专利号:WO-2025053792-A1 优先权日:2023-09-06 标题:Collective synthesis of phantomolin family through total synthesis of the sesquiterpene lactone molephantin 发明人:CHIBA SHUNSUKE; PATOURET REMI HENRI LOUIS; LI HOI YEUNG; LAI SOAK KUAN 权利人:UNIV NANYANG TECH 摘要:Disclosed herein are processes to generate an intermediate in the total synthesis of (+)- molephantin or a derivative thereof, and a total synthesis of (+)-molephantin or a derivative thereof. Also disclosed herein are methods of forming a compound of formula XIV and of forming a compound of formula XV, wherein compound of formula XIV and compound of formula XV are as defined in the description.
专利号:US-11136335-B2 优先权日:2016-06-30 标题:Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHASE CHARLES E; CHOI HYEONG-WOOK; ENDO ATSUSHI; FANG FRANCIS G; KIM DAE-SHIK 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
专利号:US-6579725-B1 优先权日:1999-03-05 标题 :Linkers for synthesis of oligosaccharides on solid supports 发明人:SEEBERGER PETER H; ANDRADE RODRIGO B 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention relates to versatile linkers for tethering a molecule to a solid support, e.g., for tethering a monomer, oligomer or polymer to a solid support, which are stable to a wide range of reaction conditions, but can be cleaved under well-defined conditions, thereby liberating the molecule from the solid support. Preferably, the linkers are used to tether to the solid support unprotected, partially-protected or fully-protected monosaccharides or oligosaccharides, or unprotected, partially-protected or fully-protected glycoconjugates. The linkers of the present invention may be used to tether to solid supports building blocks useful in the assembly of libraries of other types of small molecules. The present invention also relates to a molecule or plurality of molecules tethered to the solid support via a linker or linkers of the present invention. The present invention also relates to processes for synthesizing molecules, e.g., monomers, oligomers or polymers, on a solid support, wherein a starting material in the synthesis of the molecule, intermediates in the synthesis of the molecule, and the molecule itself are tethered to the solid support during the process via one of the linkers of the present invention. In certain processes of the present invention, the molecule is liberated from the solid support by cleavage of the linker of the present invention.
专利号:US-10676481-B2 优先权日:2016-02-12 标 题 :Intermediates in the synthesis of eribulin and related methods of synthesis 发明人:BARAN PHIL S; CHASE CHARLES E; FANG FRANCIS G 权利人:EISAI R&D MAN CO LTD 摘要:The invention relates to methods and intermediates useful in the synthesis of eribulin.
专利号:US-9783549-B2 优先权日:2013-11-04 标题:Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E; LEE JAEMOON 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
专利号:US-9994508-B2 优先权日:2012-12-11 标 题:Versatile and functionalised intermediates for the synthesis of vitamin D and novel vitamin D derivatives 发明人:LOPEZ PEREZ BORJA; SIGUEIRO PONTE RITA; MAESTRO SAAVEDRA MIGUEL A; MOURINO MOSQUERA ANTONIO 权利人:ENDOTHERM GMBH 摘要:Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.
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