Biocatalytic synthesis of atorvastatin intermediates
2009年12月1日 · Atorvastatin has a (3R,5S)-dihydroxyhexanoate side chain and synthesizing the intermediate for this side chain is challenging because it has two chiral centers, and greater than 99.5% e.e. and 99% d.e. are required [1].
Recent Advances in the Synthesis and Analysis of Atorvastatin …
This article focuses on the synthetic procedures of atorvastatin, including Paal-Knorr synthesis and several new synthetic strategies. It also outlines chemical and chemo-enzymatic methods for synthesizing optically active side chain of atorvastatin.
Recent Advances in the Synthesis and Analysis of Atorvastatin …
2023年10月11日 · Atorvastatin, a lipid-lowering drug that is widely used in the treatment of cardiovascular diseases, has significant clinical significance. This article focuses on the synthetic procedures of...
Atorvastatin (Lipitor) by MCR | ACS Medicinal Chemistry Letters
2019年2月7日 · A novel and efficient synthetic method of atorvastatin was described. The key step of the synthesis was the construction of the olefin linkage between the chiral side chain and skeleton via a Horner-Wadsworth-Emmons reaction, resulting in the advanced intermediate of atorvastatin under hydrogenation of the olefin over Pd/C.
[18F]Atorvastatin: synthesis of a potential molecular imaging tool …
The synthesis of the benzyl ether pyrrole intermediate 6, as well as the atorvastatin precursor 11, was performed by the treatment of the corresponding 1,4-diketone intermediates 4 and 10, respectively, with the commercially available primary amine 5 in a pivalic acid-catalyzed Paal-Knorr condensation reaction (Scheme 1).
An improved kilogram-scale preparation of atorvastatin calcium
The convenient and operationally simple conversion of an advanced intermediate of atorvastatin to the clinically used hemi-calcium salt form of the drug that is superior to the methods obtainable from the literature is now available to facilitate the production of …
Enhancing the biocatalytic manufacture of the key intermediate …
2017年2月6日 · During our development of an alternative, more efficient and economic route for chemo-enzymatic preparation of the intermediate of atorvastatin, we found that the HheC2360 previously reported...
Atorvastatin - StatPearls - NCBI Bookshelf
2020年9月25日 · In patients with dysbetalipoproteinemia, atorvastatin has been shown to decrease intermediate-density lipoprotein (IDL-C). Pharmacokinetics. The pharmacokinetic attributes of atorvastatin are covered below. Absorption Atorvastatin is rapidly absorbed after oral administration with a peak plasma concentration at 1 to 2 hours.
Atorvastatin - an overview | ScienceDirect Topics
The key advanced intermediate for atorvastatin, known as ATS8, 11, bears all of the requisite chiral functionality (Scheme 4). Codexis developed an integrated biocatalytic process to 11 leveraging four enzymes over three key steps.
Table 1, Statin Dosing and ACC/AHA Classification of Intensity
Statin Use for the Primary Prevention of Cardiovascular Disease in Adults: A Systematic Review for the U.S. Preventive Services Task Force [Internet]. From ACC/AHA, 2018. 199 Dosages shown are total daily dosages; exceptions are noted.