2-硝基-1,3-茚二酮置于氯仿,水,溴体系中,化学反应生成 N-羟基邻苯二甲酰亚胺 参考文献:Wanag; Wanag,Doklady Akademii Nauk Sssr,1953,Vol. 90,P. 59,61 标题:Wanag; Wanag,Doklady Akademii Nauk Sssr,1953,Vol. 90,P. 59,61
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:WO-2020248278-A1 优先权日:2019-06-14 标题:Method for continuous synthesis of substituted benzoic-acid organic substance 发明人:HONG HAO; ZHANG ENXUAN; LU JIANGPING; LIU ZHIQING; LI CHAO; TANG YANG 权利人:JINLIN ASYMCHEM LABORATORIES CO LTD 摘要:The present invention provides a method for the continuous synthesis of a substituted benzoic-acid organic substance. The continuous synthesis method comprises: in the presence of catalyst and organic solvent, the organic matter represented by formula (I) and oxygen are continuously inputted to a continuous reaction apparatus for continuous oxidation reaction to obtain a substituted benzoic-acid organic substance, which is discharged continuously, the substituted benzoic-acid organic substance having the structure represented by formula (II). Oxygen is a green reagent and is inexpensive and readily available; a large amount of wastewater, waste gas, and solid waste is not generated after the reaction, and the system is easy to handle. The use of a continuous reaction operation can reduce the risk of flash distillation and explosion of solvent due to a high concentration of oxygen in a batch reaction. Under the same oxidation conditions, the continuous preparation process can reduce the escape of oxygen, greatly increasing the oxygen utilization rate and also simplifying the operation, improving the safety of the reaction and the yield of the substituted benzoic-acid organic substance.
专利号:US-11059849-B2 优先权日:2014-09-02 标题 :Modified nucleotides for synthesis of nucleic acids, a kit containing such nucleotides and their use for the production of synthetic nucleic acid sequences or genes 发明人:YBERT THOMAS; GARIEL SYLVAIN 权利人:DNA SCRIPT 摘要:A modified nucleotide, intended for the synthesis of long chain nucleic acids by enzymatic processes, comprising a “naturalâ€? nitrogenous base or a natural nitrogenous base analogue, a ribose or deoxyribose carbohydrate, and at least one phosphate group, characterized in that said nucleotide comprises at least one R group, termed the modifier group, carried by said nitrogenous base or analogue and/or by the oxygen in position 3′ of the ribose or deoxyribose molecule, making it possible to block the polymerization of said nucleotide and/or to allow the interaction of said nucleotide with another molecule, such as a protein, during the nucleic acid synthesis, R comprising at least one functional terminal group.
专利号:US-7288661-B2 优先权日:2003-12-10 标 题 :Process for the synthesis of (2S,3aS,7aS)-1-[(S)-alanyl]-octahydro-1H-indole-2-carboxylic acid compounds and application in the synthesis of perindopril 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of compounds of formula (I): n nwherein R represents a hydrogen atom or a protecting group for the amino function.n n Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-2019177392-A1 优先权日:2014-09-23 标 题 :Synthesis of glp-1 peptides 发明人:PENIAS NAVON SHARON; NAVEH SHIRLY; VASILEIOU ZOI; BARLOS KONSTANTINOS 权利人:NOVETIDE LTD 摘要:Disclosed are processes for the synthesis of GLP-1 peptides, such as liraglutide and semaglutide, and a process for purifying liraglutide.