345891-62-5Relevant articles and documents
Method for synthesizing atorvastatin ester by using continuous flow tubular reactor
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Paragraph 0035-0042; 0043-0045; 0051, (2022/03/27)
The invention relates to a method for synthesizing atorvastatin ester by using a continuous flow tubular reactor, which comprises the following steps: (1) mixing a compound 1 with acetonitrile to obtain a material A; (2) uniformly mixing concentrated hydrochloric acid, acetonitrile and water to prepare a diluted hydrochloric acid solution to obtain a material B; (3) the material A and the material B are respectively pumped into a tubular reactor for a chemical reaction, the reaction temperature is 18-28 DEG C, and the reaction time is 40-90 s; and after the reaction is finished, carrying out vacuum concentration, centrifugation, washing and drying on the obtained reaction liquid to obtain the target product, and the specific synthesis route is as follows. By adopting the method disclosed by the invention, the time required by the whole reaction process is extremely short, the reaction condition is mild, and the situation that by-products are generated due to overlong reaction time or overhigh reaction temperature, so that the yield of the target product is high and reaches 97% or above, and the purity of the target product is high and reaches 99% or above is effectively avoided.
Synthesis and evaluation of atorvastatin esters as prodrugs metabolically activated by human carboxylesterases
Mizoi, Kenta,Takahashi, Masato,Haba, Masami,Hosokawa, Masakiyo
supporting information, p. 921 - 923 (2016/05/24)
We synthesized 11 kinds of prodrug with an esterified carboxylic acid moiety of atorvastatin in moderate to high yields. We discovered that they underwent metabolic activation specifically by the human carboxylesterase 1 (CES1) isozyme. The results sugges
Synthesis of some impurities and/or degradation products of atorvastatin
Stach, Jan,Havlicek, Jaroslav,Placek, Lukas,Radl, Stanislav
, p. 229 - 246 (2008/12/22)
Synthesis of some impurities and/or degradation products of atorvastatin, calcium (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl) pyrrol-1-yl]-3,5-dihydroxyheptanoate, is described. These include its desfluoro analog, the corresponding (3S,5S)-and (3S,5R)-epimers, atorvastatin lactone, and some other potential impurities. The synthesized compounds as well as the corresponding intermediates were characterized by 1H NMR, 13C NMR and MS.