9 - Hydroxy - Xanthene - 9 - (cyclic Hydrocarbon Amino) Ethyl Ethers, Compounds Were Designed And Synthesized

Anticholinergic drugs are a class of important peripheral nervous system drugs,which block cholinergic receptors,so that neurotransmitter acetylcholine receptor-binding and should not. Clinically,it is the treatment of organophosphate poisoning,one of the main drugs,in addition to drugs used to stop the secretion,mydriatics,spasmolytic and muscle relaxant analgesic agent,etc. Militarily,to deal with chemical weapons attacks,as the anti-terror drug dealing with terrorists. In recent years,studies of such drugs has become a global hot spots.Initially,the anti-cholinergic drugs are extracted from natural substances,and the present study mainly focuses on synthesis.However,many anti-cholinergic drugs have the effect to be slow and the side effect is big,which limited the clinical application of these drugs.Therefore, looking for good activity,high selectivity,the role of strong,low toxicity and a new indication for a new anticholinergic drags has become the one of the hot spots for drug synthetic workers. Anticholinergic drags are the main cholinergic neurotransmitter acetylcholine receptor M and N competition receptors,so its structure must fit M to N receptor and receptor in order to show the efficiency of the structure of biological activity.The majority of anti-cholinergic drugs has strong anti-M role but not the role of strong anti-N.Among them,the tricyclic anti-cholinergic drugs are a class of strong activity of anticholinergic drugs.Have been reported in the literature category xanthene anticholinergic drugs for many amino alcohol esters,and its ring structure can be divided into groups,nitrogen-containing ester groups and three parts.However,according to M-receptor antagonist structure-activity relationship of us know that the cyclic group with M receptor on the corresponding region of the pro-ester bond or through hydrophobic van der Waals force additional happen combination of blocking acetylcholine receptors.Ester and anti-cholinergic activity is not necessary,it could be ether bond,that is,amino-alcohol compounds.We according to the three types of ethoxy hydroxylamine anticholinergic drug design and synthesis 9-hydroxyl-xanthene-9-ethyl(cycloalkylamino)ethers to look forward to the high selectivity,the role of strong,low toxicity and a new indication for a new type of anti-cholinergic drugs.At our reference on the basic design of the synthetic route to o-chlorobenzoic acid as the starting material through Ullmann condensation and dehydration have been xanthene-one closed-loop,and then at the role of sulfur ylides under its ethylene oxide synthesis intermediates. We chose piperidine ring for the cationic compound,isonicotinic acid as raw material,after esterification,hydrogenation reduction synthesized 1-methyl-4-piperidine methanol,and finally at the role of sodium synthesized target compounds.Because of time reasons,we can not set up for the compounds to carry out activity in animal model testing.Nevertheless,it is providing a refference for future drug screening,combinatorial and pharmacological research.In addition,we used phosphorus oxychloride reagent for synthesis of the UV absorber of salicylic acid esters,phenyl salicylate and p-octylphenyl salicylate.Experiments show that the method is simple and mild conditions,the advantages of environmentally friendly,and is a suitable synthetic route for industrial production.