727382-14-1Relevant articles and documents
Chiral side chain of rosuvastatin calcium containing sulfone structure as well as preparation method and application of chiral side chain
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Paragraph 0034; 0036-0040, (2021/04/21)
The invention discloses a chiral side chain of rosuvastatin calcium containing a sulfone structure as well as preparation method and application of the chiral side chain. The chiral side chain D4-2 is prepared by taking D1-1 containing a thioether structure as a precursor; The D1-1 containing the thioether structure (Rz-S-) is synthesized through a brand-new process route and is further converted into a chiral side chain D4-2 containing the sulfone structure (Rz-SO2-), so that the separation and purification process of an intermediate is simplified; and after being modified by a sulfydryl-containing compound D1-M, the originally oily reaction intermediate is changed into a solid, so that the separation and purification effects of the intermediate are greatly improved. The chiral side chain D4-2 is used for preparing a high-grade intermediate R1 for synthesizing rosuvastatin calcium, the quality of R1 can be guaranteed, various indexes of the R1 product are excellent, and the cost is reduced; and the chiral side chain D4-2 is suitable for large-scale industrial production.
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.
Asymmetric ring opening of epoxides with cyanides catalysed by chiral binuclear titanium complexes
Maleev, Victor I.,Chusov, Denis A.,Yashkina, Lidiya V.,Ikonnikov, Nikolai S.,Il'In, Michail M.
, p. 838 - 843 (2014/06/23)
A series of Schiff bases obtained from salicylaldehydes and 3,3′-diformyl-BINOL were synthesized. The complexes of these Schiff bases with Ti(IV) were active for the asymmetric ring opening of epoxides with TMSCN. A mixture of unpurified ligands was found