- Application of flow photochemical bromination in the synthesis of a 5-bromomethylpyrimidine precursor of rosuvastatin: Improvement of productivity and product purity
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In this report we present a flow photochemical bromination of a 5-methyl-substituted pyrimidine precursor of rosuvastatin. The study demonstrated that the reaction productivity can be increased markedly with a flow-mode approach compared to a batch-mode synthesis. Indeed, reaction times can be significantly shortened from a range of hours to a range of minutes. Moreover, in addition to process intensification, the study demonstrated that significantly lower overall levels of side products are obtained when photochemical bromination is conducted in a flow mode.
- Sterk, Damjan,Jukic, Marko,Casar, Zdenko
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p. 145 - 151
(2013/03/14)
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- PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATES THEREOF
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The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvasatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2-N-O-R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.
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- PROCESS FOR THE SYNTHESIS OF ROSUVASTATIN CALCIUM
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Present invention represents process for the preparation of HMG-CoA reductsase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain
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Page/Page column 27
(2010/11/25)
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- Process for the preparation of pyrimidine derivatives
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An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group; in the presence of a base.
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Page/Page column 8; 9-10
(2010/02/11)
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