21709-18-2Relevant articles and documents
A preparation method of the clonidine hydrochloride
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Paragraph 0048; 0055; 0058; 0061; 0062, (2018/04/28)
The invention discloses a method for preparing the clonidine hydrochloride, including intermediates 1 synthesis, intermediate 2 synthesis and clonidine hydrochloride synthetic three steps, the present invention in order to 2, 6 - dichloroaniline as raw materials, through the hydroformylation reaction get intermediate 1, "one-pot" get clonidine free base, finally with hydrogen chloride ethanol solution into salt clonidine hydrochloride. By processing the raw material synthetic process, by utilizing the free alkali in the course of refining into salt after adjusting pH, and the clonidine hydrochloride is used for purification of the pulping process control such as ethyl acetate, to obtain a high-purity clonidine hydrochloride preparation method. The method not only improves the product purity and yield, impurity can also effectively control, but also greatly reducing the cost, simplifying the process, is more suitable for industrial production.
Methylation of imidazoline related compounds leads to loss of α2-adrenoceptor affinity. Synthesis and biological evaluation of selective I1 imidazoline receptor ligands
Schann, Stephan,Greney, Hugues,Gasparik, Vincent,Dontenwill, Monique,Rascente, Carla,Lacroix, Gabriel,Monassier, Laurent,Bruban, Veronique,Feldman, Josiane,Ehrhardt, Jean-Daniel,Bousquet, Pascal
experimental part, p. 4710 - 4715 (2012/09/22)
Methylated analogues of imidazoline related compounds (IRC) were prepared; their abilities to bind I1 imidazoline receptors (I1Rs), I2 imidazoline binding sites (I2BS) and α2-adrenoceptor subtypes (α
A Novel Synthesis of Clonidine, an Anti-Hypertensive Drug from o-Chloronitrobenzene
Ayyangar, N. R.,Brahme, K. C.,Srinivasan, K. V.
, p. 64 - 65 (2007/10/02)
An elegant, cost-effective synthesis of clonidine (4) is reported from readily available starting materials. o-Chlorophenylhydroxylamine (2), obtained from o-chloronitrobenzene, is formylated to N-(2-chlorophenyl)-N-hydroxyformamide (3).In a one-pot procedure, 3 is converted to clonidine by chlorination with thionyl chloride and then with thionyl chloride/sulfuryl chloride, followed by condensation with ethylenediamine.
3-Anilino-2,4-diazabicyclo[3.2.1]octenes
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, (2008/06/13)
Novel 3-anilino-2,4-diazabicyclo[3.2.1]octenes, physiologically tolerable acid addition salts thereof and method of preparing same are described. These compounds are useful as tranquilizers, diuretics and antihypertensives.