CAS: 2518-24-3; 4-Aminoisoindoline-1,3-Dione

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CAS号603-62-3 3-硝基邻苯二甲酰亚胺 | CAS号603-11-2 3-硝基邻苯二甲酸 | CAS号641-70-3 3-硝基邻苯二甲酸酐 | CAS号3682-14-2 异鲁米诺 | CAS号222036-66-0 5-氨基-2,3-二氢异吲哚-... | CAS号59434-19-4 4-氨基苯酞 | CAS号3883-64-5 7-氨基苯酞 | CAS号70478-63-6 4-溴异吲哚啉-1,3-二酮 | CAS号521-31-3 鲁米诺 | CAS号5972-09-8 4-(methylamino)... | CAS号6118-65-6 Acetamide,N-(2,...

3-硝基邻苯二甲酸酐置于ammonium Hydroxide,10% Pt/activated Carbon,氢气体系中,用 乙醇 用作溶剂,230.0 °C,202.66 Kpa 条件下,反应 26.0H,反应生成3-氨基邻苯二甲酰亚胺
参考文献:Chemoenzymatic Synthesis Of Apremilast: A Study Using Ketoreductases And Lipases
标题:Chemoenzymatic Synthesis Of Apremilast: A Study Using Ketoreductases And Lipases
摘要:在阿普雷米拉斯的化学酶合成中的关键步骤是产生手性醇(R)-1-(3-乙氧基-4-甲氧基苯基)-2-(甲磺基)乙醇,(R)-3.评估了两种酶法来获得(R)-3,一种使用酮还原酶,另一种使用脂肪酶.使用酮还原酶kred-P2-D12对1-(3-乙氧基-4-甲氧基苯基)-2-(甲磺基)乙酮(2)进行生物还原,导致(R)-3,转化率为48%,对映体过量为93% (Ee).通过利用黑曲霉脂肪酶催化,对手性纯(R)-3和4-乙酰氨基异吲哚-1,3-二酮(8)之间的反应,得到了65%的收率和67%的ee的阿普雷米拉斯.
Doi:10.21577/0103-5053.20210012

专利信息

专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

专利号:US-2006111438-A1
优先权日:2004-10-21
标 题:Asymmetric synthesis of substituted dihydrobenzofurans
发明人：GONTCHAROV ALEXANDER V; KHAFIZOVA GULNAZ; POTOSKI JOHN R; YU QING; SHAW CHIA-CHENG; STACK GARY P; ZHOU DAHUI
权利人:WYETH CORP
摘要:The present invention concerns production of a compound of the formula n n nor a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula: n n nwhere Ar, Y, R 1 , R y , R 2 , and m are as defined herein.

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-8461298-B2
优先权日:2004-11-01
标 题:Compositions and methods for modification of biomolecules
发明人：BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL
权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA
摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

专利号:US-4795828-A
优先权日:1983-01-03
标题 :Functionalized intermediate for the synthesis of alpha-functionalized derivatives and labeled conjugates of procaimamide and NAPA
发明人：BUCKLER ROBERT T; WARD FREDERICK E
权利人:MILES INC
摘要:Procainamide and N-acetylprocainamide (NAPA) immunogens, antibodies prepared therefrom, labeled conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining the respective drugs. The immunogens comprise the drugs coupled at the alpha -position of the amide side chain to an immunogenic carrier material. The labeled conjugates and synthetic intermediates similarly are alpha -position derivatives of the drugs or precursors thereof. The antibodies and labeled conjugates are particularly useful in homogeneous nonradioisotopic immunoassays for measuring the respective drugs in biological fluids such as serum.

专利号:US-9260371-B2
优先权日:2004-11-01
标题:Compositions and methods for modification of biomolecules
发明人：BERTOZZI CAROLYN RUTH; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; SLETTEN ELLEN MAY
权利人:UNIV CALIFORNIA
摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).