154026-95-6Relevant articles and documents
Rosuvastatin calcium intermediate, preparation method thereof and application of intermediate
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, (2019/04/17)
The invention discloses a rosuvastatin calcium intermediate, a preparation method thereof and an application of the intermediate. The synthesis process of the intermediate is environmentally friendly,simple and convenient to operate and low in EHS (environment health safety) risk, raw materials are easily available, and used chemical reagents are low in toxicity and low in price, so that the synthesis process of the intermediate is a green synthesis process suitable for industrial production. In addition, the intermediate is applied to synthesis of rosuvastatin calcium and key intermediates thereof, has short route and high yield, effectively reduces the industrial production cost of rosuvastatin calcium, and has a higher industrial application prospect.
Preparation method of rosuvastatin intermediate
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, (2018/10/11)
The invention discloses a preparation method of a rosuvastatin intermediate. The preparation method comprises the following steps: preparing a compound shown as a formula 2 into a compound shown as aformula 1 through ester formation, condensation, reduction and cyclization reactions. By the novel preparation method of the compound shown as the formula 1, the problems existing in the prior art aresolved, the product yield in a single step is increased, the product quality in the single step is improved and the production cost is greatly reduced; and the preparation method is suitable for industrialized large production.
Method for preparing 3,5-di-substituted hydroxyl-6-substituted capronate derivative
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Paragraph 0054; 0055; 0056; 0057; 0058; 0059; 0060; 0061, (2016/10/10)
The invention discloses a method for preparing a 3,5-di-substituted hydroxyl-6-substituted capronate derivative shown as a general formula I. The method comprises a step that carboxylate shown in a general formula II and RM are subjected to a reaction under effect of a cuprous salt catalyst. The method has the advantages that the process is simple, cost is low, a catalyst with expensive price can be avoided, generation of a by-product is reduced, the post-treatment is simple, operation is easy, reaction yield is greatly increased, and the method is more suitable for large-scale industrial production.
Method for synthesizing ADA
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Paragraph 0081; 0082; 0095; 0096; 0097; 0114, (2018/02/04)
The invention relates to a compound synthesized in the medicine field, and particularly relates to a rosuvastatin intermediate. The method for synthesizing ADA comprises the following five steps: 1, reacting S-4-chloro-3-hydroxy butyronitrile with hexamethyl-disilazane to generate an intermediate I; 2, reacting the prepared intermediate I, a reducing agent and methanesulfonic acid with tert-butyl bromoacetate to prepare an intermediate II; 3, preparing an intermediate III from the prepared intermediate II by enzyme selective reduction; 4, reacting the prepared intermediate III with acetone acetal to prepare an intermediate IV; and 5, reacting the prepared intermediate IV and tetrabutylammonium bromide with sodium acetate to prepare the target intermediate ADA. According to the method, operation for preparing ADA is more convenient; and the method has high safety coefficient and low cost, and is very suitable for industrial production.
New Statin intermediate, the preparation of the same and the preparation of Rosuvastatin using the same
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Paragraph 0161; 0162-0165, (2017/04/20)
The present invention provides a novel producing method for producing a core intermediate (chemical formula IV) of rosuvastatin, a novel intermediate used therefor and a producing method of rosuvastatin hemi-calcium salts using the same. The novel intermediate of the present invention can be prepared with high purity and in high yields in mild conditions, and thus the rosuvastatin intermediate and rosuvastatin hemi-calcium salts can be conveniently and efficiently mass-produced without complicated processes.
Stereoselective reduction of δ-hydroxy β-ketoesters to syndiol in achiral micellar system
Roy, Bhairab Nath,Singh, Girij Pal,Lathi, Piyush Suresh,Agrawal, Manoj K,Mitra, Rangan
, p. 1247 - 1251 (2015/11/24)
A novel, efficient and stereo-selective process for synthesis of statin side chain, a key intermediate for statin type cholesterol lowering drugs such as Lipitor (atorvastatin) and Crestor (rosuvastatin) in achiral micellar media is reported. The key feature of this process is sodium borohydride reduction of δ-hydroxy β-ketoester in achiral micellar system in 92% de, thereby avoiding metal chelation methods which employ triakylborane, titanium (IV) isopropoxide or cerium (III) chloride prior to reduction.
A NOVEL, GREEN AND COST EFFECTIVE PROCESS FOR SYNTHESIS OF TERT-BUTYL (3R,5S)-6-OXO-3,5-DIHYDROXY-3,5-O-ISOPROPYLIDENE-HEXANOATE
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Page/Page column 44, (2015/01/07)
The present invention provides a process of preparation of an intermediate useful for the preparation of statins more particularly the present invention relates to an eco-friendly and cost effective process for the preparation of tert -butyl (3R,5S)-6-oxo-3,5-dihydroxy- 3,5-O-isopropylidene-hexanoate [I].
Ru-catalyzed asymmetric hydrogenation of γ-heteroatom substituted β-keto esters
Fan, Weizheng,Li, Wanfang,Ma, Xin,Tao, Xiaoming,Li, Xiaoming,Yao, Ying,Xie, Xiaomin,Zhang, Zhaoguo
experimental part, p. 9444 - 9451 (2012/01/13)
A series of enantiomerically pure γ-heteroatom substituted β-hydroxy esters were synthesized with high enantioselectivities (up to 99.1% ee) by hydrogenation of γ-heteroatom substituted β-keto esters in the presence of Ru-(S)-SunPhos catalyst. These asymmetric hydrogenations provide key building blocks for a variety of naturally occurring and biologically active compounds.
Process for the preparation of dihydroxy esters and derivatives thereof
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, (2008/06/13)
A process is provided for the preparation of a compound of formula (1) wherein R and R′ represent optionally substituted hydrocarbyl groups and X represents a hydrocarbyl linking group. The process comprises either the stereoselective reduction of the keto group in a dihydroxy keto precursor followed by selective esterification of a primary hydroxy, or selective esterification of a primary hydroxy of a dihydroxy keto precursor followed by stereoselective reduction of the keto group.
