📜2-甲基噻吩置于三(五氟苯基)硼烷,氢气体系中,用 邻二氯苯 用作溶剂,100.0 °C,405.33 Kpa 条件下,反应 80.0H,反应生成2-甲基四氢噻吩 参考文献:E-h (E = R3Si Or H) Bond Activation By B(C6F5)3 And Heteroarenes; Competitive Dehydrosilylation,Hydrosilylation And Hydrogenation 标题:E-h (E = R3Si Or H) Bond Activation By B(C6F5)3 And Heteroarenes; Competitive Dehydrosilylation,Hydrosilylation And Hydrogenation 摘要:R3Si-H-B(C6F5)3对杂环芳烃的加成会产生令人惊讶的复杂和取决于底物的混合物,这是因为竞争性的去氢硅化,氢硅化和氢化作用. Doi:10.1039/c3Cc47372D
专利号:WO-2020208409-A1 优先权日:2019-04-10 标 题 :Improved processes for the preparation of peptide intermediates/modifiers 发明人:BUDHDEV DR RAJEEV REHANI; NARIYAM MUNASWAMY SEKHAR; AKULA SWAPNA; KAIPU RAMAKRISHNA REDDY; KOMATI SHRAVAN KUMAR; KARTHIK RAMASWAMY; KOMARAVOLU YAGNA KIRAN KUMAR 权利人:Dr Reddy’s Laboratories Ltd 摘要:The present application relates to improved processes for the preparation of peptide intermediates/modifier compounds of Formula (I) and their use in the synthesis of peptide derivatives. The present application further provides the compound of Formula I with high chemical purity of >98% and chiral purity of >99% and its use to make pharmaceutical peptide like Liraglutide.
专利号:US-10927095-B2 优先权日:2017-08-14 标 题:Processes for the preparation of Niraparib and intermediates thereof 发明人:LUTHRA PARVEN K; VASOYA SANJAY L; PATIL BHATU T; TANEJA AMIT K; SRIVASTAV NAVEEN C; SINGH RINKU 权利人:TEVA PHARMACEUTICALS INT GMBH 摘要:The present invention relates to novel procedures and novel intermediates useful in the synthesis of Niraparib or any salt thereof.
专利号:US-4311862-A 优先权日:1979-09-04 标 题:Preparation of unsaturated ethers 发明人:DRENT EIT 权利人:SHELL OIL CO 摘要:Process for the preparation of olefinically unsaturated ethers by reacting a conjugated diene and a lower alkanol with the aid of an acidic catalyst in the presence of a non-basic aprotic polar solvent. The olefinically unsaturated ethers are of interest as solvents and gasoline additives and can also be used as starting materials for e.g. the synthesis of ketones.
专利号:US-4593113-A 优先权日:1985-01-14 标 题:Synthesis of transition metal dithiene complexes 发明人:KAUFFMAN MARTIN H 权利人:US NAVY 摘要:The preparation of transition metal dithiene complexes is disclosed. By the process improved yields of the metal dithiene complexes are realized by substituting highly polar aprotic solvents such as N-methylpyrrolidinone or high boiling point solvents such as diethylene glycol in place of dioxane in the reaction sequence.
专利号:US-8703747-B2 优先权日:2008-07-23 标题 :Aminophosphinic derivatives that can be used in the treatment of pain 发明人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE 权利人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE; PHARMALEADS 摘要:The present invention relates to a compound of the following general formula (I): R 1 —NH—CH(R 2 )—P(â•?O)(OR 3 )—CH 2 —C(R 4 )(R 5 )—CONH—CH(R 6 )—COOR 7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R 1 represents a —C(â•?O)—O—C(R 8 )(R 9 )—OC(â•?O)—R 10 group; R 2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R 3 represents a hydrogen atom or a —C(R 12 )(R 13 )—OC(â•?O)—R 14 group; R 4 and R 5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R 4 represents a hydrogen atom and R 5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R 6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R 7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, —CHMe—COOR 18 , —CHR 19 —OC(â•?O)OR 20 and —CHR 19 —OC(â•?O)OR 20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more avantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
专利号:US-2007275962-A1 优先权日:2003-09-10 标 题:Heterobicyclic Compounds as Pharmaceutically Active Agents 发明人:KOUL ANIL; KLEBL BERT; MULLER GERHARD; MISSIO ANDREA; SCHWAB WILFRIED; HAFENBRADL DORIS; NEUMANN LARS; SOMMER MARC-NICOLA; MULLER STEFAN; HOPPE EDMUND; FREISLEBEN ACHIM; BACKES ALEXANDER; HARTUNG CHRISTIAN; FELBER BEATRICE; ZECH BIRGIT; ENGKVIST OLA; KERI GYORGY; ORFI LASZLO; BANHEGYI PETER; GREFF ZOLTAN; HORVATH ZOLTAN; VARGA ZOLTAN; MARKO PETER; PATO JANOS; SZABADKAI ISTVAN; SZEKELYHID ZSOLT; WACZEK FRIGYES 权利人:GPC BIOTECH AG 摘要:Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
参考标题:An Aryne Triggered Ring-Opening Fluorination Of Cyclic Thioethers With Potassium Fluoride 作者:Rong Fan,Binbin Liu,Tianyu Zheng,Kun Xu,Chen Tan,Tianlong Zeng,Shuaisong Su,Jiajing Tan 摘要:Report An Aryne Triggered Ring-Opening Fluorination Protocol Of A Great Variety Of Saturated Sulfur Heterocycles. A Key Factor For The Success Is The Identification Of A Suitable Mediator. Compared To Previous Methods, This Transition-Metal Free Protocol Employs Low-Cost Potassium Fluoride As The Fluorine Source. The Operational Simplicity And Mild Reaction Conditions Allow For The Rapid Synthesis Of A
合成参考文献
参考文献:10.1007/s42978-025-00331-1 摘要:Chou H, Craster A, Arthur K, Boyle B, Allsworth M, Kelley EF, Stewart GM, Wheatley-Guy CM, Schwartz J, Fermoyle CC, Ziegler BL, Johnson KA, Robach P, Basset P, Johnson BD. Novel Correlations Between Lung Function and Gut Microbial-Produced VOCs in the Exhaled Breath of Ultramarathon Runners: Insights from the 2019 Ultra-Trail du Mont Blanc. J. of SCI. IN SPORT AND EXERCISE. 2025 Sep 15;(). doi: 10.1007/s42978-025-00331-1. 参考文献:10.1134/s096554412560136x 摘要:Izoitko AI, Koveza VA, Potapenko OV. Effects of ZSM-5 Modification with Manganese and Iron Cations on n-Dodecane/2-Methylthiophene Conversion Pathway. Pet. Chem. 2025 Oct;65(10):1160–9. doi: 10.1134/s096554412560136x.