- Recycling method of 1-phenyl-5-hydroxytetrazole
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The invention discloses a recycling method of 1-phenyl-5-hydroxytetrazole, and belongs to the technical field of medicinal chemistry. The preparation method comprises the following steps: a byproduct1-phenyl-5-hydroxytetrazole generated in preparation process of a rosuvastatin calcium intermediate is converted into 1-phenyl-5-mercaptotetrazole; and meanwhile, the 1-phenyl-5-mercaptotetrazole is further used for preparing a rosuvastatin calcium intermediate or rosuvastatin calcium. According to the method disclosed by the invention, reasonable recycling of the byproduct 1-phenyl-5-hydroxytetrazole is realized, the raw materials are fully utilized, the production cost of rosuvastatin calcium and the intermediate thereof is reduced, and the emission of three wastes is reduced.
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- PROCESSES FOR THE PREPARATION OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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The present invention relates to processes for the preparation of rosuvastatin calcium of formula I and pharmaceutically acceptable salts thereof using novel intermediates, and to a pharmaceutical composition containing the same.
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- INTERMEDIATE OF STATIN DRUGS AND PREPARATION THEREOF
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The present invention relates to the field of pharmaceutical chemistry, specifically relates to a statin intermediate having formula I and preparation thereof. The advantages of the method used to prepare the chiral sulfone intermediate having formula I are that a fluorophore is introduced at the beginning of the synthesis, and the intermediates are mostly solid, which enables quality control to be easily carried out.
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Paragraph 0086
(2014/08/06)
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- AN INTERMEDIATE OF STATIN DRUGS AND PREPARATION THEREOF
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The present invention relates to the field of pharmaceutical chemistry, specifically relates to a statin intermediate having formula (I) and preparation thereof. The advantages of the method used to prepare the chiral sulfone intermediate having formula (I) are that a fluorophore is introduced at the beginning of the synthesis, and the intermediates are mostly solid, which enables quality control to be easily carried out.
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- PROCESS FOR THE PREPARATION OF DIOL SULFONES
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The present invention relates to a process for the preparation of a diol sulfone derivative comprising reaction of a halomethyl substrate with a thio-aryl compound to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.
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Page/Page column 13-14
(2012/08/07)
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