Modification Of The Glycosylation Structure Of T614 Derivatives And Aspirin And Its Derivatives

This thesis consisted of two sections, the synthesis of T614's derivatives and studies on the structure modifying of Aspirin and its derivatives in carbohydrate.At this article we briefly summarized the progress in research of the Non-steroidal Anti-inflammatory Drugs - Cyclooxygenase-2 inhibitors, designed on the structure modifying of T614 by p-naphthol alkylation, anmino tosylation and benzol acetylation, mainly prepared one derivative of T614 and 16 lateral-chained structure modified compounds of its parted intermediates, the exploratory research had been done in order to search after the lead compounds possessing improved biological activities.The novel methods for the synthesis of T614's derivatives were described, the total synthetical process included seven steps from 4-chloro-3-nitroanisole in which some improvements and innovations of the methods compare to the reference were worked out. In the end, we obtained the termination-product with high overall yield-3-(acylamino) -6-phenoxy-7-(p-tolylsulfonylamino) -4H-1 -benzopyran-4-one.To modify the structure and optimize the activities of Aspirin, a series of glucosides of Aspirin and its derivatives also natural product-Salicin were prepared via using bromo-glucose protected by acetyl and salicylic acid and its derivatives reacted by way of phase transfer catalysis, then applied the acetylation or catalytic hydrogenation before acetylation and deacetyltion to the corresponding acquired glucosides. These methods were proved to be relatively simple and stable with high yields and superior practical value.The purities of most compounds above were analyzed by HPLC, Their structures were confirmed and characterized by MS, NMR and IR.