CAS: 572924-54-0; (1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34As)-9,27-Dihydroxy-10,21-Dimethoxy-6,8,12,14,20,26-Hexamethyl-1,5,11,28,29-Pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34A-Tetracosahydro-3H-23,27-Epo

上下游产品

sirolimus dimethylphosphinic acid chloride 31-(triethylsilylether)rapamycin 31-(trimethylsilylether)rapamycin

31-(Triethylsilylether)Rapamycin置于3,5-二甲基吡啶,硫酸,水体系中,用 四氢呋喃,二氯甲烷 作为反应溶剂,化学反应 2.17H,反应生成 42-(二甲基亚膦酰)雷帕霉素
参考文献:Method For Preparing 42-(Dimethylphosphinate) Rapamycin
标题:Method For Preparing 42-(Dimethylphosphinate) Rapamycin
摘要:提供了一种制备42-(二甲基磷酸酯)雷帕霉素(利达福林)(i)的方法,具有高转化率和不产生31,42-双(二甲基磷酸酯)雷帕霉素(iii)的优点.在本发明的方法中,首先将雷帕霉素(II)与三乙基氯硅烷在碱性条件下反应,形成31,42-双(三乙基硅醚)雷帕霉素(iv-B),然后通过选择性去保护过程获得31-三乙基硅醚雷帕霉素(v-B).接下来,通过在碱性溶液中使用二甲基磷酸氯酯进行磷酸化反应得到粗产品.最后,通过在稀硫酸溶液中进行去保护反应得到利达福林(i)的粗产品.由于本发明方法的每个步骤的转化率均高于98%,表明该方法适用于工业生产.

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-2021220331-A1
优先权日:2016-05-03
标题:Inhibitors of ires-mediated protein synthesis
发明人：GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA
权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS
摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.

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-8722880-B2
优先权日:2012-08-22
标题:Method for preparing 42-(dimethylphosphinate) rapamycin
发明人：LEE KWANG-CHUNG; TUNG YEN-SHIH; LEE TZU-AI; SHIH YU-HSUAN
权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD; CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
摘要:A method for preparing 42-(dimethylphosphinate) Rapamycin (Ridaforolimus) (I) is provided, which has advantages of high conversion rate and no 31,42-bis(dimethyl phosphinate) Rapamycin (III) generated. In the method of the present invention, Rapamycin (II) is firstly reacted with triethyl chlorosilane in a base condition to form 31,42-bis(triethylsilylether) Rapamycin (IV-b), followed by a selective deprotection process to obtain 31-triethylsilylether Rapamycin (V-b). Next, a phosphorylation reaction is performed by using dimethylphosphinic chloride under a base solution to obtain a crude product. Finally, a deprotection reaction is performed in a diluted sulfuric acid solution to obtain a crude product of Ridaforolimus (I). Since the conversion rate of each step of the method of the present invention is higher than 98%, it indicates that the method of the present invention is suitable for industrial production.