13118-11-1Relevant articles and documents
Synthesis process of glycopyrronium bromide
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Paragraph 0063; 0089-0091, (2021/10/02)
The invention discloses a synthesis process of a glycopyrronium bromide bulk drug, and the process comprises the following steps: carrying out hydroxyl protection on an a-cyclopentyl mandelic acid compound by using a dihydropyran compound, carrying out esterification reaction, removing a protecting group, and finally carrying out quaternization reaction to obtain glycopyrronium bromide. The method is mild in reaction condition, does not need to introduce a large amount of auxiliaries and solvents, conforms to the green chemistry principle, and is suitable for industrialization.
Substitutes of glycopyrronium bromide as well as preparation method and medical application thereof
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Paragraph 0020; 0032-0033; 0039-0040, (2020/07/14)
The invention discloses glycopyrronium bromide substitutes shown as a formula (I) and a formula (II), a preparation method of the glycopyrronium bromide substitutes and application of the glycopyrronium bromide substitutes in preparation of medicines for treating myopia, medicines for regulating ciliary muscle paralysis, medicines for preventing, treating and delaying juvenile myopia and medicinesfor treating chronic obstructive pulmonary disease (COPD), bronchitis or asthma. The compounds provided by the invention have excellent water solubility, powder flowability and suitable pH value stability of ophthalmic preparations and injections, and are in excellent medicinal alternative forms of glycopyrronium bromide.
A preparation method of the glycopyrrolate
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Paragraph 0041; 0045, (2018/04/26)
The invention discloses a method for preparation of glycopyrrolate, firstly the α - cyclopentyl mandelic acid for benzyl protected hydroxy, then the conventional method and 1 - methyl - 3 - pyrrolidinol esterification of key intermediate pyrrolidinol ester; in the middle of the invention supplies the key under the condition of Pd/C debenzylation, finally methyl bromide quaternary ammonium formation salting out the solid filter and get the glycopyrrolate crude, refined is obtained when the location of the qualified products. In order to prevent the occurrence of side reactions, the method of using very low cost introduced into hydroxyl protective agent benzyl, greatly improves the yield, simplifying the post-treatment, reduces the amount of waste water. The method of the invention with the production operation is simple, the production cost is low, raw materials are easy, high yield, low pollution and the like, the resulting product in accordance with the pharmaceutical quality standards.