220856-29-1Relevant academic research and scientific papers
Stereoselective chelate-controlled addition of Grignard reagents to unsaturated medium-ring heterocycles
Adams, Jeffrey A.,Heron, Nicola M.,Koss, Ann-Marie,Hoveyda, Amir H.
, p. 854 - 860 (1999)
Various medium-ring heterocycles, beating a C2-substituent that contains an accessible Lewis basic heteroatom, react with Grignard reagents with high levels of regio- and stereochemical control. The substrates can be prepared in the optically pure form by the Zr-catalyzed kinetic resolution; subsequent reaction with alkylmagnesium halides leads to the formation of optically pure alkylation products. The studies outlined herein probe the influence of the length and position of the heteroatom side chain on the facility and regio- and stereoselective outcome of the allylic substitution process. A catalytic procedure for the subsequent removal of the requisite heteroatom chelating group is presented.
Optically pure (R)-4-n-propyl-dihydrofuran-2(3H)-one preparation method
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, (2018/09/28)
The present invention relates to an optically pure (R)-4-n-propyl-dihydrofuran-2(3H)-one preparation method, wherein optically pure (S)-3-n-pentanoyl-4-substituted oxazole-2-one is used as a raw material, alkylation reaction with an olefin or alkyne reagent, reducing removal of a chiral auxiliary group, oxidation of double bond or triple bond and other steps are performed to prepare the opticallypure (R)-4-n-propyl-dihydrofuran-2(3H)-one. According to the present invention, the preparation method has characteristics of easily available raw material, low cost, high total yield, high optical purity of the obtained product, simple reaction conditions and simple operation process.
New preparation method of brivaracetam
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Paragraph 0139; 0140; 0141; 0142, (2018/11/04)
The present invention relates to a new preparation method of brivaracetam, According to the new preparation method, a chiral compound represented by a formula III and (S)-2-aminobutyramide or a salt thereof are subjected to a condensation reaction in the presence of a condensing agent to obtain a compound represented by a formula IV and having two chiral centers; a hydroxy protecting group R1 is removed to obtain a compound represented by a formula V; the compound represented by the formula V and a chlorinating reagent are subjected to a chlorinating reaction to obtain a compound represented by a formula VI; the compound represented by the formula VI is subjected to a substitution reaction in the presence of an alkaline agent, and ring closure is performed to obtain a formula I. Accordingto the present invention, the structure represented by the formula I contains two chiral centers, the intermediate compound represented by the formula IV has two chiral centers, and the chiral centersare not changed during a series of the reactions until the final product is generated; and with the method, the high optical purity brivaracetam can be directly obtained without the separation with the chiral chromatography, and the method is suitable for industrial production.
NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF
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, (2014/09/29)
The present invention relates to a compound of the Formula (I)): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, and hair loss.
MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES
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, (2014/01/08)
Provided are compounds of Formula I and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
