- Stable carteolol hydrochloride, preparation method thereof and eye medicine combination
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The invention relates to stable carteolol hydrochloride, a preparation method thereof and an eye medicine combination, in particular to a method for preparing carteolol hydrochloride. The method comprises the following steps of preparing 3-amino-2-cyclohexenone, tetrahydro-2,5(1H, 6H)-quinolinone, 5-hydroxy-3,4-dihydro-2(1H)-carbostyril and 5-(2,3-epoxypropoxy)-3,4-dihydro-2(1H)-carbostyril, and then the carteolol hydrochloride is obtained. Furthermore, the invention provides the carteolol hydrochloride crude medicine obtained according to the method, the eye medicine combination prepared by using the obtained carteolol hydrochloride as the crude medicine, and applications of the obtained carteolol hydrochloride to preparation of drugs for treating or preventing glaucoma or ocular hypertension. The method has excellent pharmaceutical characteristics, for example, the obtained crude medicine and a preparation has excellent stability.
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Paragraph 0121; 0131; 0143; 0154; 0165; 0175; 0176; 0187
(2017/12/06)
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- A process for the preparation of 5-(3-tert-butylamino-2-hydroxypropoxy)-3,4-dihydrocarbostyryl.
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A process for the preparation of 5-(3-tert-butylamino-2-hydroxypropoxy)-3,4-dihydrocarbostyryl hydrochloride of formula (I), by reacting 5-hydroxy-3,4-dihydrocarbostyryl with epichlorhydrine in a mixture of aprotic solvent, selected from dimethylsulphoxide, dimethylformamide and methylpyrrolidone, with water at room temperature, in the presence of alkali hydroxides, reacting the compound thus obtained with tert-butylamine in the presence of dimethylsulphoxide and salifying the final product.
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- 3,4-DIHYDROCARBOSTYRIL DERIVATIVES AND PROCESS FOR PRODUCING THE SAME
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Novel compounds represented by the formula STR1 wherein R. sup.1, R. sup.2, and R' and R" are defined as hereinafter, having a blocking activity on β-adrenergic nerves, novel intermediates useful for synthesis thereof and processes for preparing the same are disclosed. When substitution is at the 5-position and R 1 and R 2 are hydrogen, R' and R" are not simultaneously hydrogen and a 1 to 4 carbon atom alkyl group in the claimed compound. "
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