N-Trimethylsilyl Urea 反应 0.5H,反应生成三甲基硅基异氰酸酯 参考文献:Kozyukov,V. P.; Muzovskaya,E. V.; Mironov,V. F.,Journal Of General Chemistry Of The Ussr,1983,Vol. 53,# 5,P. 972-978 标题:Kozyukov,V. P.; Muzovskaya,E. V.; Mironov,V. F.,Journal Of General Chemistry Of The Ussr,1983,Vol. 53,# 5,P. 972-978
专利号:WO-2024218783-A1 优先权日:2023-04-17 标题 :Green chemistry approach for synthesis of mavacamten and its intermediate using novel methodology 发明人:CHEEPIRISHETTI SHANKAR; CHEEPIRISHETTI ASHRIT; KOMARRAJ SNEHITHA; KAUSHAL KISHORE; BORREDDY SIVA PRASAD REDDY; BASANTHI DEVI; SHAIK SAYYAD SHAMSHUDDIN; KUMAR MUKES 权利人:DASHA PHARMACEUTICALS PRIVATE LTD 摘要:The present invention discloses a green chemistry approach for synthesis of Mavacamten (Compound of formula I). The present invention also discloses a novel process for preparation of an intermediate 1-isopropylpyrimidine-2,4,6(1H,3H,5H)-trione (Compound of formula VII) and further preparation of Mavacamten using this intermediate, following novel methodology.
专利号:US-5286901-A 优先权日:1990-03-09 标题:Prescursors for and synthesis of mono- and difunctionalized acetylenes and difunctional 1,3-diynes 发明人:STANG PETER J; CRITTELL CHARLES M; WILLIAMSON BOBBY L; ZHDANKIN VIKTOR 权利人:UNIV UTAH RES FOUND 摘要:Precursors and methods for the synthesis of mono- and difunctionalized acetylenes are described. The invention includes novel tricoordinate iodonium transfer reagents and novel alkynyldi(phenyliodonium) salts, both of which are precursors for the functionalized acetylenes. The iodonium transfer reagents take the general form of mixed iodonium sulfonates PhI + (X)OSO 2 R f , where X may be OAc, NHAc, NCO, or CN. These mixed iodonium sulfonates are produced by reaction of iodosobenzene with certain substituted trimethylsilanes. n To make the alkynyldi(phenyliodonium) salt PhI + C.tbd.CI + Ph•2 R f SO 3 - ,a mixed iodonium sulfonate is reacted with a bistin acetylene of the kind R' 3 SnC.tbd.CSnR' 3 . Alternatively, the reaction may be performed with disubstituted tin diacetylenes to produce PhI + C.tbd.C-C.tbd.CI + Ph•2 R f SO 3 - to produce a dialkynyldi(phenyliodonium) salt. Subsequent reaction of a nucleophile with the alkynyldi(phenyl-iodonium) salt or dialkynyldi(phenyliodonium) salt produces a difunctional acetylene or a difunctional 1,3-diyne, respectively.
专利号:US-5714127-A 优先权日:1992-10-08 标题 :System for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J 权利人:WARNER LAMBERT CO 摘要:A system for the multiple, simultaneous synthesis of compounds preferably uses a reaction apparatus comprising a reservoir rack having a plurality of reaction wells, a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends, a holder block, having a plurality of apertures, and a manifold, which has ports to allow introduction/maintenance of a controlled environment. The manifold top wall has a plurality of apertures in axial alignment with the reaction tubes and a gasket which allows penetration by a needle in order to dispense and aspirate materials from the reaction tubes. Sealing members, such as gaskets, are placed between the holder block, manifold and reservoir rack and the components are releasably fastened together. A robotic sample processor is used to automate the synthesis process using the reaction apparatus.
专利号:US-5702672-A 优先权日:1992-10-08 标 题 :Apparatus and method for multiple simultaneous synthesis 发明人:DEWITT SHEILA H H; KELL MICHAEL; PAVIA MICHAEL R; KIELY JOHN S; SCHROEDER MEL C; STANKOVIC CHARLES J; WARE STEVEN 权利人:WARNER LAMBERT CO 摘要:An apparatus for multiple, simultaneous synthesis of compounds which consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold.
专利号:US-8153615-B2 优先权日:2005-06-10 标 题:Synthesis of glycerolipid carbamates and dicarbamates and their use as an antitumor compounds 发明人:BITTMAN ROBERT; BYUN HOE-SUP; ARTHUR GILBERT 权利人:BITTMAN ROBERT; BYUN HOE-SUP; ARTHUR GILBERT 摘要:The syntheses and in vitro antitumor properties of carbamate-containing, dicarbamate-containing, and ureido-containing phospholipid compounds that have an ether linkage at the C-1 position of a glycerol backbone, a carbamate, dicarbamate, or ureido moiety at the C-2 position of the glycerol backbone, and a phosphocholine, phosphonocholine, or glycoside moiety at the C-3 position of the glycerol backbone are described. The synthesis and antiproliferative activity of ether lipids with a naphthol moiety at the C-1 position are also described. These compounds were shown to be potent inhibitors of cancer cell growth. These compounds are useful for killing cancer cells and treating cancer.
专利号:US-5766556-A 优先权日:1992-10-08 标题:Apparatus and method for multiple simultaneous synthesis 发明人:DEWITT SHEILA HELEN HOBBS; KIELY JOHN STEVEN; PAVIA MICHAEL RAYMOND; SCHROEDER MEL CONRAD; STANKOVIC CHARLES JOHN 权利人:WARNER LAMBERT CO 摘要:An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.