CAS: 540-37-4; 4-Iodoaniline

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CAS号636-98-6 4-硝基碘苯 | CAS号53694-87-4 1-AZIDO-4-IODOB... | CAS号1601-97-4 4-碘偶氮苯 | CAS号1059625-65-8 4-aminobenzened... | CAS号7758-19-2 亚氯酸钠 | CAS号87413-09-0 戴斯-马丁氧化剂 | CAS号107-19-7 丙炔醇 | CAS号109496-98-2 5-苯基靛红 | CAS号105752-04-3 4-碘-3-硝基苯胺 | CAS号52768-17-9 4-(1-吡咯基)苯胺 | CAS号60577-34-6 4-碘-N-甲基苯胺 | CAS号698-70-4 4-N,N-二甲氨基碘苯 | CAS号5470-49-5 4-甲磺酰基苯胺 | CAS号31271-90-6 N-(对甲苯磺酰)吲哚 | CAS号455-13-0 4-碘三氟甲苯 | CAS号2920-38-9 4-氰基联苯 | CAS号4854-84-6 4-氨基-4'-氰基联苯

N-Boc-4-碘苯胺置于甲醇,草酰氯体系中,化学反应 2.0H,以86%的收率获得产物对碘苯胺
参考文献:使用草酰氯对 N-叔丁氧羰基 (N-Boc) 基团进行温和脱保护
标题:使用草酰氯对 N-叔丁氧羰基 (N-Boc) 基团进行温和脱保护
摘要:我们报告了一种温和的方法,通过在甲醇中使用草酰氯,从结构多样的一组化合物(包括脂肪族,芳香族和杂环底物)中选择性脱保护n-Boc 基团.反应在室温条件下进行 1-4 小时,产率高达 90%.这种温和的程序应用于一种混合的药用活性化合物 Fc1,它是一种新型的 Ido1 和 Dna Pol γ 双重抑制剂.对于这种去保护策略,假设了涉及草酰氯的亲电特性的更广泛的机制.
DOI:10.1039/d0Ra04110F

专利信息

专利号:US-6919382-B2
优先权日:2000-08-31
标 题 :Preparation and uses of conjugated solid supports for boronic acids
发明人：HALL DENNIS G
权利人:UNIV ALBERTA
摘要:The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.

专利号:US-6420556-B1
优先权日:1998-12-17
标 题 :Acyl isothiocyanate resins and their use in solid-supported synthesis of guanidines
发明人：WILSON LAWRENCE JOSEPH
权利人:PROCTER & GAMBLE
摘要:The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetranikylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-2016194279-A1
优先权日:2012-12-09
标 题 :One pot process for the conversion of aroyl chlorides to acyl thioureas
发明人：CHEPURI VENKATA RAMANA; BEERAN SENTHILKUMAR
权利人:COUNCIL SCIENT IND RES
摘要:The present invention disclose an improved one pot process for synthesis of acyl thioureas of formula (I), with yield greater than 80%, from aroyl chlorides of formula (I) wherein, R′ is an aryl or a heteroarylene group substituted with one or more groups selected from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino, carboxyl, ester, halogenated hydrocarbon or an aryl or heteroaryl; R″ and R′″ are selected independently from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino or halogenated hydrocarbon.

专利号:US-3901899-A
优先权日:1973-04-27
标题 :Synthesis of indoles from anilines and intermediates therein
发明人：GASSMAN PAUL G
权利人:UNIV OHIO STATE RES FOUND
摘要:Preparing indoles and intermediates therefor by reacting an Nhaloaniline with a Beta -carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the Beta carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an Alpha -ethyl- Beta -carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures. The thio-ether-indole and thio-ether indolenine derivatives are useful as intermediates to make the indoles without the thio-ether group. The indoles are known compounds having a wide variety of uses, e.g., in making perfumes, dyes, amino acids, pharmaceuticals, agricultural chemicals and the like.

专利号:US-5446062-A
优先权日:1993-11-12
标 题:((4-alkoxypyran-4-yl) substituted) ether, arylalkyl-, arylalkenyl-, and arylalkynyl)urea inhibitors of 5-lipoxygenase
发明人：DELLARIA JOSEPH F; BASHA ANWER; BLACK LAWRENCE A; CHERNESKY LINDA J; LEE WENDY
权利人:ABBOTT LAB
摘要:Compounds of the structure where W is selected from where Q is oxygen or sulfur, R6 and R7 are hydrogen or alkyl, or R6 and R7, together with the nitrogen atoms to which they are attached, define a radical of formula Z is -CH2-, oxygen, sulfur, or -NR9, L1 and L2 are selected from a valence bond, alkylene, propenylene, and propynylene; R1 and R2 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is selected from oxygen, >NR10, and L3 is selected from alkylene of one to three carbon atoms, propenylene, propynylene, and R3, R4, and R5 are hydrogen or alkyl of one to four carbon atoms inhibit the synthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.