CAS: 5072-26-4; 2-Amino-4-(Butylsulfonimidoyl)Butanoic Acid

化学文摘社编号为5072-26-4-4,其特征是能够分解细胞内谷地内含谷地内含量,从而增加细胞内的氧化压力.这一特性使它成为研究的宝贵工具,特别是在癌症治疗,...

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    📜Tert-Butyl 4-(N-Acetyl-S-Butylsulfonimidoyl)-2-[(Tert-Butoxycarbonyl)Amino]Butanoate置于盐酸体系中,用 水 作为反应溶剂,化学反应 12.0H,以59%的收率获得产物丁硫胺酸亚砜胺(Bso)
    参考文献:蛋氨酸和丁硫氨酸亚砜肟:在温和且安全的亚胺化/氧化条件下的合成
    标题:蛋氨酸和丁硫氨酸亚砜肟:在温和且安全的亚胺化/氧化条件下的合成
    摘要:蛋氨酸和丁硫氨酸亚砜(mso和bso)是非天然氨基酸,已知会抑制谷胱甘肽(gsh)的生物合成.这些生物活性分子的当前合成涉及苛刻的反应条件和用于硫酰亚胺化的危险试剂的使用.在此,我们提出了改进的mso和bso合成方法,包括安全,温和的一锅式酰亚胺化/氧化顺序以及三种不同功能的一步脱保护.
    DOI:10.1002/adsc.201400354

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    专利信息


    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:US-8734846-B2
    优先权日:2008-06-16
    标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
    权利人:BIND BIOSCIENCES INC
    摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-8193180-B2
    优先权日:2007-01-24
    标 题 :N-amino tetrahydrothiazine derivatives, method of manufacture and use
    发明人:BRARD LAURENT; SINGH RAKESH KUMAR; KIM KYU KWANG; SAULNIER-SHOLLER GISELLE
    权利人:BRARD LAURENT; SINGH RAKESH KUMAR; KIM KYU KWANG; SAULNIER-SHOLLER GISELLE; WOMEN & INFANTS HOSPITAL
    摘要:This invention comprises the innovative synthesis of N-amino tetrahydrothiazine free bases and their salts. This invention further comprises the use of the derivatives and their therapeutic application as anticancer agents. Further this invention comprises their manufacture and use.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

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    主要参考文献


    1: Park MH, Kim SY, Moon C, Bae YC, Moon JI, Moon C. Differential cell death and Bcl-2 expression in the mouse retina after glutathione decrease by systemic D,L-buthionine sulphoximine administration. Mol Cells. 2013 Mar;35(3):235-42. doi: 10.1007/s10059-013-2276-y. Epub 2013 Feb 18.
    2: Vukovic V, Nicklee T, Hedley DW. Differential effects of buthionine sulphoximine in hypoxic and non-hypoxic regions of human cervical carcinoma xenografts. Radiother Oncol. 2001 Jul;60(1):69-73.
    13: Terradez P, Asensi M, Lasso de la Vega MC, Puertes IR, Viña J, Estrela JM. Depletion of tumour glutathione in vivo by buthionine sulphoximine: modulation by the rate of cellular proliferation and inhibition of cancer growth. Biochem J. 1993 Jun 1;292 ( Pt 2):477-83.

    合成参考文献


    参考文献:10.1007/s00232-011-9382-6
    摘要:Nazıroğlu M, Özgül C, Çiğ B, Doğan S, Uğuz AC. Glutathione Modulates Ca2+ Influx and Oxidative Toxicity Through TRPM2 Channel in Rat Dorsal Root Ganglion Neurons. The Journal of Membrane Biology. 2011 Jul 12;242(3):109. doi: 10.1007/s00232-011-9382-6.
    参考文献:10.1007/s10529-011-0684-7
    摘要:Upadhyaya CP, Venkatesh J, Gururani MA, Asnin L, Sharma K, Ajappala H, Park SW. Transgenic potato overproducing L-ascorbic acid resisted an increase in methylglyoxal under salinity stress via maintaining higher reduced glutathione level and glyoxalase enzyme activity. Biotechnol Lett. 2011 Nov;33(11):2297–307. doi: 10.1007/s10529-011-0684-7.
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