- Preparation method of 6-(3-chloropropyl)amino-1,3-dimethyluracil
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The invention belongs to the technical field of drug synthesis processes, and provides a preparation method of 6-(3-chloropropyl)amino-1,3-dimethyluracil. 6-(3-hydroxypropyl)amino-1,3-dimethyluracil is used as a raw material, and 6-(3-chloropropyl)amino-1,3-dimethyluracil is obtained by chlorination with thionyl chloride. According to the reaction, thionyl chloride is directly used as a reaction reagent and solvent, the yield can reach 85% or above, the highest yield can reach 90% or above, and the highest purity can reach 98% or above. Compared with the prior art, the method has the advantages that the yield and the purity are obviously improved, the post-treatment is convenient, the post-treatment solvent can be recycled, and more importantly, the use of 1,2-dichloroethane which is carcinogenic and harmful to human and environment is avoided. When the method is used for synthesizing an antihypertensive drug urapidil, not only are the types of solvents reduced, but also the analysis of a 1,2-dichloroethane residual solvent in the drug quality analysis is avoided, and the method is a green and safe preparation method which is very suitable for industrial production.
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Paragraph 0020-0058
(2021/09/21)
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- Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H1 antagonists
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A series of phenothiazine carboxylic acid derivatives, having 6-amino-pyrimidine-2,4(1H,3H)-dione moiety via a appropriate linker, were synthesized and evaluated for their affinity toward human histamine H1 receptor and Caco-2 cell permeability. Selected compounds were further evaluated for their oral anti-histaminic activity in mice and bioavailability in rats. Finally, promising compounds were examined for their anti-inflammatory potential in mice OVA-induced biphasic cutaneous reaction model. Among the compounds tested, phenothiazineacetic acid compound 27 showed both histamine H1-receptor antagonistic activity and anti-inflammatory activity in vivo model.
- Kubota, Katsumi,Kurebayashi, Hirotaka,Miyachi, Hirotaka,Tobe, Masanori,Onishi, Masako,Isobe, Yoshiaki
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scheme or table
p. 2766 - 2771
(2009/12/31)
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