121660-37-5Relevant articles and documents
Preparation method of pitavastatin calcium intermediate
-
Paragraph 0044; 0046; 0048; 0050; 0052; 0054, (2020/02/14)
The invention belongs to the field of drug synthesis, and particularly relates to a preparation method of a pitavastatin calcium intermediate. The preparation method comprises the following steps: 1,carrying out a chemical reaction on a compound II and triphenylphosphine at a temperature of 10-150 DEG C to prepare a compound III; 2, in the presence of triethylamine, with oxalyl chloride and dimethyl sulfoxide as oxidants, subjecting a compound IV to a chemical reaction to prepare a compound V; and 3, subjecting the compound III and the compound V to a chemical reaction at 20-150 DEG C in thepresence of a basic catalyst so as to prepare a compound I. The intermediate prepared by using the method provided by the invention has the advantages of easy availability of raw materials, simple operation, high yield and high purity. The specific synthetic route of the method is shown in the specification.
Substrate stereocontrol in bromine-induced intermolecular cyclization: Asymmetric synthesis of pitavastatin calcium
Chen, Weiqi,Xiong, Fangjun,Liu, Qian,Xu, Lingjun,Wu, Yan,Chen, Fener
, p. 4730 - 4737 (2015/07/27)
A novel approach to synthesize pitavastatin calcium (1), an effective HMG-CoA reductase inhibitor, based on readily available and attractively functionalized (R)-3-chloro-1,2-propanediol is reported. This work highlights an intermolecular diastereoselective bromine-induced cyclization of homoallylic carbonate to meet stereochemical challenges in the synthesis of statins. An efficient route to a new triphenylphosphonium tetrafluoroborate salt of a quinoline core is also presented.
PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES FOR THE SYNTHESIS OF STATINS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
-
, (2012/02/13)
The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.