123254-58-0Relevant articles and documents
A practical chemoenzymatic synthesis of (R)-isovaline based on the asymmetric hydrolysis of 2-ethyl-2-methyl-malonamide
Nojiri, Masutoshi,Yoshida, Fumi,Hirai, Yoshinori,Nishiyama, Akira,Yasohara, Yoshihiko
, p. 1 - 5 (2015)
(R)-Isovaline has potential applications in drug development, and therefore the development of an efficient method for the production of (R)-isovaline is desired. Herein we have investigated the asymmetric hydrolysis of 2-ethyl-2-methyl-malonamide into (S)-2-ethyl-2-methyl-malonamic acid, a useful synthetic intermediate in the production of (R)-isovaline, using CsAM, which is a recombinant amidase originally derived from Cupriavidus sp. KNK-J915. The produced (S)-2-ethyl-2-methyl-malonamic acid (98.6% ee) could be easily converted into (R)-isovaline by the Hofmann rearrangement. Starting from diethyl 2-methylmalonate, we obtained (R)-isovaline (99.1% ee) in 58.6% yield over eight steps, including the CsAM-catalyzed asymmetric hydrolysis of 2-ethyl-2-methyl-malonamide.
Compounds used as JAK inhibitor, and use of compounds
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Paragraph 0471; 0472; 0473, (2017/08/27)
The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.
Preparation and synthetic applications of (S)- and (R)-N-boc-N, O- isopropylidene-α-methylserinals: Asymmetric synthesis of (S)- and (R)-2- amino-2-methylbutanoic acids (Iva)
Avenoza, Alberto,Cativiela, Carlos,Corzana, Francisco,Peregrina, Jesus M.,Zurbano, Maria M.
, p. 8220 - 8225 (2007/10/03)
This report describes an efficient and convenient large-scale synthesis procedure for (S)- and (R)-N-Boc-α-methylserinal acetonides (3 and 4) starting from (R)-2-methylglycidol 5. The application of both of these compounds as valuable chiral building blocks in the asymmetric synthesis of α-methylamino acids is also demonstrated by the synthesis of (S)- and (R)- isovalines (Iva) (6 and 7).