| In recent years,Organic chemists pay special concentration to the role of CF3 groups,CF3 groups have special high voltage negative and other special properties of fluorine atoms.Its role is more than just influence the molecular space structure.There are statistics show that in the drugs approved by FDA,twenty percent of them contain CF3 groups.Clearly,it is not a simple accident phenomenon.In the field of new drug research,screening he best the lead molecular is the key step,which is of high value to medicinal chemists.According to the fact that 25%of the drug molecules cotain CF3 groups,and is often found in high level drugs and new drugs,it is necessary to analysis some similar structure to known drug containing CF3 groups.In this paper,we showed that pyrrolidine containing CF3 groups is extremely like some existed marketed drug.As a ring structure,during the synthesis procedure,it is easier to control the stereoselectivity to provide chiral centers.Chiral drug imitate the enzyme's substrate or the transition state of enzyme-substrate,making it possible for human to influence metabolism process in the maximum degree.To synthesis five-membered heterocyclic structure,the most convenient way is[3+2]cycloaddition,In order to avoid harsh anhydrous anaerobic conditions on the operation,organic catalysis is one of the most simple and effective choice.In line with the value of low cost,low toxicity and simple starting materials,our group chose trifluoro ethyl amine hydrochloride(CF3CH3N + Cl-)as a CF3 group provider.The first part of this article will introduce the latest CF3 synthesis research of ring structure,including metal catalysis and organic catalysis,and introduce our work about how to synthesis alpha CF3 pyrrolidine ring structure using the innovative trifluoro ethyl amine hydrochloride(CF3CH3N + Cl-)(>20:1 dr,>99%ee);the second part introduces how to use the trifluoro ethyl amine hydrochloride(CF3CH3N + Cl-)to synthesis 5'-CF3 Spiro[pyrrolidin-3,2'-oxindoles](>20:1 dr,>99%ee)... |
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