One-pot Synthesis Of Aromatic Aminoalkyl Sulfur?Oxygen Compounds

Ruzadolane is a non-narcotic analgesic that acts on the central nervous system.Ruzadolane and its analogues are widely used in the field of medical fields.Aryl aminoalkyloxides have a wide range of biological and pharmacological activities and can be used as antipsychotics and histamine H1 receptor antagonists.However,the synthesis of aromatic aminoalkylthio compounds exists some deficiencies such as complicated multi-step,wasting of resources and increasing the cost of production,and synthesis generally involved iterative stepwise transformation with multi-step manufacture and purification,which made the procedures for drug production inefficientand cost-ineffective.Improving synthesis efficiency and reducing resource consumption are the future development trend of chemical.Therefore,developing a simple and high efficiency,low pollution and low cost method to realize the synthesis of these compounds is needed,and it is an imperative research field to improve the drug manufactures with more sustainability and less environmentally impactful.This paper mainly introduces the synthesis of aromatic aminoalkylthio and its analogues firstly.Subsequently,the synthesis of aromatic aminoalkyl ether compounds is stated in this paper.From this point of view,A novel multicomponent reaction and efficient synthesis method was developed.Ruzadolane aromatic aminoalkyl sulfides and oxygen compounds were synthesized by one-step multi-component reaction using the derivatives of phenylene precursor,cyclic tertiary amine,sodium phenylthiophenol and sodium phenol as reaction substrates.31 aromatic aminoalkyl sulfide and oxygen compounds were obtained.The cascade nucleophilic substitution of various components displayed facilitativity,high chemoselectivity and good substrate compatibility.