专利号:US-11866398-B2 优先权日:2018-05-15 标 题:Total synthesis of prostaglandin J natural products by stereoretentive metathesis 发明人:LI JIAMING; CHEN XU; AHMED TONIA S; STOLTZ BRIAN M; GRUBBS ROBERT H 权利人:CALIFORNIA INST OF TECHN 摘要:This invention relates generally to the synthesis of Δ12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. Δ12-Prostaglandin J products were generated with excellent selectivity (>99% Z) and in moderate to high/good yields (47% to 80% yield; 58% to 80% yield).
专利号:US-10995049-B2 优先权日:2019-07-19 标 题 :Total synthesis of prostaglandin J natural products and their intermediates 发明人:LI JIAMING; XU CHEN; AHMED TONIA S; GRUBBS ROBERT H; STOLTZ BRIAN M 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure is directed to methods of preparing prostaglandin J natural products by stereoretentive metatheses reactions and intermediates used in the synthesis of these natural products, including the use of intermediates of Formula (I-A), where R 1 is defined in the specification
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-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-4910310-A 优先权日:1988-10-03 标 题:Synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives 发明人:CAMPBELL ARTHUR L; BEHLING JAMES R; BABIAK KEVIN A; NG JOHN S; MUELLER RICHARD A; FLEET GEORGE W J 权利人:SEARLE & CO 摘要:Novel intermediates and method for the chemical synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives are provided. A preferred intermediate is 1,5-dideoxy-1,5-imino-3, 4-O-isopropylidene-L-fucitol which is used to prepare the HIV inhibitor 1,5-dideoxy-1,5-imino-[N-ω-methyl caproate]-L-fucitol. These compounds are prepared in a short synthesis from the known compound 2,3-O-isopropylidene-D-lyxono-1,4-lactone or in a multi-step synthesis from D-galactose.
专利号:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
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