Diphenyl Glycolic Acid Ester Anti-cholinergic Drug Synthesis Intermediates Microwave Catalytic Synthesis

Anticholinergic drug is the antagonist of Acetycholine, which is an important neural drug. Inmilitary affairs, it can be used in the fields of prevention, first aid and treatment of injury caused bynerve agents. Meanwhile, for it can create hallucinations and is not inclined to cause death,anticholinergic drug is applied in antiterrorism to overmaster terrorists. In civil life, it has a certaindegree of therapeutic effect on parkinsonism, car sickness, seasickness, stomach convulsion, gastriculcer and intestinal functional diseases. It is also one of the drugs used to cure and save patientswith organophosphorus pesticide poisoning. The literature also shows that such drugs may have thetherapeutic effect of blocking human dreams and rehabilitation.In this paper, 3-quinuclidinyl benzilate (QNB), a classical anticholinergic compound, wassynthesized, which is an M receptor antagonist and is widely used in fundamental experiments asthe tool medicine for research on the structure and function of M receptor. Benzaldehyde was firstused as the starting material, via the reactions of benzoin condensation, esterification,rearrangement under alkalinity condition, Benzilic acid was obtained, and through the reactions ofesterification and transesterification, 3-quinuclidinyl benzilate was obtained. This paper as wellexplored the influence on each step, of different conditions, such as the catalysts, reaction time andthe methods of post-processing.For the side effects of 3-quinuclidinyl benzilate are comparatively strong, of which the cationgroup is replaced, according to research, in the way that quinine ring is replaced with tropine ringand piperidine ring, and as a result, benzilic esters were synthesized. In the synthesizing process,good experimental results were achieved by using tropine alcohol and 4-substituted piperidinealcohol, while nearly no experimental result can be achieved if morpholine alcohol andN-substituted piperidine alcohol were used.Benzilic esters are classical M receptor antagonists, the antinicotinic activity of which iscomparatively weak. According to the research, diphenyls are linked by oxygen atoms, and rigidXanthene ring is formed, which enhances the antinicotinic activity. In this experiment, xanthenecarboxyl acid was used as the starting material to synthesize hydroxyl xanthene carboxylates, ofwhich the receptor selectivity is enhanced due to their good binding with the receptor. During the synthesizing process of the two intermediates, methyl benzilate and methyl xanthene carboxylate,microwave catalysis was utilized, which greatly shortened the reaction time and increased thereaction efficiency. Also, the ideal reaction condition of microwave catalyisis of esterification wasfound via orthogonal experiment. Microwave radiation to promote the organic synthesis reaction isa new focus in the field of Organic Chemistry, which has gradually developed since the 80s lastcentury. It has received wide attention due to its characteristics, like short reaction time, highefficiency, good stereoselectivity, easy post-processing, and environmental friendliness and so on.