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-2012165520-A1 优先权日:2010-12-23 标题:Process for the synthesis of prodrugs of opioids 发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
专利号:WO-2021035382-A1 优先权日:2019-08-23 标题:Method forcontinuous synthesis of 2-cyclopentene-1-one 发明人:HONG HAO; LU JIANGPING; BAO DENGHUI; YUAN LONG; WANG BO 权利人:LIAONING ASYMCHEM LABORATORIES CO LTD 摘要:Provided is a method for the continuous synthesis of 2-cyclopenten-1-one. The continuous synthesis method comprises: loading a catalyst in a continuous reaction device, then continuously conveying cyclopentene, an oxidant and a solvent into the continuous reaction device for an oxidation reaction, and continuously discharging 2-cyclopentene-1-one. In the presence of the catalyst and the solvent, cyclopentene is used as a starting material, and same is directly oxidized by the oxidant, which can avoid the generation of a large amount of halogen-containing three wastes; at the same time, the entire continuous synthesis process is carried out in the continuous reaction device, which can effectively inhibit the occurrence of safety risks during scale-up production; in addition, after the reaction is complete, the product system of the oxidation reaction can be simply concentrated to obtain the target product (2-cyclopenten-1-one). Thus, the purity (up to 98% and above) and separation rate (up to 79%) of the product are greatly improved, and production can be easily scaled up.
专利号:US-7199257-B1 优先权日:1999-06-10 标题 :Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide 发明人:SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; BOR ADAM; DEMETER ADAM; TRISCHLER FERENC; HORVATH JANOS; BRLIK JANOS 权利人:RICHTER GEDEON VEGYESZET 摘要:A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.
专利号:US-8084007-B2 优先权日:2004-01-30 标题 :Methods of synthesis of isotropically enriched borohydride and methods of synthesis of isotropically enriched boranes 发明人:SPIELVOGEL BERNARD; COOK KEVIN S 权利人:SPIELVOGEL BERNARD; COOK KEVIN S; SEMEQUIP INC 摘要:The invention provides new methods for the synthesis of isotopically enriched metal borohydrides, metal tetrahydroundecaborate salts, and decaborane from isotopically enriched 10 B-boric acid or 11 B-boric acid. The invention is particularly useful for synthesis of isotopically enriched sodium or lithium borohydride, MB 11 H 14 (where M is Li, Na, K, or alkylammonium), and decaborane.
专利号:US-2008086013-A1 优先权日:2006-06-15 标 题:Carbometallation of alkynes and improved synthesis of uniquinones 发明人:LIPSHUTZ BRUCE H 权利人:UNIV CALIFORNIA 摘要:Methods for the carbometallation of alkynes are presented. Those are useful for the synthesis of CoQ 10 and other ubiquinones as well as for the synthesis of ubiquinol analogs.
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