Synthesis Of 2-Methoxy-Isobutylisonitrile?MIBI? And Preparation Of Cu?MIBI?₄BF₄

Atpresent,withthedevelopmentofimagingequipmentand radiopharmaceuticals,the role of radionuclide imaging in medical imaging technology is becoming more and more important.Single-Photon Emission Computed Tomography?SPECT?and Positron Emission Tomography?PET?are two kinds of CT techniques of nuclear medicine.Since they are all imaging gamma rays emitted from patients,they are collectively referred to as Emission Computed Tomography.Among them,SPECT is widely used in thyroid imaging,bone imaging and myocardial perfusion imaging because of its easy access to^99mTc,low cost,wide adaptability to imaging agents,high specificity and low radioactivity.The advancement of nuclear medicine imaging technology mainly relies on the coordinated development of three elements of nuclear medicine imaging equipment,processing software and imaging agents.Therefore,the importance of imaging agents in nuclear medicine imaging is self-evident,and the development of synthetic and effective imaging agents has become one of the important topics in the field of modern nuclear medicine.Myocardial perfusion imaging is used for non-invasive examination of heart disease.It began in the 1970s.After nearly 40 years of development,its huge diagnostic value has been widely accepted worldwide,and it has become an important imaging method for the diagnosis,efficacy evaluation and prognosis of coronary heart disease.In 1984,Holman et al.developed a new class of^99mTc?I?isonitriles,of which^99mTc-MIBI?MIBI:hexakis methoxy isobutyl isonitrile?is the most promising imaging agent for ^99mTc-labeled isonitrile-based myocardial perfusion imaging agents.It has been widely used in the clinic and is a cash cow in the nuclear medicine department.^99mTc-MIBI is another new ^99mTc labeled myocardial perfusion imaging agent developed after^99mTc-TBI and^99mTc-CPI.It overcomes the shortcomings of^99mTc-TBI,^99mTc-CPI in liver and lung,and low ratio of heart/liver and heart/lung.It is the most widely used^99mTc labeled myocardial perfusion imaging drug.Three-dimensional ventricular amelioration can be obtained by using^99mTc-MIBI in combination with SPECT.In recent years,it has been found to be of great value in the diagnosis of lung cancer,thyroid cancer,breast cancer and other multidrug resistance studies,and is widely used.Early diagnosis of cardiovascular disease is of great significance in the prevention and treatment of cardiovascular diseases.MIBI is the ligand for the most mainstream myocardial perfusion imaging agent ^99mTc-MIBI.The advantages and disadvantages of its synthesis method play an important role in the cost and quality of the product.Based on the problems of the past synthesis methods,this paper uses acetone cyanohydrin as raw material to select the four-step reaction to prepare the final product MIBI by MIBF.Through the study of the synthesis reaction of each step,the optimal synthesis reaction conditions and the key process parameters of each reaction were determined,and a synthetic route with stable process,high yield and low risk was obtained.At the same time,the MIBI metal complex Cu?MIBI?₄Cl is preserved for a long time and structural confirmation.