2,2,2-三氯-1-(4-(二甲氨基)苯基)乙醇置于aqueous Alkali体系中,化学反应生成对二甲氨基苯甲醛 参考文献:Technology And Gender: Thomas I. Voire And The Case Of The Peeping Tom 标题:Technology And Gender: Thomas I. Voire And The Case Of The Peeping Tom 摘要: Doi:10.1111/j.1533-8525.2002.Tb00056.X
专利信息
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-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-12404534-B1 优先权日:2024-10-29 标题:Method for separating amoxicillin and phenylacetic acid from reaction solution in one-step enzymatic synthesis of amoxicillin 发明人:YANG ZHONGHUA; YIN XIAOYAN 权利人:XINGZHI COLLEGE ZHEJIANG NORMAL UNIV 摘要:A method for separating amoxicillin and phenylacetic acid from reaction solution in one-step enzymatic synthesis of amoxicillin is provided. The method employs immobilized penicillin acylase mutant to catalyze the one-step synthesis of amoxicillin from penicillin potassium, and develops a separation process for the resulting reaction mixture. The technical scheme mainly comprises: Firstly separating the immobilized penicillin acylase mutant from the reaction solution through filtration; subsequently isolating amoxicillin via crystallization; followed by separating and recovering phenylacetic acid through toluene extraction and back extraction. This separation method enables rapid and efficient isolation of amoxicillin with high production yield, achieving an average crystallization rate of 93.22%. Concurrently, it demonstrates effective separation and recovery of phenylacetic acid while allowing recyclable use of the toluene extractant.
专利号:US-6159673-A 优先权日:1996-07-17 标 题:Oxonol compound, light-sensitive material and process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which Z is an atomic group that forms a cyclic amide ring; each of W1 and W2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.
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.
专利号:US-2023279562-A1 优先权日:2021-12-30 标题 :Process for the Electrochemical Synthesis of Ammonia (NH3) and the Ammonia Produced Thereby 发明人:GHORAI UTTAM KUMAR; PAUL SOURAV; ADALDER ASHADUL; SARKAR SOUGATA 权利人:GHORAI UTTAM KUMAR; RAMAKRISHNA MISSION VIDYAMANDIRA 摘要:This invention relates to a process for the electrochemical synthesis of ammonia (NH3) and the ammonia produced thereby. Ammonia is synthesized by the electrochemical reduction of nitrogenous materials such as nitrogen or nitrates (NO3-) using metal phthalocyanine such as iron phthalocyanine (FePc) or β-cobalt phthalocyanine (CoPc) or iron phthalocyanine-molybdenum disulfide (FePc-MoS2) or cobalt phthalocyanine- carbon nitride (CoPc-C3N4) catalyst at very low pressure and room temperature by applying low potential.
参考文献:10.1186/1476-511x-10-116 摘要:An HM, Park SY, Lee DK, Kim JR, Cha MK, Lee SW, Lim HT, Kim KJ, Ha NJ. Antiobesity and lipid-lowering effects of Bifidobacterium spp. in high fat diet-induced obese rats. Lipids in Health and Disease. 2011 Jul 12;10(1):116. doi: 10.1186/1476-511x-10-116. 参考文献:10.1107/s1600536811006234 摘要:Fischer J, Schmitt V, Schollmeyer D, Detert H. Monoclinic polymorph of 2,5-bis[4-(dimethyl-amino)-styr-yl]-3,6-dimethyl-pyrazine. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o875. 参考文献:10.1107/s1600536811019234 摘要:Li Y, Wang H, Chen H, Chen LT, Liu J. 9-{[4-(Dimethyl-amino)-benz-yl]amino}-5-(3,4,5-trimeth-oxy-phen-yl)-5,5a,8a,9-tetra-hydro-furo[3',4':6,7]naphtho-[2,3-d][1,3]dioxol-6(8H)-one. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1538–9. 参考文献:10.1007/s11671-008-9132-6 摘要:Li X, Zhang L, Mu J, Qiu J. Fabrication and Properties of Porphyrin Nano- and Micro-particles with Novel Morphology. Nanoscale Research Letters. 2008 May 21;3(5):169. doi: 10.1007/s11671-008-9132-6.