CAS: 299-75-2; (2S,3S)-2,3-Dihydroxybutane-1,4-Diyl Dimethanesulfonate

该化合物是一种合成化合物,被归类为双功能烷基制剂,主要用于治疗某些癌症的化疗,特别是在干细胞移植之前的调节疗法中;其化学结构具有磺酸盐组,有助于其反应和形成与DNA交叉联系的能力,最终导致细胞死亡; 特雷苏尔硫丹以相对有利的安全特征而闻名,因为其与其他烷基制剂相比,它对正常组织毒性较低; 它一般是静脉注射,其特点是水溶性,便于其在临床环境中使用; 化合物在体内进行代谢转化,导致形成具有治疗作用的活性代谢物; 特雷苏尔硫丹的动作机制涉及形成DNA交叉联系,这破坏了快速分裂癌症细胞的复制和转录过程; 总的来说, 特雷苏尔是肿瘤学中的一个重要治疗选择,特别是对正在接受血压干细胞移植的病人而言.

结构式图片

欧盟法规

C&L通报REACH预注册

合成工艺路线路线简述

    📜2,2-二甲基-1,3-二氧戊环-4,5-二甲醇 (4S,5S)-4,5-二甲烷磺酸酯置于甲烷磺酸体系中,用 乙醇,水 用作溶剂,以85%的收率获得曲奥舒凡
    参考文献:2,2'-生物环氧乙烷的手性.
    标题:2,2'-生物环氧乙烷的手性.
    摘要:合成了2,2'-生物环氧乙烷的两种对映异构体,并通过旋光法,振动圆二色性(vcd)和拉曼光学活性(roa)在各种溶剂中彻底研究了它们的手性.在b3Lyp / Aug-Cc-Pvtz水平密度泛函理论(dft)计算显示三个构象(存在ģ +,G ^-,和顺式分别为51,44和5%吉布斯种群的分离的分子,) .两个主要的构象异构体的人口比例进行了修改为显示更高介电常数(溶剂ģ-形式降低,而g ^ +形式增加).通过使用可极化连续体模型(pcm),通过与时间有关的dft计算可以正确地再现特定溶剂在不同旋光度值下的行为,但对于苯,必须使用显式溶剂模型.最后,Vcd和roa光谱完全由dft / Pcm计算为玻尔兹曼平均再现ģ +和g ^-构象.
    Doi:10.1002/chir.22814

    海关参考信息

    专利信息


    专利号:US-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    专利号:US-8828984-B2
    优先权日:2012-11-19
    标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
    发明人:CHE CHI MING; ZOU TAOTAO
    权利人:UNIV HONG KONG; UNIV HONG KONG
    摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

    专利号:US-10577387-B1
    优先权日:2018-08-09
    标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
    发明人:CHE CHI MING; Fung Sin Ki; Chen tian feng
    权利人:UNIV HONG KONG
    摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

    专利号:US-8877171-B2
    优先权日:2010-02-03
    标 题 :Polyanionic multivalent macromolecules for intracellular targeting of proliferation and protein synthesis
    发明人:LICHA KAI; SCHIRNER MICHAEL; WELKER PIA; HAAG RAINER; WEINHART MARIE; PAULUS FLORIAN
    权利人:LICHA KAI; SCHIRNER MICHAEL; WELKER PIA; HAAG RAINER; WEINHART MARIE; PAULUS FLORIAN; MIVENION GMBH
    摘要:The present invention relates generally to methods and compositions for targeting of intracellular molecules involved in proliferation and protein synthesis of activated cells using polyanionic multivalent macromolecules. In particular aspect, multiple sulfate groups linked to polyol are specifically targeted to the cytoplasm and nucleus of proliferating and activated cells. The invention further comprises novel polyanionic macromolecular compounds and formulations.

    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.

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    主要参考文献


    1: Choudhary D, Sharma SK, Gupta N, Kharya G, Pavecha P, Handoo A, Setia R, Katewa S. Treosulfan-Thiotepa-Fludarabine-Based Conditioning Regimen for Allogeneic Transplantation in Patients with Thalassemia Major: A Single-Center Experience from North India. Biol Blood Marrow Transplant. 2012 Nov 15. doi:pii: S1083-8791(12)00480-6. 10.1016/j.bbmt.2012.11.007. [Epub ahead of print] doi: 10.1016/j.jpba.2012.10.005. Epub 2012 Oct 16. doi: 10.1016/j.clim.2012.10.003. Epub 2012 Oct 14. Review. doi: 10.1182/blood-2012-04-423822. Epub 2012 May 29. doi: 10.1007/s00432-012-1221-3. Epub 2012 Apr 15.
    8: Michallet M, Sobh M, Milpied N, Bay JO, Fürst S, Harousseau JL, Mohty M, Nicolini FE, Labussière H, Tedone N, Morisset S, Vigouroux S, Baumgart J, Tabrizi R, Blaise D. Phase II prospective study of treosulfan-based reduced-intensity conditioning in allogeneic HSCT for hematological malignancies from 10/10 HLA-identical unrelated donor. Ann Hematol. 2012 Aug;91(8):1289-97. doi: 10.1007/s00277-012-1429-y. Epub 2012 Feb 25. doi: 10.1038/bmt.2012.4. Epub 2012 Feb 13. doi: 10.1016/j.jpba.2011.12.021. Epub 2011 Dec 24. doi: 10.1038/bmt.2011.242. Epub 2011 Dec 12. doi: 10.1111/j.1600-0609.2011.01732.x. Epub 2011 Nov 22. doi: 10.3324/haematol.2011.043810. Epub 2011 Jun 9.
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    合成参考文献


    摘要:
    摘要:
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    摘要:https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/214759s000lbl.pdf
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