877-95-2Relevant articles and documents
Alpha-carbonyl alkenyl ester compound as well as preparation method and application thereof
-
Paragraph 0450-0455, (2021/08/25)
The invention provides an alpha-carbonyl alkenyl ester compound and a preparation method thereof. The alpha-carbonyl alkenyl ester compound is also used for reacting with primary or secondary amine to prepare an amide compound. Two steps of reactions are combined to develop an amido bond and peptide bond forming method which takes carboxylic acid and amine as starting raw materials and allene ketone as a condensing agent. Meanwhile, the alpha-carbonyl alkenyl ester compound of the alpha-amino acid is used as a polypeptide synthesis building block for solid-phase synthesis of polypeptide. The method is mild in reaction condition, simple to operate and high in yield. Compared with an existing amido bond condensation reagent, allene ketone has the advantages of being easy and convenient to prepare, good in stability, small in molecular weight and free of racemization when alpha-chiral carboxylic acid is activated and the like. The compound is a novel amido bond and peptide bond condensation reagent.
New approach for induction of alkyl moiety to aliphatic amines by NaBH(OAc)3 with carboxylic acid
Tamura, Satoru,Sugawara, Aoi,Sato, Erika,Sato, Fuka,Sato, Keigo,Kawano, Tomikazu
supporting information, (2020/04/15)
We had found the novel N-alkylation method, which utilizes carboxylic acids as alkyl sources with sodium triacetoxyborohydride [NaBH(OAc)3]. Our methodology had been revealed to have some advantages over the reported similar procedures. Through
Styrene sulfone NLRP3 inflammasome inhibitor, preparation method and application thereof
-
Paragraph 0053; 0156-0157, (2020/10/30)
The invention relates to the field of styrene sulfone compounds and NLRP3 inhibitors, and particularly provides a styrene sulfone NLRP3 inflammasome inhibitor, a preparation method and application thereof, wherein the inhibitor is represented by a formula (1), n is selected from 0 and 1, X is selected from N and O, R1 is selected from different electron withdrawing or electron donating substituents, and R2 is selected from different fat or aromatic substituents. According to the invention, it is verified that the compounds represented by the general formula have NLRP3 inhibitory activity.