专利号:US-2022298204-A1 优先权日:2019-07-05 标题 :Synthesis of a-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:EP-3792250-A1 优先权日:2019-09-13 标题:Synthesis of alpha-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:WO-9741093-A1 优先权日:1996-04-30 标 题:Methods for the synthesis of fmoc protected amines 发明人:BAER TED ALLEN; RAILLARD STEPHEN PETER 权利人:AFFYMAX TECH NV; BAER TED ALLEN; RAILLARD STEPHEN PETER 摘要:Methods for the synthesis of Fmoc-protected amines are provided. These methods involve the treatment of an amine component with a silylating agent and then an activated Fmoc-reagent. The methods can be conducted under anhydrous conditions.
专利号:US-9605019-B2 优先权日:2011-07-19 标 题:Methods for the synthesis of functionalized nucleic acids 发明人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL 权利人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL; WAVE LIFE SCIENCES LTD 摘要:The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.
专利号:EP-0135088-B1 优先权日:1983-08-13 标 题 :7-Amino-3[1-pyridiniomethyl]-8-oxo-5-oxa-1-azabicyclo[4.2.0]oct-2-en-2-carboxylates, process for their preparation and their use as intermediates in the synthesis of beta-lactam antibiotics 摘要:1. Compounds of the general formula (1) see diagramm : EP0135088,P12,F1 in which R represents hydrogen or methoxy, and X and Y, independently of one another, represent the following meanings : hydrogen ; halogen ; cyano ; hydroxyl ; C1 -C4 -alkoxy ; phenoxy ; amino, C1 -C4 -alkylamino, C1 -C4 -dialkylamino or C1 -C4 -alkanoylamino ; carboxyl ; C1 -C4 -alkanoyl ; benzoyl ; phenyl-C1 -C4 -alkanoyl ; C1 -C4 -alkoxycarbonyl ; sulphamoyl ; carbamoyl ; N-C1 -C4 -alkyl-, N,N-C1 -C4 -dialkyl- or N-C1 -C4 -alkoxycarbonylcarbamoyl ; allophanoyl and 4-C1 -C4 -alkylallophanoyl ; C1 -C4 -alkylsulphonyl ; C1 -C4 -alkylthio ; C1 -C6 -alkyl or alkenyl, C3 -C7 -cycloalkyl or cycloalkenyl, phenyl, heterocyclyl having 5- to 6-membered rings and 1 to 4 heteroatoms from the group comprising O, N and/or S, phenylalkyl or heterocyclylalkyl in the above mentioned meaning with 1 to 2 C atoms in the alkyl moiety, each of which is optionally substituted one or more times by hydroxyl, C1 -C4 -alkoxy, halogen, cyano, carboxyl and C1 -C4 -alkoxycarbonyl, C1 -C4 -alkanoyl, C1 -C4 -alkylsulphonyl or -sulphinyl, amino, or mono- or di-C1 -C4 -alkylamino, or C1 -C4 -alkoxyimino, excepting the radicals hydrogen-hydrogen, amino/hydrogen and carbamoyl/hydrogen ; or X and Y together represent a carbocyclic radical which is fused to the pyridine ring in 2.3 or 4.5 position and has 5 - 7 carbon atoms which are optionally replaced by O, S or N heteroatoms.
专利号:WO-2024146948-A1 优先权日:2023-01-05 标题:Peptide synthesis method involving sterically hindered tri-tert-butyl-tryptophan (tbt) residue 发明人:EKSTEEN JACOBUS JOHANNES; SVENDSEN JOHN SIGURD; MALMEDY FLORENCE; GUEVARA JONATHAN 权利人:AMICOAT AS 摘要:The invention is directed to a method of peptide synthesis comprising reacting a compound of Formula (I) or a salt thereof with a carbodiimide reagent to form an O-acylisourea intermediate; reacting the O-acylisourea intermediate with an additive to form an activated ester; and reacting the activated ester with an amino-containing moiety which is an amino acid, a peptide or a salt thereof comprising an amino group, wherein the amino group forms an amide bond with the carbonyl marked * in Formula (I); wherein the compound of Formula (I) has the structure: and wherein R1 and R2 are as defined in the disclosure. The invention is also directed to a compound of Formula (III) as defined in the disclosure or a salt thereof.
[参考文献]: Akiko Maehara, Et Al. Comparison Of Stent Expansion Guided By Optical Coherence Tomography Versus Intravascular Ultrasound: The Ilumien Ii Study (Observational Study Of Optical Coherence Tomography [参考文献]: Constanza E Fernández, Et Al. Effect Of The Probiotic Lactobacillus Rhamnosus Lb21 On The Cariogenicity Of Streptococcus Mutans Ua159 In A Dual-Species Biofilm Model. Caries Res. 2015;49(6):583-90. [参考文献]: Hannah L F Cooper, Et Al. Racialized Risk Environments In A Large Sample Of People Who Inject Drugs In The United States. Int J Drug Policy. 2016 Jan:27:43-55. [参考文献]: Hong Zhai, Et Al. Development Of Dual-Emission Ratiometric Probe-Based On Fluorescent Silica Nanoparticle And Cdte Quantum Dots For Determination Of Glucose In Beverages And Human Body Fluids. Food Chem. 2016 Aug 1:204:444-452. [参考文献]: Ming Yan, Et Al. Cytotoxicity Of Cdte Quantum Dots In Human Umbilical Vein Endothelial Cells: The Involvement Of Cellular Uptake And Induction Of Pro-Apoptotic Endoplasmic Reticulum Stress. Int J Nanomedicine. 2016 Feb 2:11:529-42.
合成参考文献
摘要:Spivey, A. C.; Diaper, C. M., Science of Synthesis, (2003) 5, 134. 摘要:Bailey, T. R., Science of Synthesis, (2005) 21, 815. 摘要:Bailey, T. R., Science of Synthesis, (2005) 21, 813.