CAS: 14337-43-0; Ethyl 2-Chloro-2-(Hydroxyimino)Acetate

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30673-27-9 73188-60-0

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甘氨酸乙酯盐酸盐置于sodium Nitrite体系中,化学反应生成氯代肟基乙酸乙酯
参考文献:亚硝基羰基杂diels-Alder环加合物向有用的异恶唑啉-碳环氨基的转化
标题:亚硝基羰基杂diels-Alder环加合物向有用的异恶唑啉-碳环氨基的转化
摘要:详细介绍了一种用于合成异恶唑啉-碳环核苷的有用前体的新方法,该方法从易于获得的n-苯甲酰基-2,3-氧杂氮杂硼烷-5-烯开始,并通过1,3-双极性环加成反应引入更多的极性和亲水性官能团由相应的羟肟基氯生成的或更方便地通过与硝基乙酸乙酯催化缩合生成的碳乙氧基甲腈氧化物.
Doi:10.1016/j.Tet.2009.10.062

专利信息

专利号:WO-2022156692-A1
优先权日:2021-01-22
标 题 :Cyclic peptide viral protease inhibitor, preparation method therefor, and application thereof in antiviral drugs
发明人：LI XINGZHOU; XU LEI; LI SONG; ZHONG WU; CAO RUIYUAN; XIAO JUNHAI; ZHOU XINBO; ZHENG ZHIBING; LI WEI; FAN SHIYONG; XIAO DIAN; WANG ZIHAO; XIE FEI
权利人:ACAD OF MILITARY MEDICAL SCIENCES
摘要:The present invention relates to the field of pharmaceutical chemicals, relates to a cyclic peptide compound as shown in formula M or a stereoisomer, a tautomer or a mixture of the compound, a pharmaceutically acceptable salt, a polymorph, a eutectic or a solvate of the compound, or a stable isotope derivative, a metabolite or a prodrug of the compound, and further relates to a method and an intermediate for synthesis of the cyclic peptide compound. The provided cyclic peptide compound has a strong inhibitory effect on 3CL protease of coronavirus and 3CL protease of picornaviridae, such as Enterovirus EV71 virus. By means of cell level activity testing, the provided cyclic peptide compound has a significant inhibitory effect on EV71 virus and coronavirus. Moreover, the cyclic peptide compound as shown in formula M can generate a virus inhibition effect on a cell level by inhibiting viral protease activity, and has a good application prospect in antiviral drugs.

专利号:US-10858390-B2
优先权日:2016-09-02
标 题 :Use of excess carbodiimide for peptide synthesis at elevated temperatures
发明人：COLLINS JONATHAN M; SINGH SANDEEP K
权利人:CEM CORP
摘要:An improved method of coupling amino acids into peptides or peptidomimetics is disclosed in which the activation and coupling are carried out in the same vessel, in the presence of a carbodiimide in an amount greater than 1 equivalent as compared to the amino acid, in the presence of an activator additive, and at a temperature greater than 30° C.

专利号:US-3862225-A
优先权日:1961-08-18
标 题:D-ring substituted tetracyclines
发明人：CONOVER LLOYD H; WOODWARD ROBERT B
权利人:PFIZER
摘要:The total synthesis of tetracycline-type antibiotics by a multistep process beginning with 3,4,10-trioxo-1,2,3,4,4a,9,9a, 10-octahydroanthracenes comprising: (1) an aldol condensation with a glyoxalic acid ester to give a 2-carboxymethylidene3,4,10-trioxo-1,2,3,4,4a,9,9a,10-octahydroanthracene ester; (2) Michael reaction of said ester with an amine to produce 3,4,10trioxo-1,2,3,4,4a,9,9a,10-octahydroanthracene-2-( Alpha amino)acetic acid ester; (3) conversion of the triketone to the corresponding 4,10-diketone by (a) selective reduction of the Michael reaction product to the corresponding 3-hydroxy compound, followed by conversion of the 3-hydroxy compound to the corresponding 3-formyloxy compound and removal of the 3-formyloxy group by treatment with zinc dust to give a 4,10-dioxo1,2,3,4,4a,9,9a,10-octahydroanthracene-2-( Alpha -amino)acetic acid ester; or (b) conversion of the hydrochloride salt of the Michael reaction product to a lactone by reaction with ptoluenesulfonic acid and treatment of the lactone with zinc dust formic acid; (4) conversion of the 4,10-diketo-1,2,3,4,4a,9,9a, 10-octahydroanthracene-2-( Alpha -amino)-acetic acid to a mixed anhydride; (5) followed by acylation of a malonic acid ester with the mixed anhydride; (6) cyclization of the acyl malonate derivative to a 12a-deoxytetracycline which is then hydroxylated to a tetracycline. The preparation of the 3,4,10-trioxo1,2,3,4,4a,9,9a,10-octahydroanthracenes from benzoyl halides by (a) Friedel-Crafts reaction of a benzoyl halide with a pyrocatechol ether, e.g., a di-(lower)alkyl ether, to produce a 3,4-di-(lower)alkoxybenzophenone; (b) conversion of the benzophenone by partial or complete reduction of the carbonyl group by chemical or catalytic methods to a 3,4-di-(lower)alkoxy diphenyl methanol or 3,4-di-(lower)alkoxy diphenyl methane; or to a 3,4-di-(lower)alkoxy diphenyl alkane via a Grignard reaction and reduction of the thus-produced alkanol; (c) oxidation of the 3,4-di-(lower)alkoxy diphenyl alkane, or the corresponding dihydroxy compound, to a dienedioic acid ester or dienedioic acid; (d) hydrogenation of the dienedioic acid compound to a benzyl adipic acid derivative; (e) cyclization of said compound to a 2-(2-carbalkoxyethyl)-4-tetralone by means of dehydrating or dehydrohalogenating agents; (f) cyclization of the 4-tetralone derivatives by condensation with a dialkyloxalate to give a 2carbalkoxy 3,4,10-trioxo-octahydroanthracene; and (g) removal of the 2-substituent by decarboxylation. The intermediates and final products are useful as bactericides and/or chelating agents.

专利号:US-10393752-B2
优先权日:2011-05-14
标 题:Mass spectrometry-cleavable cross-linking agents
发明人：RYCHNOVSKY SCOTT D; HUANG LAN
权利人:UNIV CALIFORNIA
摘要:Provided herein is synthesis of novel mass spectrometry-cleavable cross-linking agents. The novel mass spectrometry-cleavable cross-linking agents can be used in mass spectrometry, tandem mass spectrometry, and multi-stage tandem mass spectrometry to facilitate structural analysis of intra-protein interactions in proteins and inter-protein interactions in protein complexes. Also provided are methods of mapping intra-protein interactions in proteins and inter-protein interactions in protein complexes.

专利号:US-10308677-B2
优先权日:2014-12-19
标题:Coupling method for peptide synthesis at elevated temperatures
发明人：COLLINS JONATHAN M; SINGH SANDEEP KUMAR
权利人:CEM CORP
摘要:An improved method for coupling carboxylic acids and amines is disclosed that includes the steps of combining a hyper-acid sensitive linker connecting an amine and a resin, a carboxylic acid, a carbodiimide, an activator additive, and a base, and carrying out the activation and coupling at a temperature greater than 30° C.

专利号:CA-2977720-A1
优先权日:2016-09-02
标题 :Use of excess carbodiimide for peptide synthesis at elevated temperatures