CAS: 459-57-4; 4-Fluorobenzaldehyde

上下游产品

CAS号64002-52-4 acetic acid,(4-... | CAS号352-34-1 4-氟碘苯 | CAS号201230-82-2 carbon monoxide | CAS号1194-02-1 对氟苯腈 | CAS号459-56-3 对氟苯甲醇 | CAS号460-00-4 对氟溴苯 | CAS号459-23-4 4-氟苯甲醛肟 | CAS号1063716-66-4 | CAS号405-99-2 4-氟苯乙烯 | CAS号1774-35-2 4,4'-二甲苯亚砜 | CAS号111729-74-9 2-[(4-fluorophe... | CAS号104941-02-8 1-[3-(4-chlorop... | CAS号1065102-64-8 Methyl 2-(4-flu... | CAS号111436-61-4 3-[4-(bromometh... | CAS号110677-45-7 4-(9H-咔唑-9-基)苯甲醛 | CAS号104314-04-7 3-(4-氟苯基)-2-噻吩-2-丙烯酸 | CAS号105966-78-7 2-(benzenesulfo... | CAS号39769-09-0 4-氟-N-(4-氟苯亚甲基)苯胺 | CAS号61343-99-5 4-(4-氯-苯氧基)- 苯乙酮 | CAS号41498-10-6 4-[1,2,3]噻唑-1-苯甲醛

扁桃腈置于potassium Cyanide,二氧化碳,Titanium(Iv)Isopropoxide,1,8-二氮杂双环[5.4.0]十一碳-7-烯,1,3-二-叔丁基咪唑氯化物,Lithium Hexamethyldisilazane,Sodium T-Butanolate体系中,用 四氢呋喃,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,12.0~78.0 °C,101.33 Kpa 条件下,反应 56.25H,反应生成 对氟苯甲醛
参考文献:醛对二氧化碳的umpolung反应性
标题:醛对二氧化碳的umpolung反应性
摘要:二氧化碳是本质上稳定的分子.因此,其活化需要以反应性试剂和/或活化的催化剂的形式以及通常苛刻的反应条件的形式输入额外的能量.此处报道的是芳香醛与二氧化碳的直接羧化反应,以提供α-酮酸作为增值产品.在操作温和的反应条件下(25-40°C,1 Atm Co 2),原位反应生成反应性氰醇是成功进行羧化反应的关键.所得的α-酮酸可作为还原性胺化反应合成α-氨基酸的平台,说明了从二氧化碳化学合成基本生物活性分子的过程.
DOI:10.1002/anie.201806569

专利信息

专利号:US-2008032964-A1
优先权日:2006-04-10
标题:Process for the synthesis of azetidinone
发明人：KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.

专利号:US-6251689-B1
优先权日:1998-05-14
标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof
发明人：LABORDE EDGARDO; MATSUMOTO YUKIHARU
权利人:TELIK INC
摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.

专利号:US-5861532-A
优先权日:1997-03-04
标 题:Solid-phase synthesis of N-alkyl amides
发明人：BROWN EDWARD G; NUSS JOHN M
权利人:CHIRON CORP
摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.

专利号:US-6177564-B1
优先权日:1998-09-11
标题:Process for the synthesis of N-benzyl-3-(4-fluorophenyl)-1-4-oxazin-2-one
发明人：NELSON TODD D; BHUPATHY MAHADEVAN
权利人:MERCK & CO INC
摘要:The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of the formula:This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.

专利号:US-2009270630-A1
优先权日:2006-06-23
标题:Process for the synthesis of benzylidene rosiglitazone base
发明人：CZIBULA LASZLO; SEBOK FERENC; DOBAY LASZLO; WERKNE PAPP EVA; DEUTSCHNE JUHASZ IDA; NAGYNE BAGDY JUDIT; UBERHARDT TAMASNE
权利人:CZIBULA LASZLO; SEBOK FERENC; DOBAY LASZLO; WERKNE PAPP EVA; DEUTSCHNE JUHASZ IDA; NAGYNE BAGDY JUDIT; UBERHARDT TAMASNE
摘要:Process for the synthesis of 5-{4-[N-methyl-N-(2-pyridyl)-amino-ethoxy]-benzylidene}-thiazolidine-2,4-dione (INN name: benzylidene-rosiglitazone) of formula (I), which consist of the following steps: n n n n n n n n n n n n Step a) reaction of 2-chloro-pyridine and 2-(N-methylamino)-ethanol n Step b) reaction of the obtained compound of formula (III) with 4-fluorobenzaldehyde n Step c) reaction of the obtained compound of formula (IV) with thiazolidine-2,4-dione n n n n n n n n n n n n n n characterized byn dissolving 4-{2-[N-methyl-N-(2-pyridyl)amino]-ethanol of formula (III) obtained in Step a) in toluene and using it in Step b) without isolation; reacting the solution of compound of formula (III) in toluene in Step b) with 4-fluorobenzaldehyde in the presence of aqueous alkali hydroxide solution and phase transfer catalyst at 25-50° C.; reacting the solution of the benzaldehyde derivative of formula (IV) obtained in Step b) in toluene in Step c) and isolating the desired product.

专利号:US-10266565-B2
优先权日:2011-04-12
标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN
权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.