- Discovery of atorvastatin as a tetramer stabilizer of nuclear receptor RXRα through structure-based virtual screening
-
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
-
-
Read Online
- Method for synthesizing atorvastatin ester by using continuous flow tubular reactor
-
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.
- -
-
Paragraph 0035-0042; 0046-0048; 0051
(2022/03/27)
-
- Synthesis and evaluation of atorvastatin esters as prodrugs metabolically activated by human carboxylesterases
-
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
-
supporting information
p. 921 - 923
(2016/05/24)
-
- Enantioselective synthesis of allylboronates and allylic alcohols by copper-catalyzed 1,6-boration
-
Chiral secondary allylboronates are obtained in high enantioselectivities and 1,6:1,4 ratios by the copper-catalyzed 1,6-boration of electron-deficient dienes with bis(pinacolato)diboron (B2(pin)2). The reactions proceed efficiently using catalyst loadings as low as 0.0049 mol %. The allylboronates may be oxidized to the allylic alcohols, and can be used in stereoselective aldehyde allylborations. This process was applied to a concise synthesis of atorvastatin, in which the key 1,6-boration was performed using only a 0.02 mol % catalyst loading. 1,6-Borations of electron-deficient dienes with bis(pinacolato)diboron using copper catalyst loadings as low as 0.0049 mol % provided chiral allylboronates that, after oxidation, result in allylic alcohols in high enantioselectivities and 1,6:1,4 ratios. The allylboronates can also be used in stereoselective allylations of aldehydes. This process was applied to a concise synthesis of atorvastatin.
- Luo, Yunfei,Roy, Iain D.,Madec, Amael G. E.,Lam, Hon Wai
-
supporting information
p. 4186 - 4190
(2014/05/06)
-
- PROCESS FOR THE PREPARATION OF ATORVASTATIN
-
The present invention relates to a process for preparing the cholesterol biosynthesis inhibitor atorvastatin, (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- (phenylcarbamoyl)-lH-pyrrol-l-yl]-3,5-dihydroxyheptanoic acid calcium salt, which comprises
- -
-
Page/Page column 23
(2009/05/30)
-