Cynthesis Of Cubstituted Thiophenols And Indobufen

Thiophenols,having a broad synthetic utility as pharmaceutical,pesticide,material,catalyst and natural product synthesis,However,the traditional synthetic methods more or less have the disadvantages of harsh reaction conditions,the use of toxic,harmful,expensive reagents,cumbersome reaction steps and so on.Isoindolinones are pivotal fragments in natural products and synthetic drugs.As a kind of isoindolinone drugs,indobufen has been widely used in the treatment of cardiovascular and cerebrovascular diseases.A lot of methods have been developed for the preparation of indobufen,However,They usually have some disadvantages,such as long route,low yield,complex post-reaction treatment,and more liquid slag.Therefore,to explore a simple,efficient and universal synthesis method of the two compounds has become the top priority.The synthesis of sulphonation reduction of para-substituted thiophenols was studied in this thesis,and the process was optimized to make it less by-products,less waste residue,higher yield and higher purity.P-chlorobenziophenol,p-fluorobenziophenol and p-bromothiophenol were synthesized with the highest yield of 65.0% and 99.5% purity,43.6% and 99.5% purity,respectively.The synthesis of ortho-substituted thiophenols and meta-substiuted thiophenols was studied in this thesis.We studied its diazotization and sulfurizing reagents synthetic route,and also explore the effect of different sulfurizing reagents on the synthetic yield,try to replace the traditional system of potassium ethyl xanthatenine with hydrated sodium sulfide system,compared with the traditional system,it is more economical and environment friendly,has higher atom utilization rate,and without producing toxic xanthogenic acid waste liquid.O-ethylphenthiophenol,o-chlorphenthiophenol and m-methylphenthiophenol were synthesized in a maximum yield of 43.8%,42.0% and 34.4%,respectively.The synthesis of indobufen under the condition of solvent-free and catalyst-free was studied in this thesis.Indobufen was synthesized with the highest yield of 91.7%and the purity of 99.0%,which is more green and efficient than the traditional synthesis method.