碳酸甲丙酯置于sodium Monobenzoxyborohydride体系中,用 四氢呋喃 用作溶剂,化学反应 5.0H,以93%的收率获得2-甲基吡啶-N-甲硼烷 参考文献:A Safe And Scalable Procedure For Preparation Of α-Picoline-borane From Sodium Mono-Acyloxyborohydrides And α-Picoline 标题:A Safe And Scalable Procedure For Preparation Of α-Picoline-borane From Sodium Mono-Acyloxyborohydrides And α-Picoline 摘要:Sodium Monobenzoxyborohydride,Which Is Easily Prepared From Sodium Borohydride And Benzoic Acid In Thf In Situ,Is Treated With Alpha-Picoline In Thf Under Mild Conditions To Give Alpha-Picoline-Borane In An Excellent Yield. This Method Can Be A Practical Preparation For Alpha-Picoline-Borane. Doi:10.1021/op2003858
专利号:US-2024199637-A1 优先权日:2021-04-21 标题 :Improved process for the preparation of 7-(morpholinyl)-2-(n-piperazinyl)methylthieno[2, 3-c]pyridine derivatives 发明人:KOMPELLA AMALA; VAGICHERLA KAMESWARA RAO; LANKI REDDY TIRUMALA REDDY; PESARU NARMADA; MUDDASANI PULLA REDDY; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD 摘要:The present invention describes an improved second generation process for the synthesis of NRC-1111 (1,5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-7-(4-morpholinyl)thieno[2,3-c] pyridine-5-yl]-2-pyrimidinamine) dimethane sulfonate and NRC-1109 (II, 5-[3-methyl-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-7-morpholino-thieno[2,3-c]pyridin-5-yl]pyrimidin-2-amine) dimethane sulfonate. This process is cost effective, high yielding and industrially feasible process for the synthesis of compounds of formulae I and II with high purity. Formula (I) Formula (I): Râ•?H for NRC-1111 and Formula (II): Râ•?CH3 for NRC-1109 NRC-1111 and NRC-1109 are potential anti-cancer agents.
专利号:US-9512080-B2 优先权日:2012-07-10 标 题:Synthesis of acridinium compounds by N-alkylation of acridans 发明人:NATRAJAN ANAND; WEN DAVID 权利人:SIEMENS HEALTHCARE DIAGNOSTICS INC 摘要:A method is provided for N-alkylation of acridine compounds by reduction of acridines to corresponding acridans to improve the reactivity of the acridine nitrogen, and subsequent N-alkylation of the acridans in ionic liquid solvents to provide the corresponding acridinium compounds in high yield. This inventive process improves chemical conversion, and does not require the use of highly toxic alkylating agents, such as 1,3-propane sultone.
专利号:US-12234209-B2 优先权日:2018-06-25 标题 :N-alkylation of acridans 发明人:NATRAJAN ANAND 权利人:SIEMENS HEALTHCARE DIAGNOSTICS INC 摘要:The present invention provides compounds used in the synthesis of chemiluminescent acridinium compounds and methods of producing these compounds. Specifically, methods are provided for the N-alkylation of acridan compounds using alkylating reagents. Typically, these alkylating reagents comprise a protected sulfonate group protected with an acid-labile protecting group.
专利号:US-12435049-B2 优先权日:2020-05-06 标 题:Synthesis of vinylic protected alcohol intermediates 发明人:SMITH AUSTIN G; HUANG LIANG 权利人:AMGEN INC 摘要:Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound D, wherein OPG and R1 are described herein. Compound D can be useful in synthesizing compound A1, or a salt of solvate thereof, and compound A2, or a salt of solvate thereof.
专利号:US-11590142-B2 优先权日:2018-03-28 标题 :Oxazolidinone antibiotic compounds and process of preparation 发明人:PEER MOHAMED SHAHUL HAMEED; BHARATHAM NAGAKUMAR; KATAGIHALLIMATH NAINESH; SHARMA SREEVALLI; NANDISHAIAH RADHA; RAMACHANDRAN VASANTHI 权利人:BUGWORKS RES INC 摘要:Compounds of Formula I, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivative thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments are provided. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention, or suppression of diseases, and conditions mediated by microbes. Methods for the synthesis and characterization of the aforementioned substances are also provided.
专利号:US-2023174496-A1 优先权日:2020-05-06 标 题:Synthesis of Vinylic Protected Alcohol Intermediates
参考标题:Activation Of Sodium Borohydride Via Carbonyl Reduction For The Synthesis Of Amine- And Phosphine-Boranes 作者:P. Veeraraghavan Ramachandran,Henry J. Hamann,Randy Lin 摘要:Carbonyl Reduction By Sodium Borohydride Is Described. Unlike The Prior Bicarbonate-Mediated Protocol, Which Proceeds Via A Salt Metathesis Reaction, The Carbon Dioxide-Mediated Synthesis Proceeds Via Reduction To A Monoformatoborohydride Intermediate. This Has Been Verified By Spectroscopic Analysis, And By Using Aldehydes And Ketones As The Carbonyl Source For The Activation Of Sodium Borohydride. This
合成参考文献
参考文献:10.1007/s10570-025-06847-7 摘要:Solberg A, King AWT, Koso T, Rodríguez-Fabià S, Syverud K. Hydroxylamine grafting of periodate oxidized cellulose microfibrils and its impact on fibre adhesion. Cellulose. 2025 Dec 07;33(2):717–31. doi: 10.1007/s10570-025-06847-7.