225377-55-9Relevant academic research and scientific papers
Preparation method of (R)-4-propyl-dihydrofuran-2-one and preparation intermediate of (R)-4-propyl-dihydrofuran-2-one
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Paragraph 0047; 0049, (2020/07/14)
The invention discloses a preparation method of (R)-4-propyl-dihydrofuran-2-one and a preparation intermediate of (R)-4-propyl-dihydrofuran-2-one. The preparation method of the intermediate comprisesthe following steps: (1) in the presence of an acid or an alkali, carrying out hydrolysis reaction on a compound I to obtain a compound II or a salt thereof; and (2) carrying out reduction reaction onthe compound II or the salt thereof and a reducing agent to obtain a compound III. According to the preparation route disclosed by the invention, the use of flammable and explosive reaction reagentsin the existing route is avoided; reagents which are low in cost and easy to obtain in industry are used; compared with the prior art, the method has the advantages of low cost, safety in production,realization of the purification and the separation of the intermediate by using the acid-base property of the compound and adopting the mode of adjusting the pH value of the system in the reaction process and the post-treatment operation, avoiding of recrystallization, filtration and other tedious operation modes, simplification of the operation, and suitableness for industrial large-scale production.
A (R)-4 - propyl - dihydrofuran -2 - ketone
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, (2019/04/10)
The invention discloses a process for preparing (R)- 4 - propyl - dihydrofuran - 2 - one method, the key intermediate type B compound, type C compound and its preparation method; (R)- 4 - propyl - dihydrofuran - 2 - one of the preparation method of the operability of the strong, is suitable for industrial production.
New synthesis method of brivaracetam
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Paragraph 0061; 0062; 0063, (2017/10/13)
The invention provides a synthesis method of brivaracetam. The method adopts cheap and easily available pentanoic acid or valeryl halide as an initial raw material, and provides a brand new synthesis route of a brivaracetam medicine, and the whole reaction route has a high total yield. The method has the advantages of high productivity, low cost, and suitableness for large-scale industrial production.
Method for preparing chiral 4-substituted dihydrofuran-2(3H)-ketone
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, (2017/06/02)
The invention provides a method for preparing chiral 4-substituted dihydrofuran-2(3H)-ketone. The method comprises the following steps: (a) dropwise adding acyl chloride (3) into an organic solvent solution of a compound (1), enabling reaction to obtain an acyl chloride intermediate solution, then dropwise adding an organic solvent solution of a compound (2) and enabling reaction to obtain a compound (4); (b) dropwise adding a bis(trimethylsilyl)amide alkali metal salt solution into an organic solvent solution of the compound (4), enabling reaction, dropwise adding a compound (5) into the obtained reaction liquid and enabling reaction to obtain a compound (6); (c) enabling reaction between the compound (6) and alkali to obtain a compound (7); (d) enabling reaction between the compound (7) and a reducing agent to obtain a compound (8), wherein R is selected from aryl, arylmethyl or alkyl, R1, R2 and R3 are independently selected from alkyl, and X is selected from Cl, Br or I. The method is simple in process, strong in operability and easy for industrial production. The reaction route is shown in the description.
Treatment of diseases using ICE inhibitors
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Page/Page column 13, (2008/06/13)
This invention relates to methods and compositions for treating autoinflammatory diseases. The invention also assays for evaluating the ability of an ICE inhibitor to treat autoinflammatory diseases.
Caspase inhibitors and uses thereof
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, (2008/06/13)
This invention provides compounds of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; next to R3 represents a single or double bond; Y is an elect
Discovery of non-peptidic P2-P3 butanediamide renin inhibitors with high oral efficacy
Simoneau, Bruno,Lavallee, Pierre,Anderson, Paul C.,Bailey, Murray,Bantle, Gary,Berthiaume, Sylvie,Chabot, Catherine,Fazal, Gulrez,Halmos, Ted,Ogilvie, William W.,Poupart, Marc-Andre,Thavonekham, Bounkham,Xin, Zhili,Thibeault, Diane,Boelger, Gordon,Panzenbeck, Maret,Winquist, Raymond,Jung, Grace L.
, p. 489 - 508 (2007/10/03)
A new series of non-peptidic renin inhibitors having a 2-substituted butanediamide moiety at the P2 and P3 positions has been identified. The optimized inhibitors have IC50 values of 0.8 to 1.4nM and 2.5 to 7.6nM in plasma renin assays at pH 6.0 and 7.4, respectively. When evaluated in the normotensive cynomolgus monkey model, two of the most potent inhibitors were orally active at a dose as low as 3mg/kg. These potent renin inhibitors are characterized by oral bioavailabilities of 40 and 89% in the cynomolgus monkey. Inhibitor 3z (BILA 2157 BS) was selected as candidate for pre-development. Copyright (C) 1999 Elsevier Science Ltd.
