📜乙胺,L-脯氨酸置于吡啶,二氯二甲基硅烷,盐酸体系中,用 水 作为反应溶剂,化学反应 3.0H,以83.1%的收率获得产物l-脯氨酰胺乙酯盐酸盐 参考文献:One-Step Facile Synthesis Of L-Proline Ethylamide Hydrochloride 标题:One-Step Facile Synthesis Of L-Proline Ethylamide Hydrochloride 摘要: DOI:10.1007/s10593-014-1474-7
专利号:WO-2023030277-A1 优先权日:2021-08-30 标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog 发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN 权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD 摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.
专利号:US-8013117-B2 优先权日:2005-11-25 标 题 :Solution-phase synthesis of leuprolide and its intermediates 发明人:KADZIMIRSZ DANIEL; JAS GERHARD; AUTZE VOLKER 权利人:NANOKEM S A 摘要:A process for producing a nonapeptide leuprolide and an intermediate N-protected oligopetides, wherein at least one peptide bond of the compound is formed by reacting an activated carboxylic acid and an amine component in a continuous flow.
专利号:US-11420997-B2 优先权日:2018-04-13 标题:Peptide synthesis method 发明人:SUZUKI HIDEAKI; MUTO SUSUMU; FUJITA SHUJI; KUBO DAISUKE 权利人:JITSUBO CO LTD 摘要:The present invention has an object of shortening the process time and reducing use of a poor solvent for solidifying a carrier (Tag)-peptide component, by removing impurities without conducting solid-liquid separation (condensation, solid-liquid separation and drying operation) of a Tag-peptide component, in an Fmoc method using a Tag for liquid phase peptide synthesis. Provided is the peptide synthesis method that includes the following steps a-d: step a: a carrier-protected amino acid, carrier-protected peptide, or a carrier-protected amino acid amide, and an N-Fmoc-protected amino acid or an N-Fmoc-protected peptide are condensed in an organic solvent or a mixed solution of organic solvents, to obtain an N-Fmoc-carrier-protected peptide, step b: a water-soluble amine is added to the reaction solution after the condensation reaction, step c: the Fmoc group is deprotected from the protected amino group in the presence of a water-soluble amine, and step d: the reaction solution is neutralized by adding an acid, and further, by adding and washing with an acidic aqueous solution, then, by liquid-liquid separation an aqueous layer is removed to obtain an organic layer.
专利号:US-2009005535-A1 优先权日:2005-11-25 标题:Solution-Phase Synthesis of Leuprolide and Its Intermediates
专利号:CN-114181285-A 优先权日:2021-12-31 标题 :A kind of method of solid-liquid synthesis of nafarelin