125995-13-3Relevant articles and documents
AN IMPROVED AND COMMERCIALLY VIABLE PROCESS FOR PREPARATION OF PYRROLE DERIVATIVES WITH IMPROVED IMPURITY PROFILE & MINIMISATION OF UNIT OPERATIONS.
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Page/Page column 68; 69; 70-71, (2020/02/14)
The present invention relates to improved process for the preparation of a pyrrole derivative as a racemic mixture, an enantiomer, a diastereoisomer, a mixture thereof, a tautomer thereof or a pharmaceutically acceptable salt and hydrates thereof and also intermediates involved therein. Particularly invention is directed to improved processes for the preparation of pyrrole derivatives such as (4R,cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluorophenyl)-5-(1-methyl-ethyl)-pyrrole-1-yl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester of formula IV followed by its conversion into [R-(R*, R*]-2-(4-fluorophenyl)- β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1- heptanoic acid particularly calcium salt and its hydrate represented by Formulae I/IA respectively wherein formation of the impurities is either eliminated or minimized in the corresponding intermediaries.
Preparation method of atorvastatin calcium intermediate
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, (2018/10/11)
The invention belongs to the field of medicines and chemical industry, and particularly relates to the field of pharmacy, in particular to a preparation method of an atorvastatin calcium intermediate.The preparation method comprises the following steps: firstly preparing a compound II into a lithium reagent, then reacting with methyl chloroformate, introducing an ester group, aminolyzing the ester group into amine, dehydrating the amide, and finally reducing a cyano group to obtain a target compound. By the brand-new preparation method of the atorvastatin calcium intermediate, a compound VI can be synthesized under the premise that highly toxic substances such as hydrocyanic acid, hydrobromide and the like are not used, and the compound VI is used for preparing a compound I; reagents usedin the whole preparation process are safe and environment-friendly, and the preparation method is more suitable for industrial production.
Preparation method of synthetic intermediate of Lipitor
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, (2016/10/09)
The invention discloses a novel preparation method for a side-chain fragment compound, ATS-9, of Lipitor and solves a problem that poisonous reagents, such as Raney nickel, are required in synthesis in the prior art. The preparation method includes the steps of: with epoxy chloropropane as an initial raw material, performing a ring opening reaction with Grignard reagent to obtain a first chiral hydroxyl group; performing cyano substitution, hydrolyzing the substituted cyano group into ester, performing homologation reaction to extend the carbon chain, and performing reduction with diethylmethoxylborane and sodium borohydride, and protecting the two hydroxyl groups and finally performing the Staudinger reaction to prepare the ATS-9.