditions and the synthetic steps shorter without the additional purification.