Synthesis Of Several Pharmaceutical Intermediates

Nitrogenous heterocyclic compounds are ubiquitous in nature,and are also the main subjects in the fields of medicine,pesticide and so on.The effective components of many Chinese herbal medicine alkaloids are nitrogenous heterocyclic compounds,the similar alkaloids in living organisms,which has a high specificity to the target,and has excellent environmental compatibility,antibacterial,antitumor,antiviral,anti malarial and other activity quality.The emergence of high-throughput screening techniques and the development of sequencing methods for human genomes and genomics of biochemistry,a series of new modern science and technology,make the establishment of high efficiency,diversity,skeleton and three-dimensional structure complex"natural products"compound database become extremely urgent.Library synthesis of a class of multi class"natural products"compounds and a variety of biological activity tests will lead to a qualitative leap in synthetic drug research and organic reaction methodology.Organic synthetic chemists usually use two classical methods synthesizing organic small molecules:One is directed synthesis of the target compound;the second is directed towards the synthesis of small molecules of diversity.Professor of Harvard University put forward the target oriented synthesis of compounds in the last century,it is generally a complex organic molecules as target compounds,using reverse synthesis analysis method,from the complex to the simple screening,in order to launch a starting material to carry on the experiment.The first target compound directed synthesis method was adopted.This paper is divided into two parts:Part 1:The main research progress of several kinds of pharmaceutical intermediates are reviewed:This paper mainly introduces the research and development of nitrogen-containing heterocyclic compounds,chiral compounds and cyclopropyl compounds at home and abroad;mainly discusses piperazine,piperidine,pyridine,imidazole and cyclopropane alkane chemical intermediates,application and development prospect of comprehensive;A comprehensive study of the origin,the use of many chiral drugs and chiral separation methods.Part 2:This paper describes the properties of three kinds of pharmaceutical intermediates and characterization methods of preparation,and synthesized three kinds of pharmaceutical intermediates,namely 4,7-two aza spiro[2.5]octane-7-formic acid tert butyl ester?(R)-1-tert butoxycarbonyl-3-benzyl-3-piperidine formic acid and cyclopropane sulfonamide,and the structures of the compounds were determined by melting point test ~1HNMR,and MS.In this paper,the synthesis technology of TTBE,RBPA and CSD of the target product was studied,the synthetic route was improved,and the reaction conditions were improved.The selection of cheap material,simple operation process,mild reaction conditions and easy control and low cost avoids the harsh requirement of equipment under normal temperature conditions,unstable properties,high price and poor safety of raw materials;The yield of final product is high,the quality of the product is good,It has a vast prospect of industrialization.