Facile Syntheses of Oxazolines and Thiazolines with <i>N</i>-Acylbenzotriazoles under Microwave Irradiation
作者:Alan R. Katritzky、Chunming Cai、Kazuyuki Suzuki、Sandeep K. Singh
DOI:10.1021/jo0355092
日期:2004.2.1
Microwave reactions of 2-amino-2-methyl-1-propanol (2) or 2-aminoethanethiol hydrochloride (4) with readily available N-acylbenzotriazoles 1a−j in the presence of SOCl2 produced 2-substituted 2-oxazolines 3a−j in 84−98% yields and 2-substituted thiazolines 5a−i in 85−97% yields, respectively. With use of this method chiral oxazoline 6, bisoxazoline 7, bisthiazoline 8, and 5,6-dihydro-4H-1,3-oxazines
在SOCl 2的存在下,2-氨基-2-甲基-1-丙醇(2)或2-氨基乙硫醇盐酸盐(4)与易于获得的N-酰基苯并三唑1a - j的微波反应产生了2-取代的2-恶唑啉3a - j分别以84-98%的产率和2-取代的噻唑啉5a - i的产率为85-97%。使用该方法时,手性恶唑啉6,双恶唑啉7,双噻唑啉8和5,6-二氢-4 H -1,3-恶嗪9或10还制备了82-96%的产率。这些结果证明了N-酰基苯并三唑在温和条件下和微波辐射下反应时间短的情况下在恶唑啉和噻唑啉制备中的新应用。
Straightforward microwave-assisted synthesis of 2-thiazolines using Lawesson's reagent under solvent-free conditions
作者:Julio A. Seijas、M. Pilar Vázquez-Tato、José Crecente-Campo
DOI:10.1016/j.tet.2008.07.027
日期:2008.9
2-Thiazolines are synthesized from carboxylic acids and 1,2-aminoalcohols in the presence of Lawesson's reagent under solventless conditions. The developed method is valid for either substituted or unsubstituted aminoalcohols and a wide variety of aromatic, heteroaromatic and aliphatic carboxylic acids; thus it constitutes a general synthetic method for these kinds of compounds. The role of Lawesson's
A straightforward metal-free synthesis of 2-substituted thiazolines in air
作者:Michael Trose、Faïma Lazreg、Mathieu Lesieur、Catherine S. J. Cazin
DOI:10.1039/c5gc00286a
日期:——
A range of 2-substituted 4,5-dihydrothiazoles was easily synthesised from the reaction of nitriles with cysteamine in the presence of a catalytic amount of NaOH.
一系列2-取代的4,5-二氢噻唑易于在催化剂量的NaOH存在下,通过腈与半胱氨酸的反应合成。
Peptide compound and method for producing same, composition for screening use, and method for selecting peptide compound
申请人:FUJIFILM Corporation
公开号:US11319347B2
公开(公告)日:2022-05-03
An object of the present invention is to provide a novel cyclic peptide compound excellent in cell membrane permeability, a method for producing the same, a composition for screening use, and a method for selecting a cyclic peptide compound that binds to a target substance. According to the present invention, a peptide compound represented by Formula (1) or a salt thereof is provided. In the formula, the symbols have the meanings as defined in the specification of the present application.