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CAS号6228-73-5 环丙酰胺 | CAS号13021-02-8 1-硝基环丙烷 | CAS号73330-91-3 环丙基氨基甲酸甲酯 | CAS号1759-53-1 环丙甲酸 | CAS号3187-77-7 Cyclopropanamin... | CAS号13324-66-8 N-环丙基苄胺 | CAS号75-19-4 环丙烷 | CAS号60-29-7 乙醚 | CAS号10026-13-8 五氯化磷 | CAS号51761-72-9 (Z)-1-环丙基乙酮肟 | CAS号1090815-16-9 N-Cyclopropyl 4... | CAS号110931-74-3 N-(1-naphthylme... | CAS号110192-06-8 N-chlor°Cyclopr... | CAS号402959-34-6 N-B°C-(1S)-3-[3... | CAS号4747-72-2 异氰酰基环丙烷 | CAS号385382-48-9 5-溴-N-环丙基烟酰胺 | CAS号401589-92-2 N-环丙基-3-硝基苯磺酰胺 | CAS号56541-14-1 N-环丙基硫代脲 | CAS号50908-62-8 5'-(N-环丙基)甲酰氨基腺苷 | CAS号1453-50-5 Cyclopropanecar...1-硝基环丙烷置于三乙胺体系中,用 水 作为反应溶剂,化学反应 6.0H,以91%的收率获得产物环丙胺
参考文献:聚甲基氢硅氧烷衍生的钯纳米粒子,用于水中脂肪族和芳香族硝基化合物的化学和区域选择性氢化†
标题:聚甲基氢硅氧烷衍生的钯纳米粒子,用于水中脂肪族和芳香族硝基化合物的化学和区域选择性氢化†
摘要:通过使用环保的氢化剂聚甲基氢硅氧烷,在nap-氧化镁载体上高效聚硅氧烷稳定的" Pd"纳米颗粒,已经实现了将多种脂族,不饱和,芳族和杂芳族硝基化合物进行化学和区域选择性加氢成相应的胺的作用. [pmhs]在水中.通过还原nap-Mg-Pdcl 4制备高度稳定且活性高的pd纳米颗粒用作还原剂和封端剂的pmhs.在nap-Mgo催化剂上分散非常好的钯纳米颗粒在二硝基苯氢化成相应的硝基苯胺中也显示出极好的区域选择性.该催化剂在氢化反应期间具有抗烧结的高耐久性,并且可以在不损失其活性的情况下重复使用.
DOI:10.1039/c4Ra01333F
专利信息
专利号:US-5977301-A
优先权日:1992-09-24
标题 :Synthesis of N-substituted oligomers
发明人:ZUCKERMAN RONALD N; KERR JANICE M; KENT STEPHEN B H; MOOS WALTER H; SIMON REYNA J; GOFF DANE A
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
专利号:EP-0671928-B1
优先权日:1992-09-24
标题 :Synthesis of n-substituted oligomers
发明人:ZUCKERMANN RONALD N; KERR JANICE M; KENT STEPHEN BRIAN HENRY; MOOS WALTER H; SIMON REYNA J; GOFF DANE A
权利人:CHIRON CORP
摘要:Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R<9>) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using the automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-2006287520-A1
优先权日:2005-05-16
标 题 :Synthesis of salinosporamide A and analogues thereof
发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI
权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI
摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-7910623-B2
优先权日:2005-07-22
标 题 :Synthesis of scabronines and analogues thereof
发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P
权利人:SLOAN KETTERING INST CANCER
摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:WO-2012047907-A9
优先权日:2010-10-04
标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto
发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.