CAS: 1072833-77-2; (R)-(1-(2-(2,5-Dichlorobenzamido)Acetamido)-3-Methylbutyl)Boronic Acid

上下游产品

2,5-dichlorobenzoic acid 2-[(2,5-dichlorobenzoyl)amino]acetic acid 2,5-dichloro-N-[2-({(1R)-3-methyl-1-[(3aS,4S,6S,7aR)-3a,5,5-trimethylhexa-hydro-2H-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl}amino)-2-oxoethyl]benzamide N-(fluoren-9-ylmethoxycarbonyl)glycine 2,2'-{2-[(1R)-1-({[(2,5-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]-5-oxo-1,3,2-dioxaborolane-4,4-diyl}diacetic acid 4-(carboxymethyl)-2-((R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dioxaborinane-4-carboxylic acid 2-chloro-5-chloro-N-[2-({(1R)-3-methyl-1-[(5R)-4-oxo-5-phenyl-1,3,2-dioxaborolan-2-yl]butyl}amino)-2-oxoethyl]benzamide

📜在 甲醇,Ammonium Hydroxide,异丁基硼酸,1-羟基苯并三唑体系中,用 正己烷,二氯甲烷 用作溶剂,化学反应 4.01H,反应生成艾沙佐米
参考文献:一种硼酸酯类化合物及其药学上可接受的盐,其制备方法及其用途
标题:一种硼酸酯类化合物及其药学上可接受的盐,其制备方法及其用途
摘要:如式(1)所示硼酸酯类化合物及其药学上可接受的盐,其制备方法及其用途,该硼酸酯类化合物结构新颖且具有抑制蛋白酶体功能.本发明的硼酸酯类化合物在溶液中的稳定性远远高于ixazomib.特别是在ph1.2和ph6.8时,本发明的化合物稳定性更有优势.此外,微粒体稳定性结果表明,本发明的化合物在5种不同肝微粒体具有较好的稳定性,而ixazomib在食蟹猴中的微粒体半衰期太长,药物基本不代谢,会引起严重的毒性,可用于在制备治疗炎症,免疫相关性疾病,癌症或者过度增殖性疾病,改变生物体中蛋白酶体产生的抗原肽的药物方面的用途.

专利信息

专利号:US-2025101045-A1
优先权日:2022-01-18
标题:Synthesis of boron-containing amidoxime reagents and their application to synthesize functionalized oxadiazole and quinazolinone derivatives
发明人：DAS BHASKAR
权利人:LONG ISLAND UNIV
摘要:The present disclosure is concerned with borylated amidoximes useful in the synthesis of biologically relevant drug-like molecules, including functionalized oxadizole and quinazolinone derivatives. Also disclosed are methods of making borylated amidoximes, methods of making functionalized oxadiazole and quinazolinone compounds using the amidoximes, and functionalized oxadiazole and quinazolinone compounds prepared from borylated amidoximes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-2023212216-A1
优先权日:2019-12-20
标 题:Synthesis of lactone derivatives and their use in the modification of proteins
发明人：MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH
权利人:GENIE BIOTECH UK LTD
摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:US-11542283-B2
优先权日:2018-05-28
标题 :Synthesis of peptide borate ester compound and use thereof
发明人：QIN YANRU
权利人:JIANGSU CHIA TAI FENGHAI PHARMACEUTICAL CO LTD
摘要:Provided are a peptide borate ester compound or a pharmaceutically acceptable salt thereof, a preparation method therefor, and pharmaceutical use thereof. The peptide borate ester compound or pharmaceutically acceptable salt thereof has a structure as shown in Formula (I), and is useful in the preparation of proteasome inhibitors to treat solid tumors and hematoma.

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.