专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-4118386-A 优先权日:1977-04-04 标 题:Synthesis of imidazo[1,5-a]diazepine-3-carboxylates 发明人:WALSER ARMIN 权利人:HOFFMANN LA ROCHE 摘要:A process to produce diazepine-3-carboxylates of the formula ##STR1## is selected from the group consisting of ##STR2## R 6 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, and lower alkanoyl; n R 4 is lower alkyl; R 3 is selected from the group consisting of phenyl, mono-substituted phenyl, disubstituted phenyl, pyridyl and mono-substituted pyridyl; and R 2 is hydrogen or lower alkyl which comprises reacting a compound of the formula ##STR3## wherein R 1 is of the formula ##STR4## AND R 5 is lower alkyl with a compound of the formula n n Nâ•?C-CH.sub.2 --COOR.sub.4 n n in the presence of a base sufficiently strong to generate the anion of the isocyanoacetate.
专利号:EP-1105392-B1 优先权日:1999-06-30 标 题:Process for the preparation of imidazodiazepine intermediates 发明人:DHAON MADHUP K; LABIB PARVIS; DAVIS DEBORAH A; ESSER GRANT L 权利人:ABBOTT LAB 摘要:The present invention relates to a process for the synthesis of a compound having formula XI, from a compound of formula X.
参考文献:10.1016/j.bmcl.2008.05.065 摘要:Cheng P, Zhang Q, Ma YB, Jiang ZY, Zhang XM, Zhang FX, Chen JJ. Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives. Bioorg Med Chem Lett. 2008 Jul 01;18(13):3787–9. doi: 10.1016/j.bmcl.2008.05.065.