专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:WO-9931124-A1 优先权日:1997-12-12 标 题:Cholic acid-based scaffolds for multidimensional molecular presentation of peptides 发明人:HOEEG-JENSEN THOMAS 权利人:NOVO NORDISK AS; HOEEG JENSEN THOMAS 摘要:A solid phase method for the synthesis of a plurality of differently substituted cholic acid scaffolds with a wide variety of peptide chain, pseudo-peptide chain or peptoid chain substitutents, as leads or compounds of potential therapeutic interest. The substituted cholic acids are prepared by initial solution synthesis of a scaffold holding amino acids with 3 orthogonal protecting groups. Subsequent solid-phase synthesis provides the build-up of the target molecules, either as discretes or in mixture. The molecules may be screened on the resin or cleaved from the resin and then screened in solution. The method disclosed here provides an easy and fast access to highly diverse compounds, potential peptide mimetics and potential leads for compounds of therapeutic interest. The method is amenable to automatization.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:WO-2024134682-A1 优先权日:2022-12-21 标题:(n-alkyldihydrol-2h-oxazinyl)-cannabidiol as anti-proliferative agent and process for preparation thereof 发明人:CHAM PANKAJ SINGH; SINGH AJEET; JAMWAL ASHIYA; SINGH RATTANDEEP; - SHABU; THAPA SONIA; WAZIR PRIYA; NANDI UTPAL; SINGH SHASHANK KUMAR; SINGH PARVINDER PAL 权利人:COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF S 摘要:The present invention relates to ring annulated analogues of cannabidiol where either one or both sides of the aromatic ring are attached to the oxazinyl ring, their method of preparation and use as anti-proliferative agents. The present invention provides a ring annulated cannabidiol analogue compound of Formula I. The present invention further provides a process for the synthesis of ring annulated cannabidiol analogue compound of Formula I.
专利号:US-6541653-B2 优先权日:2001-04-26 标题 :Synthesis of carbamate through low pressure heterogeneous oxidative carbonylation of amines 发明人:CHUANG STEVEN S C; CHI YAWU; CHEN BEI; TOOCHINDA PISANU 摘要:The process disclosed herein satisfies the need in the art for an industrially viable oxidative carbonylation catalytic system, and is capable of producing carbamates at a significantly higher rate than those processes reported in journal and patent literature. This reaction process takes place via a reaction mechanism that does not involve drastic conditions. Specifically, the catalytic system of the present invention employs Group VIII metal catalysts and/or copper-based catalysts with halide promoters to produce carbamates through heterogeneous oxidative carbonylation at atmospheric pressure and relatively non-drastic temperatures in a gas-solid carbonylation process.
专利号:US-7482492-B2 优先权日:2007-04-12 标 题 :Cost effective method for synthesis of triarylamine compounds 发明人:COGGAN JENNIFER A; HU NAN-XING 权利人:XEROX CORP 摘要:A process for forming a triarylamine compound includes reacting a halogenated aryl alcohol with an alcohol protecting agent and a first base to form a halogenated protected aryl alcohol compound, and reacting the halogenated protected aryl alcohol compound with an amine in the presence of a suitable catalyst and a second base.
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合成参考文献
参考文献:10.1007/s00894-011-1169-2 摘要:Singh DV, Adeppa K, Misra K. Mechanism of isoproturon resistance in Phalaris minor: in silico design, synthesis and testing of some novel herbicides for regaining sensitivity. Journal of Molecular Modeling. 2011 Jul 15;18(4):1431–45. doi: 10.1007/s00894-011-1169-2.