Alkali Promotes The Synthesis Of Potential Drug Sulfur Compounds

Sulfur-containing sulfone and sulfide compounds are widely used in the medical field because of their unique characteristics.Sulfone compounds can be used as small molecule PLK1 inhibitors and TRPV4 receptor antagonists;arylamine alkyl sulfides have a wide range of biological and pharmacological activities can be used as analgesics and 5-HT4 receptor antagonists.Therefore,the activity and synthetic methodology of these two types of compounds have attracted extensive attention.Overcoming the shortcomings of traditional synthetic process steps and achieving efficient synthesis of sulfone and arylamine alkyl sulfide compounds have become a hot research content and an important research goal in the pharmaceutical synthesis industry.This thesis mainly studies the synthesis methods of these two types of compounds.1.Synthesis of aromatic amine alkyl sulfone compounds: Based on the strategy of double-functionalization of C-N bonded tertiary amine with potassium tert-butoxide,a simple halogenated aromatic hydrocarbon,cyclic tertiary amine and alkyl sulfone were constructed New multicomponent reaction of raw materials.Through this multi-component reaction,the efficient synthesis of arylamine alkyl sulfone compounds is achieved.Halogenated aromatic hydrocarbons,as highly reactive substrates,are cheap and easy to obtain,saving costs;cyclic tertiary amines are used as a key component to initiate the cleavage of a simple C-N bond to provide an alkyl and nitrogen source to achieve more bifunctionalization Component reaction;alkylation of sulfone through alkyl sulfone ?-C,avoiding the shortcomings of traditional synthesis methods such as: the large amount of oxidant used in the oxidation of sulfide and the pungent odor of thiol.This system uses a catalyst-free,simple reaction process to quickly assemble halogenated aromatic hydrocarbons,cyclic tertiary amines and alkyl sulfones and other structural units onto complex-structured aromatic amine alkyl sulfone compounds with good to excellent production.Rate,providing an effective way to efficiently obtain aromatic amine alkyl sulfone.2.Synthesis of arylamine alkyl sulfide compounds: mainly describes tri-(di-phenylpyridine)iridium-catalyzed multi-component reactions with halogenated aromatic hydrocarbons,cyclic tertiary amines and aryl sulfides as substrates,The corresponding arylamine alkyl sulfide compounds are obtained.The corresponding configuration inversion of the cyclic tertiary amine is restricted and shows higher nucleophilicity,so it can be used as an amine source to carry out amination reaction with aromatic halides;meanwhile,it provides alkyl groups to realize the alkylation of sulfides.In this paper,the reaction solvent,time and temperature of the reaction system are discussed in detail.It is determined that tris(2-phenylpyridine)iridium(0.5 mol%)is used as the catalyst,t-BuOK is used as the base,and DMSO is used as the solvent at 120 ? At the reaction temperature of 12 hours,it is the best reaction condition for this reaction.In this paper,27 arylamine alkyl sulfide compounds with different substituents were synthesized.pounds,a total of 40 aromatic amine alkyl sulfone compounds.