- Method for synthesizing atorvastatin ester by using continuous flow tubular reactor
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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.
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Paragraph 0035-0042; 0043-0045; 0051
(2022/03/27)
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- Discovery of atorvastatin as a tetramer stabilizer of nuclear receptor RXRα through structure-based virtual screening
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Retinoid X receptor alpha (RXRα), a central member of the nuclear receptor superfamily and a key regulator of many signal transduction pathways, has been an attractive drug target. We previously discovered that an N-terminally truncated form of RXRα can b
- Wang, Xin,Chong, Shuyi,Lin, Huiyun,Yan, Zhiqiang,Huang, Fengyu,Zeng, Zhiping,Zhang, Xiaokun,Su, Ying
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p. 413 - 419
(2019/01/23)
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- Synthesis and evaluation of atorvastatin esters as prodrugs metabolically activated by human carboxylesterases
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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
- Mizoi, Kenta,Takahashi, Masato,Haba, Masami,Hosokawa, Masakiyo
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supporting information
p. 921 - 923
(2016/05/24)
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- Asymmetric synthesis of the HMG-CoA reductase inhibitor atorvastatin calcium: An organocatalytic anhydride desymmetrization and cyanide-free side chain elongation approach
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An efficient asymmetric synthesis of atorvastatin calcium has been achieved from commercially available diethyl 3-hydroxyglutarate through a novel approach that involves an organocatalytic enantioselective cyclic anhydride desymmetrization to establish C(
- Chen, Xiaofei,Xiong, Fangjun,Chen, Wenxue,He, Qiuqin,Chen, Fener
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p. 2723 - 2728
(2014/04/17)
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- Synthesis of some impurities and/or degradation products of atorvastatin
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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.
- Stach, Jan,Havlicek, Jaroslav,Placek, Lukas,Radl, Stanislav
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p. 229 - 246
(2008/12/22)
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- Process for the production of atorvastatin calcium un amorphous form
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A process for the production of amorphous atorvastatin calcium and stabilized, amorphous atorvastatin calcium is provided.
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Page/Page column 16
(2010/11/30)
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- HMG-CoA reductase inhibitors and P-glycoprotein modulation
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1. Five 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins), (e.g. atorvastatin, fluvastatin, lovastatin, pravastatin and simvastatin), were investigated for their ability to reverse P-glycoprotein (P-gp) mediated rhodamine 123 (R123) transport in a murine monocytic leukaemia cell line that over-expresses the multi-drug resistance protein la/b (mdrla/lb). 2. P-gp modulation was studied by a fluorimetric assay and confocal microscopy by means of R123 efflux and uptake experiments, respectively. 3. Atorvastatin acid, methyl ester and lactone, lovastatin lactone and simvastatin lactone inhibited R123 transport in a concentration-dependent manner. Lovastatin acid, simvastatin acid, fluvastatin and pravastatin did not show a significant inhibition of the R123 transport in our cell system. Atorvastatin methyl ester and lactone showed the highest affinities for P-gp and results were comparable for both methods. 4. In conclusion, monitoring of R123 transport in living cells by confocal microscopy in addition to fluorimetric assay is a sensitive tool to study P-gp affinity in drug screening that is especially useful for early phases of drug development.
- Bogman, Katrijn,Peyer, Anne-Kathrin,Toeroek, Michael,Kuesters, Ernst,Drewe, Juergen
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p. 1183 - 1192
(2007/10/03)
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