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N-乙基马来酸置于sodium Acetate,乙酸酐体系中,化学反应生成N-乙基马来酰亚胺
参考文献:一种"摆脱平地"的方法:化学酶促合成和桥联双环化合物库的生物学分析†
标题:一种"摆脱平地"的方法:化学酶促合成和桥联双环化合物库的生物学分析†
摘要:当前通过化学合成开发药物的成功率低的主要原因是大部分准平面候选分子.因此,建议采用"逃离平地"的策略来产生生物活性化学实体.在测试该建议的首次尝试中,我们通过将一组环状二烯与一组亲二烯体结合,合成了少量的具有刚性球形核结构的桥联双环化合物.我们从平面联苯类似物开始,并通过酶促双氧合作用将其转化为羟基化的二烯结构.使用新合成的双亲性小库,将二烯通过以下途径转化为桥连自行车:Diels-Alder反应.首先基于干扰哺乳动物细胞增殖的通用测定法对所得的78个结构的集合进行生物活性测试.随后,利用一种更具机制针对性的生物活性分析方法,即利用细胞阻抗监测,以获取有关那些在增殖测定中最活跃的化合物所发挥作用方式的建议.可以确认9种候选物中的8种对蛋白酶体的抑制作用.尽管这些分子中的7个对蛋白酶体的活性显示出相对较弱的干扰,但一个候选分子却表现出中等但明显的抑制作用.考虑到化合物库的小尺寸,该结果是显着
Doi:10.1039/c5Ob02539G

专利信息

专利号:US-12012427-B2
优先权日:2019-10-31
标 题 :Synthesis of Fmoc-protected morpholino monomers and their use in the synthesis of morpholino oligomer
发明人：SINHA SURAJIT; KUNDU JAYANTA; GHOSH UJJWAL
权利人:INDIAN ASS FOR THE CULTIVATION OF SCIENCE
摘要:Present invention relates to stable Fmoc protected Morpholino monomers and corresponding oligonucleotides (PMO) and efficient synthesis of the same involving chlorophosphoramidate and H-Phosphonate chemistry. Successful syntheses of the oligonucleotide with higher yield and lesser time have been accomplished employing solid phase synthesis and easy deprotection of Fmoc group with Piperidine.

专利号:US-7041479-B2
优先权日:2000-09-06
标题 :Enhanced in vitro synthesis of active proteins containing disulfide bonds
发明人：SWARTZ JAMES ROBERT; KIM DONG-MYUNG
权利人:TRUSTESS OF THE LELAND STANFOR
摘要:Compositions and methods are provided for the enhanced in vitro synthesis of polypeptides containing disulfide bonds. In order to improve the performance of in vitro protein synthesis reactions, pre-treatment and redox buffering of the reaction mix is performed in order to optimize the redox potential. Exogenous enzymes that enhance protein folding and disulfide bond formation may also be added to the reaction.

专利号:US-2020148541-A1
优先权日:2017-06-01
标题 :An approach to a bottom-up synthesis of nanocarbons
发明人：GIDRON ORI; PHATANGARE SUNITA; DISHI OR; BEDI ANJAN
权利人:YISSUM RES DEV CO OF HEBREW UNIV JERUSALEM LTD
摘要:Provided is a method for the synthesis of a Ï€-conjugated system from oligofurans, under conditions involving cycloaddition.

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-6548276-B2
优先权日:2000-09-06
标题:Enhanced in vitro synthesis of active proteins containing disulfide bonds
发明人：SWARTZ JAMES ROBERT; KIM DONG-MYUNG
权利人:UNIV LELAND STANFORD JUNIOR
摘要:Compositions and methods are provided for the enhanced in vitro synthesis of polypeptides containing disulfide bonds. In order to improve the performance of in vitro protein synthesis reactions, pre-treatment and redox buffering of the reaction mix is performed in order to optimize the redox potential. Exogenous enzymes that enhance protein folding and disulfide bond formation may also be added to the reaction.

专利号:US-2004038331-A1
优先权日:2002-08-23
标题:Solid phase synthesis of biomolecule conjugates
发明人：REDDY M PARAMESWARA; FAROOQUI FIRDOUS; BRILLHART KURT L
摘要:Processes for the solid state phase formation synthesis of biomolecule conjugates, particularly protein-oligonucleotide conjugates are shown. One of the protein or oligonucleotide is reversibly bound to a solid substrate phase. At least one portion of each of the protein and the oligonucleotide molecules is activated with complementary activation groups. The activated protein and the activated oligonucleotide are then reacted, in a buffered solution resulting in the formation of the desired conjugate which remains reversibly bound to the substrate. The nature of the buffered solution is then modified causing the conjugate to be released from the substrate solid phase.