专利号:US-11661406-B2 优先权日:2018-08-13 标 题 :Method for producing intermediate useful for synthesis of SGLT inhibitor 发明人:LI QING RI; YOON HEE KYOON 权利人:DAEWOONG PHARMACEUTICAL CO LTD 摘要:A method of preparing an intermediate useful for the synthesis of a diphenylmethane derivative that can be used as an SGLT inhibitor is described. A method of synthesizing a compound of Formula 7 can address problems of existing synthesis processes requiring the synthesis of the Grignard reagent and management of related substances. In addition, the method can minimize the generation of related substances, and thus does not require reprocessing of reaction products, thereby simplifying the process. Accordingly, the production yield of a diphenylmethane derivative can be maximized.
专利号:US-8859763-B1 优先权日:2013-05-17 标题 :Process for the synthesis of 3,4-dimethoxybicyclo[4.2.0]OCTA-1,3,5-triene-7-carbonitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:VAYSSE-LUDOT LUCILE; LE FLOHIC ALEXANDRE; VAULTIER MICHEL; PUCHEAULT MATHIEU; KAMINSKI THOMAS 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:WO-2023126968-A1 优先权日:2021-12-29 标 题 :A process for the synthesis of bcx-1777 and bcx-4430 发明人:LANKALAPALLI RAVI SHANKAR; KARUNAKARAN ANITHA KRISHNAKUMAR; SURESH SANJAY VARMA; VELICKAKATHU OMANAKUTTAN YADHUKRISHNAN; KAPIYA SANGEETH; VALAPPIL SHIHAS AHAMMED CHEKRAIN; BERNARD PRABHA; THANGARASU ARUN KUMAR; DODDRAMAPPA DODDAMANI SHRIDEVI; JOHN JUBI; KOKKUVAYIL VASU RADHAKRISHNAN; AYYAPPANPILLAI AJAYAGHOSH 权利人:COUNCIL SCIENT IND RES 摘要:The present invention is concerned with a novel convergent route for synthesis of BCX-1777 and BCX-4430. Two key starting materials that were carefully chosen for cross-coupling were a stable sugar intermediate, unlike the imine intermediates in the prior art, and dihalogenated pyrrolopyrimidine intermediate. A chemoselective cross-coupling was achieved from the two key starting materials, which upon reduction and activation resulted in stereoselective formation of an advanced intermediate in 55% yield from protected D-ribonolactone in 6 steps. The advanced intermediate then served as a starting material for synthesis of BCX-1777 and BCX-4430 in 38% (over 8 steps) and 32% (over 9 steps) yields, respectively from protected D-ribonolactone.
专利号:US-10011580-B2 优先权日:2016-04-21 标题:Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof 发明人:WALSE SPENCER S; KUZMICH DANIEL 权利人:US AGRICULTURE 摘要:A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R 1 is ethenyl, R 2 and R 3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R 2 is ethenyl, R 1 and R 3 is methyl and n is 1), and analogs thereof (wherein: R 1 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 2 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 1 and R 2 together with the carbon atom they are attached form a C 3-6 cycloalkyl ring, R 3 is C 1-5 alkyl and n is 0-2):
专利号:US-2025179012-A1 优先权日:2022-03-04 标 题:Synthesis of sulfur(vi) compounds and reagents for same 发明人:LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.
专利号:WO-2017063617-A1 优先权日:2015-10-13 标 题 :Preparation of intermediates for the synthesis of canagliflozin and dapagliflozin 发明人:ZEZULA JOSEF; BABIAK PETR; HAJDUCH JAN 权利人:ZENTIVA KS 摘要:The present invention relates to a preparation method of the intermediates of structures la (for the synthesis of canagliflozin) and 1b (for the synthesis of dapagliflozin), where in structure la X is methyl and Ar represents 2-(5-(4-fluorophenyl)-thienyl) and in structure 1b X is chlorine and Ar represents 4-ethoxyphenyl.
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
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