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CAS号19924-43-7 3-甲氧基苯乙腈 | CAS号3179-09-7 1-(3-甲氧苯基)-2-硝基乙烯 | CAS号81625-24-3 cyano(3-methoxy... | CAS号591-31-1 3-甲氧基苯甲醛 | CAS号57854-49-6 3-(3-methoxyphe... | CAS号152356-73-5 (Z)-1-(3-methox... | CAS号874-98-6 3-甲氧基苄溴 | CAS号100-84-5 间甲基苯甲醚 | CAS号75-52-5 硝基甲烷 | CAS号110339-54-3 N-(3-甲氧基苯乙基)甲酰胺 | CAS号110192-20-6 1,2,3,4-tetrahy... | CAS号110339-54-3 N-(3-甲氧基苯乙基)甲酰胺 | CAS号588-05-6 3-(2-氨基乙基)苯酚 | CAS号42923-77-3 6-甲氧基-1,2,3,4-四氢异喹啉 | CAS号34146-68-4 8-甲氧基-1,2,3,4-四氢异喹啉 | CAS号192633-74-2 2,6-dichloro-N-... | CAS号23062-91-1 PD 102807 | CAS号3458-98-8 3-(2-氨基-乙基)苯酚盐酸盐 | CAS号252061-94-2 7-苄氧四氢异喹啉 | CAS号29973-97-5 3-苄氧基苯乙胺盐酸盐间甲基苯甲醚置于aluminum (III) Chloride,N-溴代丁二酰亚胺(Nbs),Lithium Aluminium Tetrahydride,过氧化苯甲酰体系中,用 四氢呋喃,四氯化碳,乙醚,乙醇,水 用作溶剂,化学反应 6.0H,反应生成3-甲氧基苯乙胺
参考文献:新型手性超分子配体phthalaphos的铑催化烯烃不对称加氢反应
标题:新型手性超分子配体phthalaphos的铑催化烯烃不对称加氢反应
摘要:设计并合成了19个包含邻苯二甲酸二酰胺基团(phthalaphos)的由二元醇衍生的手性单亚磷酸酯的文库.在铑催化的前手性脱氢氨基酯和酰胺的对映选择性氢化中筛选了这些新的配体.文库中的几个成员显示了对甲基2-乙酰氨基丙烯酸丙烯酸酯(6个配体产生> 97%ee),对甲基(z)-2-乙酰氨基肉桂酸甲酯(6个配体产生> 94%ee)和n-(1-P乙烯基乙烯基乙酰胺(9个配体给出了95%的ee),而只有极少数代表对具有挑战性和工业相关性的底物提供了高对映选择性n-(3,4-二氢萘-1-基)乙酰胺(一种情况下为96%ee)和甲基(e)-2-(乙酰氨基甲基)-3-苯基丙烯酸酯(99%ee)在一种情况下).在大多数情况下,新的配体比其结构上相关的单齿亚磷酸酯(它们没有能够进行氢键相互作用的官能团)更具活性和立体选择性.进行的控制实验和动力学研究使我们证明了phthalaphos配体的二酰胺基团涉及的氢
Doi:10.1002/chem.201102018
海关参考信息
- 2902600000-乙苯
2905110000-甲醇
2908199090-其他酚的卤化衍生物
2908999090-其他酚的硝化衍生物 - 💡 提示:海关信息按照顺序优先匹配,如需确认的海关信息,请参考相关资料。
- 详情请参考:📖 海关编码查询和海关进出口税则
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-4727146-A
优先权日:1980-07-03
标题 :Synthesis of chiral 1-benzyl-1,2,3,4-tetra-hydroisoquinolines by asymmetric reduction
发明人:RICE KENNER C
权利人:US HEALTH
摘要:In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids. As a special function of this invention, certain of the derivatives, namely 4'-6' and 7'-9', may be hydrogenated to 1'-3' derivative by asymmetric reduction either of the catalytic or chemical type.
专利号:US-8461384-B2
优先权日:2006-12-11
标 题 :Preparation of amides from an acid and amine for intermediates in the synthesis of morphinans
发明人:WANG PETER X; MOSER FRANK W; GROTE CHRISTOPHER W; CANTRELL GARY L
权利人:WANG PETER X; MOSER FRANK W; GROTE CHRISTOPHER W; CANTRELL GARY L; MALLINCKRODT LLC
摘要:The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl 3 that is necessary to form the 3,4-dihydroisoquinoline.
专利号:US-6653087-B1
优先权日:1997-02-07
标 题 :Convergent synthesis of combinatorial library
发明人:BOGER DALE L
权利人:SCRIPPS RESEARCH INST
摘要:Targeted C2-symmetric and unsymmetric chemical libraries for use in protein and receptor homodimerization and heterodimerization are constructed by solution phase methodologies. Exemplary libraries are prepared in a 60 to 10 sub-library format by symmetrical coupling of the constructed fragments with a mixture of tethering dicarboxylic acids. In each step of the 3-step reaction sequence, the reactants, unreacted starting material, reagents and their byproducts were removed by simple liquid-liquid or liquid-solid extractions providing the desired intermediates and final libraries in multi-milligram quantities in high purities (≧90-100%) independent of the reaction yields and without deliberate reaction optimization. The synthesis of a second prototypical library employed the olefin metathesis reaction to join and combinatorially randomize the length of linker tether. This approach provides a unique opportunity to rapidly generate a statistically controlled mixture of homo and heterodimers of remarkable diversity.