专利号:US-2004266827-A1 优先权日:2003-06-25 标 题 :Convergent asymmetric route to produce a key intermediate towards the synthesis of a garft inhibitor 发明人:NOTZ WOLFGANG REINHARD LUDWIG; MARTINEZ CARLOS ALBERTO 权利人:AGOURON PHARMA 摘要:The invention relates to processes for the preparation of a key intermediate in the synthesis of a GARFT inhibitor of formula (Ia) containing a 4-methyl-substituted thiophene core: n n n wherein said key intermediate has the following formula (I): n n n wherein each of R 1 and R 2 are independently a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; n from a compound of the formula (VI): n n n wherein R 1 is as described above, Pg 1 is an amino protecting group, and Pg 2 is an ether protecting group; wherein said processes are as described in the specification.
专利号:US-11999757-B2 优先权日:2017-11-01 标 题:Synthesis of boronate ester derivatives and uses thereof 发明人:BOYER SERGE HENRI; HECKER SCOTT J; VERZIJL GERARDUS K M; HERMSEN PETRUS J 权利人:MELINTA SUBSIDIARY CORP 摘要:Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.
专利号:US-10669292-B2 优先权日:2014-05-05 标 题 :Synthesis of boronate salts and uses thereof 发明人:HECKER SCOTT; BOYER SERGE 权利人:REMPEX PHARMACEUTICALS INC 摘要:Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.
专利号:US-8598046-B2 优先权日:2008-12-30 标 题 :Autosynthesizer for the controlled synthesis of nano- and sub-nanostructures 发明人:PACHAURI VIVEK; AHMAD ASHRAF; BALASUBRAMANIAN KANNAN; KERN KLAUS 权利人:PACHAURI VIVEK; AHMAD ASHRAF; BALASUBRAMANIAN KANNAN; KERN KLAUS; MAX PLANCK GESELLSCHAFT 摘要:The present invention relates to a method and apparatus for the synthesis of nanostructures using at least one solution providing at least one chemical element appropriate for the type of nanostructure, the method comprising the steps of: a) adding (admixing) a reducing agent to the at least one solution, b) bringing a suitable substrate into contact with the at least one solution before or after step a), c) forming nucleation growth sites on the substrate and d) maintaining the temperature at a suitable level for the growth of the nanostructures, characterized by the further steps of e) providing at least one space having at least one dimension in the micron range, e.g. in the range from 1 μm to 500 μm, adjacent a surface of the substrate, f) growing said nanostructures in said at least one space, g) periodically separating said nanostructures from the substrate and removing them.
专利号:US-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
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.
参考标题:Synthesis Of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, And 2-Pyrazolylbenzohydrazide Via 3-Substituted 3-Hydroxyisoindolin-1-Ones 作者:Hanh Nho Nguyen,Victor J. Cee,Holly L. Deak,Bingfan Du,Kathleen Panter Faber,Hakan Gunaydin,Brian L. Hodous,Steven L. Hollis,Paul H. Krolikowski,Philip R. Olivieri,Vinod F. Patel,Karina Romero,Laurie B. Schenkel,Stephanie D. Geuns-Meyer |发布日期:2012.4.20 摘要:Hydrazine, Followed By Chlorination With Pocl3. We Have Also Discovered Two Novel Transformations Of 3-Vinyl- And 3-Alkynyl-3-Hydroxyisoindolinones. Addition Of Vinyl Organometallic Reagents To N,N-Dimethylaminophthalimide (8A) Provided Dihydrobenzoazepinediones 15A-15C Via The Proposed Ring Expansion Of 3-Vinyl-3-Hydroxyisoindolinone Intermediates. 3-Alkynyl-3-Hydroxyisoindolinones React With Hydrazine And
合成参考文献
摘要:Zhang, H.; Liu, C.; Lei, A., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 167. 摘要:Nakao, Y., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 367. 摘要:Ghosh, I., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 407. 摘要:Zhang, F.-L.; Wang, Y.-F., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 388. 摘要:Selt, M.; Waldvogel, S. R., Science of Synthesis: Special Topics, (2021) 1, 262.