- Synthesis of ipratropium bromide-related compounds
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Synthesis of ipratropium bromide metabolites is described. Copyright Taylor & Francis Group, LLC.
- Tsyskovskaia, Irina,Kandil, Mustapha,Beaumier, Yves
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- Preparation method for ipratropium bromide
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The invention relates to the technical fields of chemical engineering and pharmacy, in particular to a preparation method for ipratropium bromide. The preparation method comprises the following stepsof using N-isopropylnortropine or N-isopropyl tropine as the raw material, and respectively performing methylation reaction with iodomethane, so as to obtain an iodine-containing compound; performingdeiodination reaction on the iodine-containing compound by special metal oxide, metal salt or bromine, and performing follow-up treating, so as to obtain the ipratropium bromide. The preparation method has the advantages that the storage and use condition of the methylation reagent raw material is greatly reduced, so that the transportation and storage cost of the raw material is reduced; comparedwith the bromomethane, the iodomethane has stronger reaction activity, and the reaction conditions are milder, so that the usage amount of the methylation reagent in the methylation reaction is reduced; the safety, operability and reaction effect of the original technology are enhanced by the preparation method, and the requirement on equipment is reduced.
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Paragraph 0040; 0041; 0042
(2018/11/22)
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- Preparation method of ipratropium bromide
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The invention relates to a preparation method of an M-choline receptor blocking agent of ipratropium bromide 1. The preparation method comprises the following steps of using ethyl phenylacetate as starting raw materials; performing reaction with isopropyl tropanol; generating phenylacetate isopropyl tropeine; then, performing substitution, reduction and addition reaction to obtain the ipratropium bromide. The method has the advantages that the operation is simple; safety and controllability are realized; the work protection is low; the preparation method is suitable for industrial production. The formula is shown as the accompanying drawing, and the molecular weight is 412.36.
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- Synthesis and radiolabelling of ipratropium and tiotropium for use as PET ligands in the study of inhaled drug deposition
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Ipratropium bromide [(1R,3r,5S,8r,2′RS)-3-(3′-hydroxy-2′- phenylpropionyloxy)-8-isopropyl-8-methyl-8-aza-bicyclo[3.2.1]octan-8-ium bromide] and tiotropium bromide [(1R,2R,4S,5S,7s)-7-[2′-hydroxy-2′, 2′-di(thiophen2″-yl)acetoxy]-9,9-dimethyl-9-aza-3-oxatricyclo[3.3.1. 02,4]nonan-9-ium bromide] are inhaled drugs used in the treatment of chronic obstructive pulmonary disease (COPD) and asthma. Tertiary amine precursors have been synthesized and radiolabelled with carbon-11 by N-alkylation with [11C]CH3I. The [11C] ipratropium and [11C]tiotropium positron emission tomography (PET) ligands are obtained with high radiochemical purity, in 0.3 and 0.5% non-decay corrected yields based on [11C]CO2 at end-of-synthesis and specific activities of 11 and 18 GBq μ mol-1, respectively, calculated at end-of-synthesis. These PET radioligands can be used in the study of inhaled drug deposition. CSIRO 2006.
- Issa, Fatiah,Kassiou, Michael,Chan, Hak-Kim,McLeod, Malcolm D.
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