17137-11-0Relevant articles and documents
Regioselective β-Csp3-Arylation of β-Alanine: An Approach for the Exclusive Synthesis of Diverse β-Aryl-β-amino Acids
Chowdhury, Sushobhan,Vaishnav, Roopal,Panwar, Namita,Haq, Wahajul
, p. 2512 - 2522 (2019)
An approach for the synthesis of a variety of new β-aryl-β-amino acids has been developed via a palladium-catalyzed auxiliary-directed regioselective Csp3-H arylation of the unactivated β-methylene bond of β-alanine. The use of 8-aminoquinoline amide as an auxiliary efficiently directs the desired regioselective β-Csp3-H functionalization. The developed protocol enables the easy and straightforward access to several high-value β-aryl-β-amino acids useful for peptide engineering, starting from inexpensive and readily available β-alanine precursors in moderate to excellent yields.
Perfluorinated markers for hypoxia detection: Synthesis of sulfur-containing precursors and [18F]-labelling
Cheguillaume, Arnaud,Gillart, Jacques,Labar, Daniel,Gregoire, Vincent,Marchand-Brynaert, Jacqueline
, p. 1357 - 1367 (2005)
Synthetic pathways of two novel sulfurated precursors for [ 18F]-labelling by oxidative fluorodesulfurization reaction are described. A three-step sequence starting from N-phthalimido-β-alanine allows the preparation of a new trithioorthoester as valuable precursor of the synthesis of [18F]-3,3,3-trifluoropropylamine, a convenient radiolabelled intermediate for [18F]-EF3. A five-step sequence for the preparation of methyl 4-phthalimido-2,2-difluoropropanedithioate from ethyl 2,2-difluoropropanoate, via the key conversion step of α,α′- difluorothioamidate to the corresponding α,α′- difluorodithioester, and the first results of its use as precursor for oxidative fluorodesulfurization in [18F]-radiochemistry are also presented.
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Saburi et al.
, p. 427,428 (1972)
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Quinazolinyl carboxylic ester derivative containing isoindolone group and application thereof
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Paragraph 0056-0058; 0062-0064, (2021/01/04)
The invention discloses a quinazolinyl carboxylic ester derivative containing an isoindolone group, and the derivative has a structural general formula shown as the specification, wherein R is aryl substituted alkyl, aryl substituted cyclolky or biaryl. According to the invention, the novel isoindolone group-containing quinazolinyl carboxylic ester derivative is synthesized, can effectively inhibit the growth of antibiotic-sensitive or drug-resistant bacteria, and has a new action mechanism.
A Convenient One-Pot Synthesis of 1,5-Disubstituted Tetrazoles Containing an Amino or a Carboxy Group
Obushak, M. D.,Pokhodylo, N. T.,Shyyka, O. Ya.
, p. 802 - 812 (2020/07/03)
Abstract: A convenient method is proposed for constructing the tetrazole ring by a one-pot reaction of amides with phosphorus oxychloride and sodium azide. A series of 1,5-disubstituted tetrazoles containing an amino or a carboxy group, which present interest as buildings blocks for the synthesis of biologically active substances, were obtained.