- A α2 - Adrenergic receptor agonist hydrochloric acid an le decides and its preparation method
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The invention relates to an alpha2-adrenergic receptor stimulant apraclonidine hydrochloride and a preparation method thereof. The structural formula is shown in the specification. The preparation comprises the following steps: 2, 6-dichloro-4-nitroaniline, formic acid and acetic anhydride are mixed, heated and stirred, react and recrystallize, N-(2, 6-dichloro-4-nitrophenyl) formamide is obtained and then stirred, flows back and reacts with sulfuryl chloride and thionyl chloride, N-(2, 6-dichloro-4-nitrophenyl) dichlorocarbamide is obtained and dropwise added to an ethyl acetate solution containing ethylenediamine and triethylamine, the mixture is stirred for reaction for 1-10 h under the condition of 5-8 DEG C, 2-(2',6'-dichloro-4'- nitroanilino)-2-imidazoline is prepared, then a reducing agent is added to the solvent for reduction, hydrochloric acid is finally added to a reaction liquid, and stirring and backflow are performed for 1.5 h for preparation. The preparation process is simple to operate, the yield is high, the cost is low, the reaction route is short, little three wastes are generated, and industrial production is facilitated.
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- Process for preparation of clonidine derivatives
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A novel process for preparing clonidine derivatives has been discovered which is shorter, less expensive and safer than previously known methods. A new thiourea complex has also been discovered which can be directly cyclized to produce the corresponding heterocyclic product.
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- Feed additive for improving growth in agricultural animals
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By using α-mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilisation of fodder and the ratio of muscle to fat in favor of the proportion of muscle and protein.
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- Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.
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The chemical synthesis of 2-[(2,6-dichloro-4-iodophenyl)imino]imidazolidine (PIC) and its radioiodinated analogue [125I]PIC is described. PIC was synthesized from 2,6-dichloroaniline in five synthetic steps. This agent displayed a high affinity for the alpha 2-adrenergic receptor (IC50 = 1.5 nM) in competitive binding assays conducted with purified human platelet plasma membrane fractions. For the synthesis of radioiodinated PIC the triazene intermediate 11 was synthesized from 2,6-dichloro-4-nitroaniline in five synthetic steps. Acid-catalyzed decomposition of 11 with no-carrier-added Na125I afforded high specific activity [125I]PIC. In view of its high affinity for the alpha 2-adrenergic receptor, [125I]PIC is a potentially useful probe for studies in adrenergic pharmacology.
- Van Dort,Neubig,Counsell
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p. 1241 - 1244
(2007/10/02)
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