专利号:US-2025313590-A1 优先权日:2024-03-16 标题:Phosphoramidite morpholino monomers towards synthesis/convergent synthesis of PMO, TMO, their chimera oligos in 5 prime to 3 prime direction 发明人:SINHA SURAJIT; GHOSH ATANU; BANERJEE ARPAN 权利人:INDIAN ASS FOR THE CULTIVATION OF SCIENCE 摘要:The present invention relates to 5′-morpholino amidite monomers as 5′-CE/5′- t Bu phosphoramidite morpholino monomers (2) and process chemistry for the efficient synthesis of N-Trityl or monomethoxytrityl (MMTr)-protected 5′-morpholino amidite monomers and their use in the synthesis of phosphorodiamidate morpholino oligonucleotides (PMO), thiophosphoramidate morpholino oligonucleotides (TMO) and their chimeras which can be used for antisense technology or in general oligonucleotides related research.
专利号:US-12012427-B2 优先权日:2019-10-31 标 题 :Synthesis of Fmoc-protected morpholino monomers and their use in the synthesis of morpholino oligomer 发明人:SINHA SURAJIT; KUNDU JAYANTA; GHOSH UJJWAL 权利人:INDIAN ASS FOR THE CULTIVATION OF SCIENCE 摘要:Present invention relates to stable Fmoc protected Morpholino monomers and corresponding oligonucleotides (PMO) and efficient synthesis of the same involving chlorophosphoramidate and H-Phosphonate chemistry. Successful syntheses of the oligonucleotide with higher yield and lesser time have been accomplished employing solid phase synthesis and easy deprotection of Fmoc group with Piperidine.
专利号:US-12291596-B2 优先权日:2018-11-30 标 题 :Radical cascade-enabled synthesis of precision polymers with complex main-chain structures 发明人:NIU JIA; HUANG HANCHU; WANG WENQI 权利人:THE TRUSTEES OF BOSTON COLLEGE 摘要:Radical cascade reactions enabling sequence-controlled ring-closing polymerization and ring-opening polymerization for the controlled synthesis of polymers with complex main-chain structures are provided. Facile syntheses leading to low-strain macrocyclic monomers consisting of the ring-opening triggers and extended main-chain structures are also provided. The present disclosure further provides methods for excellent control over polymer molecular weights and molecular weight distributions and high chain-end fidelity allows for the preparation of polymeric systems with well-defined architectures. Further provided are the general nature of the radical cascade-triggered transformations in polymer chemistry, and its application to the synthesis of polymers with diverse main-chain structural motifs with tailored functions. 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-5220016-A 优先权日:1991-07-29 标 题:Synthesis of navelbine analogs 发明人:MAGNUS PHILIP D; THURSTON LEE S 权利人:UNIV TEXAS 摘要:The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.
专利号:US-6376676-B1 优先权日:1993-06-30 标题 :Intermediates in the synthesis of (±)-camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; LIU HUI 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of novel intermediates in the synthesis of (±)-camptothecin and related compounds. The present synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the camptothecin compound. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
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合成参考文献
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