CAS: 637031-88-0; 3,3-Difluorocyclobutanol

该化合物是一种氟化环丁烷衍生物,具有独特的结构和电子特性; 3级存在两个氟原子,这增强了其稳定性和影响其反应力,使其成为制药和农用化学合成中有价值的中间体; 1级的氢氧基组为进一步发挥功能提供了多功能处理器,使其能够用于生物活性分子的开发; 其紧凑的硬环会助长消毒限制,这在设计符合性限制的化合物方面可能具有优势; 该化合物因其极性和代谢稳定性不同,在药用化学中特别有助于结构活动关系.

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CAS号637031-86-8 ((3,3-difluor°C...

合成工艺路线路线简述

  • 合成目标产物 3,3-Difluorocyclobutanol 主要起始原料 ((3,3-Difluorocyclobutoxy)Methyl)Benzene
  • (文献来源)合成步骤主要原料 ((3,3-Difluorocyclobutoxy)Methyl)Benzene
1,1-Difluoro-3-[(2-Methylpropan-2-yl)Oxy]Cyclobutane置于盐酸体系中,用 1,4-二氧六环 作为反应溶剂,以7.97 G的收率获得产物3,3-二氟环丁醇
参考文献:C4 / C5 3,3-二氟环丁基取代的结构单元的多重图合成
标题:C4 / C5 3,3-二氟环丁基取代的结构单元的多重图合成
摘要:摘要 描述了一种3,3-二氟环丁基取代的结构单元(包括羧酸,胺,醇,叠氮化物,三氟硼酸酯)的多谱图合成方法.结果表明,在大多数情况下,3,3-二氟环丁烷甲酸乙酯是获得目标衍生物的方便的常用合成中间体.为了制备3,3-二氟环丁醇或-环丁酮,应采用通过二氯乙烯酮与叔丁基或苄基乙烯基醚反应的替代途径. 描述了一种3,3-二氟环丁基取代的结构单元(包括羧酸,胺,醇,叠氮化物,三氟硼酸酯)的多谱图合成方法.结果表明,在大多数情况下,3,3-二氟环丁烷甲酸乙酯是获得目标衍生物的方便的常用合成中间体.为了制备3,3-二氟环丁醇或-环丁酮,应采用通过二氯乙烯酮与叔丁基或苄基乙烯基醚反应的替代途径.
DOI:10.1055/s-0037-1610237

海关参考信息

专利信息


专利号:US-2025091989-A1
优先权日:2023-09-19
标 题 :Small molecule protein synthesis modulators
发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.

专利号:US-12247037-B2
优先权日:2018-12-12
标题:1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-A][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders
发明人:BRANDT GARY
权利人:NEUMORA THERAPEUTICS INC
摘要:The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).

专利号:WO-2025128873-A1
优先权日:2023-12-12
标题:Heterocyclic pyridinone compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人:HOUZE JONATHAN B; PANDYA BHAUMIK
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).

专利号:WO-2023131254-A1
优先权日:2022-01-06
标 题 :Pseudouridine modified at n1 position and use thereof in mrna synthesis
发明人:LI SONG; GUO CHUANXIN; CAI XIAORU; QIAN QIJUN
权利人:MAXIRNA SHANGHAI PHARMACEUTICAL CO LTD; MAXIRNA ZHEJIANG TECH CO LTD
摘要:Provided in the present invention are a pseudouridine modified at an N1 position and the use thereof in mRNA synthesis. Specifically, the compound of the present invention comprises compounds represented by formula I and formula II, and the definition of each group in the formula is as described herein. The compound of the present invention can be used for preparing mRNA to reduce the autoimmunogenicity of the mRNA, improve the stability of the mRNA itself, and/or enhance the expression time and expression efficiency of the mRNA in a target cell.

专利号:US-2024409557-A1
优先权日:2023-05-09
标 题 :5,6-fused and 6,6-fused bicyclic alcohols and ethers and compositions for use as 15-prostaglandin dehydrogenase modulators
发明人:GREENMAN KEVIN LLOYD; PICKRELL ALEXANDER J; LI KEXUE; AMEGADZIE ALBERT K; WANG HUI-LING; WEIRES NICHOLAS ANTHONY; ALLEN JOHN G; BOURBEAU MATTHEW P
权利人:AMGEN INC
摘要:The present disclosure provides novel 15-hydroxy-prostaglandin dehydrogenase inhibitors, pharmaceutical compositions comprising such compounds, and methods of using such compounds and compositions in treating 15-hydroxy-prostaglandin dehydrogenase-mediated disease. Also provided are methods of making such compounds and intermediates thereof. The compounds have a general Formula (A).Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (A).

专利号:US-11858943-B2
优先权日:2017-06-05
标题:Vasopressin receptor antagonists and products and methods related thereto
发明人:JONES ROBERT M; URBANO MARIANGELA; BRANDT GARY; HARDICK DAVID; KNIGHT CHRIS; TIERNEY JASON
权利人:NEUMORA THERAPEUTICS INC
摘要:Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof:wherein A, B, G, R1, R1b, R1c, R2 and X are as defined herein.
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合成参考文献


参考文献:10.1055/s-0037-1610237
摘要:Ryabukhin S, Melnykov K, Granat D, Volochnyuk D, Grygorenko O. Multigram Synthesis of C4/C5 3,3-Difluorocyclobutyl-Substituted Building Blocks. Synthesis. 2018 Aug 20;50(24):4949–57. doi: 10.1055/s-0037-1610237.
参考文献:10.1007/s00044-023-03088-w
摘要:Wehn PM, Yang S, Grina JA, Rizzi JP, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Czerwinski RM, Ged EL, Huang H, Halfmann MM, Maddie MA, Morton ER, Olive SR, Tan H, Xie S, Josey JA, Wallace EM. Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→π*Ar interaction. Med Chem Res. 2023 Jul;32(7):1510–31. doi: 10.1007/s00044-023-03088-w.
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