Compound N-2-methylsulfonyl ethyl group-2 beta-carbo methoxy group-3-beta-(4-chlorphenyl) nortropane, and synthetic method
A technology of methanesulfonylethyl and carbonylmethoxy, applied to compounds N-2-methanesulfonylethyl-2β-carbonylmethoxy-3β-(4-chlorophenyl) desmethyltropane and In the field of synthesis, it can solve the problems of unstable yield, cumbersome operation, and difficulty in automation, and achieve the effect of reducing radiation exposure, no special requirements, and realizing automation.
Inactive Publication Date: 2005-10-26
JIANGSU INST OF NUCLEAR MEDICINE
View PDF0 Cites 4 Cited by
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
[0008] The disadvantages of this method are: (1) cumbersome operation, unstable yield, and about 3 hours of required time, which is not conducive to the radiation protection of operators; (2) complex process, difficult to automate, and unfavorable for popularization and application
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View moreImage
Smart Image Click on the blue labels to locate them in the text.
Smart ImageViewing Examples
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0017] The raw material 2β-carbonylmethoxy-3β-(4-chlorophenyl) demethyltropane (nor-CClT) was synthesized by literature method;
[0018] A). Synthesis of N-(2-hydroxyethyl)-2β-carbonylmethoxy-3β-(4-chlorophenyl) demethyltropane (HOCClT, 4): N 2 Under atmosphere, add 0.28g nor-CClT, 0.50g 2-bromoethanol, and 0.75mL triethylamine to 15mL anhydrous acetonitrile, and stir at room temperature for 10-15min to completely dissolve nor-CClT. STOP N 2 , the oil bath was heated to 60° C. for 4 h, the heating was stopped, and the mixture was concentrated under reduced pressure to obtain a light yellow solid. Dissolve with 35mL dichloromethane, wash with 20mL 5% NaOH and 20mL water successively, and wash the organic phase with anhydrous NaOH 2 SO 4 Dried, distilled off CH 2 Cl 2 The crude product was obtained and purified by silica gel column chromatography: crude product: silica gel = 1:80, the developer was diethyl ether: triethylamine: methanol = 7: 0.1: 0.1, and 0.27 g of a white ...
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More PUM
Login to View More Abstract
The compound N-2-methylsulfonylethyl-2 beta-carbomethoxyl-3 beta-(4-chlorophenyl) demethyltropane and its synthesis method relate to the field of synthesis technology of nuclear pharmaceuticals labelled precursor compound. The synthesis method of demethyltropane (MsOCC1T) uses 2 beta-carbomethoxy-3 beta-(4-chlorophenyl) demethyltropane as raw material, and said invention adopts literature synthesis method, then first step reaction uses 2 beta-carbomethoxyl-3-beta-(4-chlorophenyl) demethyltropane and 2-bromoethanol and makes them react to synthesize intermediate product N-(2-ethoxyl)-2 beta-carbomethoxyl-3 beta-(4-chlorophenyl) demethyltropane, and the second step reaction makes said intermediate product be reacted with methyl sulfoacid anhydride to synthesize target compound.
Description
technical field [0001] Compound N-2-methylsulfonylethyl-2β-carbonylmethoxy-3β-(4-chlorophenyl) demethyltropane and its synthesis method, involving nuclear drug fluoro[18]-N-2-fluoro Technical field of synthesis of ethyl-2β-carbonylmethoxy-3β-(4-chlorophenyl) demethyltropane labeling precursor compound. Background technique [0002] Many neuropsychiatric diseases such as Parkinson's disease, schizophrenia, attention deficit hyperactivity syndrome, and cocaine addiction are closely related to the lesions of the dopamine system of the central nervous system. This lesion cannot be observed with general imaging methods (B-ultrasound, MRI, CT, etc.), but can be visually displayed by functional imaging of the dopamine system. Imaging methods mainly include: dopamine metabolism imaging, dopamine receptor imaging and dopamine transporter (DAT) imaging. Among them, dopamine transporter imaging is superior to the other two methods. It can reflect the lesion information of the dopamin...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More Application Information
Patent Timeline
Login to View More Patent Type & Authority Applications(China)
IPC IPC(8): C07D451/02
Inventor 陈正平李晓敏王颂佩张同兴杨敏吴春英徐宇平潘栋辉陆春雄蒋泉福
Owner JIANGSU INST OF NUCLEAR MEDICINE