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-3988307-A 优先权日:1974-09-06 标题 :Solid phase synthesis of peptides with carboxyl-terminal amides 发明人:GROSS ERHARD 权利人:US HEALTH 摘要:The method of utilizing α,β-unsaturated amino acids, acyl, and N-acyl derivatives as linking agents in the solid phase synthesis of peptides with the corresponding production of carboxyl terminal amides. Preferred unsaturated amino acids are dehydroalanine and dehydrobutyrine which are constituents in naturally occurring amides such as nisin and subtilin. The synthesis follows conventional lines of R. B. Merrifield et al including blocking of the amino nitrogen, with the exception that the release agent contains an amount of water equimolar to the reactant α,β-unsaturated amino acid.
专利号:WO-2023030278-A1 优先权日:2021-08-30 标题:Full-liquid-phase synthesis method for reelin drug 发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN 权利人:HUNAN SANTAI PHARMACEUTICAL CO LTD 摘要:Provided is a full-liquid-phase synthesis method for a reelin drug, belonging to the technical field of medicine synthesis. A liquid-phase method is used to synthesize 'Trp-Ser-Tyr' fragments, 'R5-Leu' fragments, 'PYR-His' fragments, and 'Arg-Pro-Gly-NH2' respectively, wherein R=D-Trp, Gly or D-2-NAL; and a reelin drug is synthesized in a '3+2+2+3' fragment condensation manner. The method has the characteristics of low reaction costs, non use of toxic reagents, a high product yield, and high purity, and is environmentally friendly, and is thus suitable for large-scale production.
专利号:WO-9610036-A1 优先权日:1994-09-27 标题 :A process for the quantitative synthesis of 3-(l-pyroglutamyl)-l-thiazolidine-4-carboxylic acid and derivatives thereof
专利号:US-7910774-B2 优先权日:2004-08-31 标题:Alternative synthesis of renin inhibitors and intermediates thereof
专利号:IT-MI941955-A1 优先权日:1994-09-27 标 题:'QUANTITATIVE SYNTHESIS OF 3- (L-PIROGLUTAMIL) -L-THIAZOLIDIN-4- CARBOXYLIC ACID AND ITS DERIVATIVES'