CAS: 179324-87-9; (R)-3-Methyl-1-((3As,4S,6S,7Ar)-3A,5,5-Trimethylhexahydro-4,6-Methanobenzo[d][1,3,2]Dioxaborol-2-yl)Butan-1-Amine 2,2,2-Trifluoroacetate

上下游产品

(1S)-(S)-pinanediol 1-bis(trimethylsilyl)amino-3-methylbutane-1-boronate trifluoroacetic acid 1,1,1-trimethyl-N-{(1R)-3-methyl-1-[(3aS,4S,6S,7aR)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl}-N-(trimethylsilyl)silanamine 2-(2-methylpropyl)-(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborole velcade N-[(1S)-1[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-2-benzyl]2-pyrazine carboxamide

(1S,2S,3R,5S)-(+)-2,3-蒎烷二醇置于正丁基锂,Zinc(II) Chloride,Lithium Hexamethyldisilazane体系中,用 四氢呋喃 用作溶剂,化学反应 6.25H,反应生成(Ar,3As,4S,6S,7Ar)-六氢-3A,8,8-三甲基-Alpha-(2-甲基丙基)-4,6-甲桥-1,3,2-苯并二氧硼烷-2-甲胺 2,2,2-三氟乙酸盐
参考文献:肽类蛋白酶体抑制剂的系统比较突出显示了α-酮酰胺亲电试剂是一种可逆的可逆铅基序.
标题:肽类蛋白酶体抑制剂的系统比较突出显示了α-酮酰胺亲电试剂是一种可逆的可逆铅基序.
摘要:遍在蛋白-蛋白酶体系统(ups)已被学术界和制药业成功地靶向用于肿瘤学和免疫学领域.典型的蛋白酶体抑制剂基于肽骨架,该肽骨架具有亲电的c末端,通过它们可与活性蛋白水解位点发生反应.尽管肽部分在亚基选择性方面引起了广泛关注,但化合物的靶标特异性和生物稳定性在很大程度上由反应性战斗部决定.在这项研究中,我们已经通过结合体外,体内和结构方法对亲电子试剂进行了系统的研究,以揭示功能和化学反应性改变的含义.从而,
Doi:10.1002/anie.201308984

专利信息

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.

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优先权日:2004-03-30
标题 :Synthesis of boronic ester and acid compounds

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优先权日:2004-03-30
标 题:Synthesis of boronic ester and acid compounds

专利号:US-2020157143-A1
优先权日:2004-03-30
标题 :Synthesis of boronic ester and acid compounds

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优先权日:2004-03-30
标 题 :Synthesis of boronic ester and acid compounds

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优先权日:2004-03-30
标题:Synthesis of boronic ester and acid compounds