专利号:WO-2023233371-A1 优先权日:2022-06-03 标 题:A continuous flow process for synthesis of organic azides 发明人:GNANAPRAKASAM BOOPATHY; PANDEY AKANKSHA M; MONDAL SHANKHAJIT 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES PUNE IISER PUNE 摘要:The present disclosure relates generally to the field of synthetic organic chemistry. More specifically, the disclosure is directed to a continuous flow process for synthesis of azides from alcohols and peroxides, wherein the process comprises azidation with trimethylsilyl azide and a catalyst Amberlyst-15. It is a non-hazardous, mild and controlled reaction giving good yields of azides. The azides can be further employed for synthesis of medicinally and industrially useful chemicals.
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-2024181781-A1 优先权日:2023-02-27 标 题:Substrate for synthesis of biological polymers having anti-aggregation function and biological polymer synthesis method using same 发明人:JANG MYOUNG HOON; CHOI JAE SUN 权利人:SP2 TX INC 摘要:The present invention relates to a substrate for the synthesis of biological polymers having an anti-aggregation function, and a biological polymer synthesis method using the substrate. The substrate according to an aspect may have anti-aggregation functionality to enable high-yield and high-purity processes in the synthesis of biological polymers.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:WO-2016056031-A1 优先权日:2014-10-08 标题:Novel diol compounds synthesis and its use for formal synthesis of (2r, 3 s)-3-hydroxypipecolic acid 发明人:CHAVAN SUBHASH PRATAPRAO; PAWAR KAILASH PRALHAD 权利人:COUNCIL SCIENT IND RES 摘要:The patent discloses novel diol derivatives of general formula I, [Formula should be inserted here] A chiral pool process for the synthesis of the compound of formula I from D glucose. Further, it discloses a process for the synthesis of (2 R , 3 S )-3-hydroxypipecolic acid from D- glucose using chiral pool approach, wherein the D-glucose used is in enantiomerically pure form.
专利号:WO-9707129-A1 优先权日:1995-08-18 标题 :Solution synthesis of peripheral acting analgesic opioid tetrapeptides 发明人:RINALDI NICHOLAS 权利人:IAF BIOCHEM INT; RINALDI NICHOLAS 摘要:This invention provides a bulk scale process for the solution synthesis of enantiomerically pure peripherally acting analgesic opioid tetrapeptides corresponding to formula (I): Tyr-(D)R1-R2-R3-NH2, where R1 is Ala or Arg; R2 is Phe or Phe(p-F); and R3 is Phe or Phe(p-F). A new and unique multi-step process is disclosed comprising the joining of two dipeptides using standard solution phase synthesis techniques, but adjusting the individual factors (e.g., solvents, activating agents, neutralizing agents etc.), to minimize racemization of the second amino acid. Tremendous cost efficiencies are achieved due to elimination of traditional sequential blocking-deblocking cycles and multiple chromatographic purification steps, which also enables these simple kilogram quantity methods to be scaled up to commercial production.
摘要:Trofimova, A.; Sirvinskas, M.; Yudin, A. K., Science of Synthesis Knowledge Updates, (2021) 2, 81. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 320. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 354. 摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2014) 4, 319. 摘要:Sainsbury, M., Science of Synthesis Knowledge Updates, (2010) 1, 251.