140235-34-3Relevant academic research and scientific papers
A PROCESS FOR THE PREPARATION OF 4-AMINO-2-HYDROXY-4-OXOBUTANOIC ACID AND PRODUCT PREPARED THEREFROM
-
Paragraph 0046, (2021/02/05)
A process for preparing 4-amino-2-hydroxy-4-oxobutanoic acid and intermediates thereof. The compound prepared by the present process is useful in management of diabetes. The present process yields 0.35gm, 63% of the desired compound. The structure of the compound prepared by the present process is confirmed by spectral data and its anti-diabetic potential is found to be at par with the herbal compound (FIIc), active anti-diabetic compound isolated from fruit pulp of Eugenia jambolana. The process of the present invention is simple, inexpensive, good yielding and can be easily adopted for commercial production with a high degree of consistency and reproducibility.
ALKYNYL ALCOHOLS AND METHODS OF USE
-
Page/Page column 402; 403, (2015/03/13)
The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over- activation of NF-kB signaling is observed.
Boric acid catalyzed chemoselective esterification of α- hydroxycarboxylic acids
Houston, Todd A.,Wilkinson, Brendan L.,Blanchfield, Joanne T.
, p. 679 - 681 (2007/10/03)
Boric acid catalyzes the selective esterification of α- hydroxycarboxylic acids without causing significant esterification to occur with other carboxylic acids. The procedure is simple, high-yielding, and applicable to the esterification of α-hydroxy carboxylates in the presence of other carboxylic acids including β-hydroxyacids within the same molecule.
Use of enantio-, chemo- and regioselectivity of acylase I. Resolution of polycarboxylic acid esters
Liljeblad, Arto,Aksela, Reijo,Kanerva, Liisa T.
, p. 2059 - 2066 (2007/10/03)
Acylase I was used to catalyze the enantioselective butanolysis of trimethyl 2-[(carboxymethyl)oxy]succinate (E=30) and N-carboxymethylaspartate (E=9) exclusively at the most sterically hindered of the three ester groups (the position α to the asymmetric centre). Gram-scale resolution allowed the preparation of the less reactive trimethyl (S)-2-[(carboxymethyl)oxy]succinate (96% e.e.), that of the (R)-butyldimethyl regioisomer (78% e.e.) at 55% conversion and finally the preparation of the corresponding trisodium carboxylate by saponification. Acylase I was shown to transform (±)-methyl N-acetylmethionine and (±)-valine to the corresponding (S)-amino acids through ester hydrolysis-N-acetyl transfer sequence with absolute chemo- and enantioselectivity. Butanolysis of methyl N-acetylmethionine stopped in the formation of the butyl ester (E=12), the valine derivative being totally unreactive.
MONOCYCLIC BETA-LACTAMS AND PROCESS FOR THE PREPARATION THEREOF
-
, (2008/06/13)
Monocyclic beta-lactam compounds represented by the formula STR1 wherein R 1 is H, NH 2, acylamino, C 1 -C 4 alkyl, etc.; R 2 is e.g. C 1 -C 4 alkyl, hydroxyalkyl, aminoalkyl, carboxy, esterified carboxy, esterified carboxyalkyl, or carboxyalkyl; and R 3 is hydrogen, benzyl, substituted benzyl, pivaloyl, --SO 3 M, or --P(C-O)(OM')2; are obtained by the cyclization of an O-substituted hydroxamate of a beta-substituted alkylcarboxylic acid. For example, alpha-ethylmalic acid monobenzyl ester is reacted with O-benzylhydroxylamine to form the O-benzylhydroxamate of the free carboxy group, and the hydroxamate is cyclized with diethyl diazodicarboxylate and triphenylphosphine to form the beta-lactam of the above formula wherein R 1 is ethyl, R 2 is benzyloxycarbonyl and R 3 is benzyl. The beta-lactam compounds are useful intermediates for preparing beta-lactamase inhibitors and monocyclic beta-lactam antibiotics and, when R 3 is --SO 3 M or -P(C-O)(OM')2 the compounds and salts thereof are antibacterial agents.
