Synthesis Of Neuroprotective Drug NS-7 And Its Derivative

At present, cerebrovascular disease is the main disease which threat humanhealth seariously. In China, the number of people that died of cerebrovascular disease is more than cardiac disease and cancer, and the percent of ischemic cerebrovascular disease is about 60%⁸0%. Every cause of cerebral ischemia will induce the necrosis of nerve cells, and the patient will be cursed by the resids. Cerebral ischemia will induce injury and death of nerve cells, according to its pathomechanism, we call it neuroprotective drug, it can inhibit the process of death of nerve cells, it main contains ion channel regulators, receptor regulators, cyclooxygenase inhibitor et al.NS-7, 4-(4-fluorophenyl)-2-methyl-6-(5-piperimidinopen- tyloxy)pyrimidine hydrochloride, a novel neuroprotective drug, discovered by Nippon Shinyaku company Japan. The investigation suggests that NS-7 readily penetrates into brain, in which it exists for the most part in parenchyma fraction. It can block the neurotoxin receptor site 2 of voltage-sensitive sodium channels in the brain, inhibit calpain activation, and it is a Na⁺ and high-voltage-activated (L- and N-type) Ca²⁺channel blocker. It is suggested that blockade of Na⁺ and Ca²⁺ channels implicated in the cerebroprotective action of hypoxic injury in...