147118-35-2Relevant articles and documents
Synthetic method for rosuvastatin intermediate
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Paragraph 0035-0040, (2019/01/08)
The invention discloses a synthetic method for a rosuvastatin intermediate and belongs to the field of medicine. The rosuvastatin intermediate is (3R)-tert-butyl dimethyl siloxyl-5-oxo-6-methyl triphenylphosphine caproate. According to the invention, (R)-3-tert-butyl dimethyl siloxyl-5-(1H-imidazole-1-group)-5-methyl oxoglutarate compound is taken as a raw material, is condensed with 5-methylsulfonyl-1-phenyl-1H-tetrazole and then reacts with phosphorus triphenyl oxide, so as to generate the (3R)-tert-butyl dimethyl siloxyl-5-oxo-6-methyl triphenylphosphine caproate. According to the invention, 5-methylsulfonyl-1-phenyl-1H-tetrazole is utilized to condense, so that the intermediate is stable; the detection is convenient; the phosphorus triphenyl oxide instead of triphenyl phosphine is usedas the raw material, so that the side product phosphorus triphenyl oxide of wittig reaction can be recycled; the process is simple and easy for industrialization.
Preparation method of novel rosuvastatin calcium intermediate
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Paragraph 0063; 0064; 0065; 0066; 0067; 0068; 0069-0083, (2017/08/29)
The invention provides a preparation method of a novel rosuavastatin calcium intermediate I which is suitable for industrial large-scale production. The preparation method comprises the step of enabling triphenyl methyl phosphorus bromide to react with a compound II, thus obtaining an intermediate I. The preparation method provided by the invention is safe and simple and is strong in operability, and a final finished product which is high in efficiency and purity can be obtained.
AN IMPROVED PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITOR INTERMEDIATES
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Page/Page column 10; 11, (2015/01/06)
The present invention relates to novel processes for the preparation of compounds of Formula-II useful as intermediates in preparation of HMG-CoA reductase inhibitors, and further conversion of said intermediates to HMG-CoA reductase inhibitors. The process for the preparation of compounds of Formula-II comprises reacting compounds of Formula-Ill with dimethylformamide dimethylacetal in the presence of a base to get compounds of Formula-IV, reacting the compounds of formula-IV with alkyl chloroformate in the presence of a base to get compounds of Formula-V, and converting the compounds of Formula-V into compounds of Formula-II. The compounds have the following structures, [Formulas should be inserted here] wherein X is hydrogen or hydroxy protecting group, R1 is carboxyl protecting group, Alk represents C1-C4 alkyl and R2, R3 and R4 are independently selected from substituted or unsubstituted C6-C10 aryl groups.