专利号:US-11161827-B2 优先权日:2019-04-05 标 题 :Catalytic systems for stereoselective synthesis of chiral amines by enantiodivergent radical C—H amination 发明人:Zhang xiao-xiang; Lang kai 权利人:TRUSTEES BOSTON COLLEGE; THE TRUSTEES OF BOSTON COLLEGE 摘要:In one aspect, the disclosure relates to a mode of asymmetric induction in radical processes based on sequential combination of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution. Also disclosed is an asymmetric system for stereoselective synthesis of strained 5-membered cyclic sulfamides via radical 1,5-C—H amination of sulfamoyl azides. The disclosed metalloradical system can control the degree and sense of asymmetric induction in the catalytic radical C—H amination in a systematic manner. The disclosed system is applicable to a broad scope of substrates with different types of C(sp 3 )—H bonds and exhibits reactivity and selectivity, providing access to both enantiomers of useful 5-membered cyclic sulfamides in a highly enantioenriched form. Also disclosed are catalysts useful in these processes. 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 disclosure.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-8975340-B2 优先权日:2010-12-15 标题 :Synthesis of sequestration resins for water treatment in light water reactors 发明人:YENGOYAN LEON; FRATTINI PAUL L; WELLS DANIEL MORGAN 权利人:YENGOYAN LEON; FRATTINI PAUL L; WELLS DANIEL MORGAN; ELECTRIC POWER RES INST 摘要:An organic synthesis of materials to achieve removal of low molecular weight ionic species, such as transition metal ions including cobalt, iron, nickel, and zinc, from aqueous solutions. The synthesis includes the steps of providing a cation exchange resin, functionalizing the cation exchange resin using a chloride intermediate to form a sulfonyl chloride resin, and reacting a multi-amine based ligand with the sulfonyl chloride resin to form a sequestration resin. The synthesis further includes the steps of cooling the sequestration resin, and washing and drying the sequestration resin.
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
[参考文献]: Alessandra Cincinelli, Et Al. Purification And Inhibition Studies With Anions And Sulfonamides Of An α-Carbonic Anhydrase From The Antarctic Seal Leptonychotes Weddellii. Bioorg Med Chem. 2011 Mar 15;19(6):1847-51. [参考文献]: Alessio Innocenti, Et Al. Carbonic Anhydrase Inhibitors. Inhibition Of Isozymes I, Ii, Iv, V, And Ix With Anions Isosteric And Isoelectronic With Sulfate, Nitrate, And Carbonate. Bioorg Med Chem Lett. 2005 Feb 1;15(3):567-71. [参考文献]: Anna Ohradanova, Et Al. Anion Inhibition Studies Of An α-Carbonic Anhydrase From The Living Fossil Astrosclera Willeyana. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1314-6. [参考文献]: Anthony Bertucci, Et Al. Carbonic Anhydrase Inhibitors. Inhibition Studies With Anions And Sulfonamides Of A New Cytosolic Enzyme From The Scleractinian Coral Stylophora Pistillata. Bioorg Med Chem Lett. 2011 Jan 15;21(2):710-4. [参考文献]: Daniela Vullo, Et Al. Carbonic Anhydrase Inhibitors: Inhibition Of The Cytosolic Human Isozyme Vii With Anions. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3139-43.
合成参考文献
参考文献:10.2165/11532540-000000000-00000 摘要:Paquet P, Piérard GE. New insights in toxic epidermal necrolysis (Lyell's syndrome): clinical considerations, pathobiology and targeted treatments revisited. Drug Saf. 2010 Mar 01;33(3):189–212. doi: 10.2165/11532540-000000000-00000. 参考文献:10.2165/11592070-000000000-00000 摘要:Watkins CC, Pieper AA, Treisman GJ. Safety considerations in drug treatment of depression in HIV-positive patients: an updated review. Drug Saf. 2011 Aug 01;34(8):623–39. doi: 10.2165/11592070-000000000-00000. 参考文献:10.1186/1471-2334-11-194 摘要:Kuntz JL, Chrischilles EA, Pendergast JF, Herwaldt LA, Polgreen PM. Incidence of and risk factors for community-associated Clostridium difficile infection: A nested case-control study. BMC Infectious Diseases. 2011 Jul 15;11(1):194. doi: 10.1186/1471-2334-11-194.