- Terbutaline sulfate intermediate, preparation method thereof and method for preparing terbutaline sulfate by using same (by machine translation)
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The invention discloses a terbutaline sulfate intermediate and a preparation method thereof as well as a method for preparing terbutaline sulfate by using the same, and belongs to the technical field of pharmaceutical chemistry. The invention provides a novel method for preparing terbutaline sulfate which is mild in reaction condition, high in yield and environmentally friendly, and firstly provides a terbutaline sulfate intermediate shown as a formula I; then, a catalyst is used as 10% Pd/C, an alcohol aqueous solution is used as a solvent, and hydrogenation is reduced to obtain the terbutaline II sulfate. The free base hydrochloride or hydrobromide of the formula I is converted into the formula I before hydrogenation reduction, then the terbutaline sulfate is directly obtained after hydrogenation reduction, and the advantages of mild reaction conditions, high product yield, high purity, low production cost and the like are avoided. (by machine translation)
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Paragraph 0083-0088
(2020/08/22)
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- Chemo-enzymatic route for (R)-terbutaline hydrochloride based on microbial asymmetric reduction of a substituted α-chloroacetophenone derivative
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To synthesize (R)-terbutaline hydrochloride, a potent β2- adrenoceptor-stimulating agent, asymmetric reduction of a substituted α-chloroacetophenone derivative with cultured whole-cell biocatalyst of the yeast Williopsis californica JCM 3600 was developed as the key reaction. The reduction proceeded by a si-facial attack of hydride in a highly enantioselective manner. Co-factor generation was enhanced by applying glycerol as the carbon source.
- Taketomi, Shohei,Asano, Masayoshi,Higashi, Toshinori,Shoji, Mitsuru,Sugai, Takeshi
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- Superoxide radical inhibitor
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A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), STR1 [wherein R1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R3 represents a group of the formula, STR2 (R4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group. m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.
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- Synthesis of bronchospasmolytically effective β phenylethyl aminoalkyl xanthines
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New theophylline and theobromine derivatives are synthesized from the β phenylethylaminoalkyl xanthines, whose phenyl substituent is substituted by one or two hydroxyl groups and partially also by other substituents. Different methods of synthesis are described, among them the production of the bronchospasmolytic 7 (3 [2 (3,5 dihydroxyphenyl) 2 hydroxy ethylamino] propyl) theophylline (reproterol . HCl).
- Klingler
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