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-9305065-A1 优先权日:1991-08-30 标 题:Preparation of peptides by a solid-phase synthesis and intermediates therefor 发明人:SHARMA RAM PRAKASH 权利人:PORTON DEV LTD 摘要:The invention relates to the preparation of polypeptides by solid phase synthesis by attachment of carboxy-protected amino acids to the carboxyl end of a peptide chain bound at its N-terminal to a solid support. The carboxy-protection is by a tertiary alkoxy silyl group. Novel tertiary alkoxy silyl amino acid esters are disclosed which may be used as intermediates.
专利号:US-2012282652-A1 优先权日:2011-02-28 标题 :Preparation of peptide mixtures by protease catalysis designed to provide useful biological and physical properties 发明人:GROSS RICHARD A; VISWANATHAN KODANDARAMAN; QIN XU 权利人:GROSS RICHARD A; VISWANATHAN KODANDARAMAN; QIN XU; POLITECHNIC INST UNIV NEW YORK 摘要:A process for preparing unique peptide mixtures with a broad range of uses using combinations of natural and non-natural amino acid alkyl ester monomers and specific combinations of these monomers as dimers, trimers and higher oligomers selected from the large group of structural motifs that lead to useful physical and/or biological properties and that have been or may be identified from solid state peptide synthesis, isolation of peptides from natural sources, and production of peptides by recombinant DNA methods, or identification of peptides by recombinant methods such as phage display, the method of peptide synthesis comprising a) admixing one or more natural and non-natural amino acid alkyl ester monomer, dimer, trimer and higher oligomers with one or more proteases in a reaction medium; b) heating the mixture to between about 5° C. to about 90° C. for between 5 minutes and 24 hours; and c) recovering the formed oligopeptide.
专利号:US-2006252134-A1 优先权日:1999-10-29 标 题 :Enantioselective oligomerization of alpha-hydroxy carboxylic acids and alpha-amino acids 发明人:LORBERT STEVE; SCHASTEEN CHARLES S; URAIZEE FAROOQ; KAPILA SHUBHENDER 权利人:NOVUS INT INC 摘要:An enzymatic synthesis and composition of oligomers and co-oligomers comprised of α-hydroxy carboxylic acids and α-amino acids or peptides is disclosed. In a preferred embodiment, a α-hydroxy carboxylic acid with a specific chiral configuration is linked by an amide linkage to a α-amino acid specific with a specific chiral configuration or linked by an amide linkage to a peptide made up of α-amino acid monomers having identical chiral configurations. Proteolytic enzymes catalyze oligomerization of the α-hydroxy carboxylic acid and α-amino acid. The degree and distribution of oligomerization varies upon the type and concentrations of different reaction mixtures utilized and upon the length of allowed reaction time. The resultant oligomers may be provided to animals such as ruminants as bioavailable amino acid supplements that are resistant to degradation in the rumen and other animals such as swine, poultry and aquatic animals.
专利号:US-2023151034-A1 优先权日:2020-03-17 标题:Peptidomimetic n5-methyl-n2-(nonanoyl-l-leucyl)-l-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds as inhibitors of norovirus and coronavirus replication 发明人:JACOBSON IRINA C; LEE SAM SK; PIZARRO NOVOA JUAN CARLOS 权利人:COCRYSTAL PHARMA INC 摘要:Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and B1 to B66; tables A to E).
专利号:US-6939693-B2 优先权日:1999-10-29 标 题 :Enantioselective oligomerization of α-hydroxy carboxylic acids and α-amino acids 发明人:LORBERT STEPHEN J; SCHASTEEN CHARLES S; NAM PAUL K S; FORCINITI DANIEL; RAJESH MATHUR P; KAPILA SHUBHENDER 权利人:NOVUS INT INC 摘要:An enzymatic synthesis and composition of oligomers and co-oligomers comprised of α-hydroxy carboxylic acids and α-amino acids or peptides is disclosed. In a preferred embodiment, a α-hydroxy carboxylic acid with a specific chiral configuration is linked by an amide linkage to a α-amino acid specific with a specific chiral configuration or linked by an amide linkage to a peptide made up of α-amino acid monomers having identical chiral configurations. Proteolytic enzymes catalyze oligomerization of the α-hydroxy carboxylic acid and α-amino acid. The degree and distribution of oligomerization varies upon the type and concentrations of different reaction mixtures utilized and upon the length of allowed reaction time. The resultant oligomers may be provided to animals such as ruminants as bioavailable amino acid supplements that are resistant to degradation in the rumen and other animals such as swine, poultry and aquatic animals.
1: Gao NY, Banwell MG, Willis AC. Biomimetic Total Synthesis of the Pentacyclic Amaryllidaceae Alkaloid Derivative Gracilamine. Org Lett. 2017 Jan 6;19(1):162-165. doi: 10.1021/acs.orglett.6b03465. Epub 2016 Dec 12.
合成参考文献
摘要:R.W. Hay and L.J. Porter. J. Chem. Soc., B 1967, 1261.