63095-51-2Relevant articles and documents
COMPOUND AND USE THEREOF IN SYNTHESIS OF BRIVARACETAM INTERMEDIATE AND CRUDE DRUG
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Page/Page column 0096-0100, (2021/08/27)
The present application provides a compound in formula III, and further provides a use of the compound in the synthesis of a Brivaracetam intermediate and a crude drug, and a synthesis method. A raw material involved in the method of the present application is low in costs and easily available; (R)-4-propyl-dihydrofuran-2-ketone having high optical purity can be prepared; complicated separation and purification steps are avoided; costs are reduced, and the method is more applicable to industrial production.
Preparation method of brivaracetam intermediate
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Paragraph 0025; 0070-0071, (2021/09/04)
The invention provides a preparation method of a brivaracetam intermediate (R)-3-propyl-gamma-butyrolactone, which comprises the following steps: by taking 4-chloro-4-oxobutyric acid methyl ester as a starting raw material, connecting a chiral auxiliary group, introducing R configuration propyl, removing a ligand, reducing carboxyl, and finally esterifying to form a ring, thereby obtaining the (R)-3-propyl-gamma-butyrolactone. The synthesis route ingeniously utilizes the chiral adjuvant (R)-4-benzyl-2-oxazolidinone, optimizes the reaction conditions, has the advantages of few reaction steps, high yield, good reaction stereoselectivity and the like, meanwhile, the raw materials are cheap and easy to obtain, the operation is simple, convenient and safe, and the method has a better industrial application prospect;.
Synthesis method of (R)-4-propyldihydrofuran-2-ketone
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Paragraph 0016; 0022; 0025-0026; 0027; 0030-0031, (2020/12/30)
The invention discloses a synthesis method of (R)-4-propyldihydrofuran-2-ketone, and belongs to the field of organic chemical synthesis. A new process route is developed to overcome the defects that (R)-4-propyldihydrofuran-2-ketone is relatively high in material price, low in product purity, difficult to produce and amplify and the like. Meldrum's acid and R-epichlorohydrin are used as initial raw materials, and the compound is obtained by taking (1S, 5R)-3-oxabicyclo [3.1. 0]-2-hexanone as an intermediate through a two-step reaction of closing a three-membered ring and opening a ring by using a Grignard reagent. The (R)-4-propyldihydrofuran-2-ketone is synthesized by adopting the synthesis method, a novel process route is adopted in the process, the total molar yield is greater than 50%,and the method has the characteristics of novel and short route, high optical purity, low cost and the like.