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: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-2022395800-A1 优先权日:2019-11-04 标题:Device for automated synthesis of oligo- and polysaccharides 发明人:SEEBERGER PETER H; DANGLAD FLORES JOSE; LE MAI HOANG KIM; PARDO VARGAS ALONSO; SLETTEN ERIC; SALWICZEK MARIO 权利人:MAX PLANCK GESELLSCHAT ZU RFERDERUNG DER WSS E V; GlycoUniverse GmbH & Co KG&A 摘要:The present invention generally relates to automated synthesis technology, and more particularly, to a device and method for automated synthesis of oligo- and polysaccharides on a solid support. In particular the present invention relates to a device for automated synthesis of oligo- and polysaccharides on a solid support comprising a reaction vessel, a reagent storing component, a reagent delivery system, a cooling device for cooling reaction vessel, and a pre-cooling device for pre-cooling the reagents to be supplied.
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:WO-2021035382-A1 优先权日:2019-08-23 标题:Method forcontinuous synthesis of 2-cyclopentene-1-one 发明人:HONG HAO; LU JIANGPING; BAO DENGHUI; YUAN LONG; WANG BO 权利人:LIAONING ASYMCHEM LABORATORIES CO LTD 摘要:Provided is a method for the continuous synthesis of 2-cyclopenten-1-one. The continuous synthesis method comprises: loading a catalyst in a continuous reaction device, then continuously conveying cyclopentene, an oxidant and a solvent into the continuous reaction device for an oxidation reaction, and continuously discharging 2-cyclopentene-1-one. In the presence of the catalyst and the solvent, cyclopentene is used as a starting material, and same is directly oxidized by the oxidant, which can avoid the generation of a large amount of halogen-containing three wastes; at the same time, the entire continuous synthesis process is carried out in the continuous reaction device, which can effectively inhibit the occurrence of safety risks during scale-up production; in addition, after the reaction is complete, the product system of the oxidation reaction can be simply concentrated to obtain the target product (2-cyclopenten-1-one). Thus, the purity (up to 98% and above) and separation rate (up to 79%) of the product are greatly improved, and production can be easily scaled up.
专利号:US-4351767-A 优先权日:1981-06-29 标题 :Synthesis of 24,25-dihydroxycholesterol 发明人:KAISER EMIL T 权利人:KAISER EMIL T 摘要:This invention relates to the synthesis of steroids which are useful for their biological activity or which may be converted to steroids which have such activity. More particularly, the invention pertains to the synthesis of 24,25-dihydroxycholesterol. It includes intermediate sterols of this synthesis and processes for their preparation.
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