专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:US-9938509-B2 优先权日:2010-12-08 标 题 :Biocatalysts and methods for the synthesis of armodafinil 发明人:ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN 权利人:CODEXIS INC 摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.
专利号:US-11571456-B2 优先权日:2017-05-23 标题 :Process for the linear synthesis of gram-positive class II bacteriocins and compositions and uses thereof 发明人:BÉDARD FRANÇOIS; BIRON ÉRIC; HAMMAMI RIADH; FLISS ISMAIL 权利人:UNIV LAVAL 摘要:A process for the linear synthesis of a gram-positive class II bacteriocin or a variant thereof is disclosed herein. The process comprises the stepwise addition of selected amino acids to a solid support; pseudoproline positioning and reopening; and cleavage of the gram-positive class II bacteriocin or the variant thereof from the solid support to provide a linear gram-positive class II bacteriocin or variant thereof; and in situ disulfide bond formation. Various applications and uses of the synthetic bacteriocins are also disclosed. The synthetic process can also be used to synthesize variants of bacteriocins by the selective substitution of one or more amino acids and/or additions and/or deletions of selected amino acids.
专利号:US-2023337702-A1 优先权日:2017-05-23 标 题 :Process for the linear synthesis of gram-positive class ii bacteriocins and compositions and uses thereof 发明人:BÉDARD FRANÇOIS; BIRON ÉRIC; HAMMAMI RIADH; FLISS ISMAIL; RENAUD ARIANE; DALLAIRE LAURENT 权利人:UNIV LAVAL 摘要:A process for the linear synthesis of a gram-positive class II bacteriocin or a variant thereof is disclosed herein. The process comprises the stepwise addition of selected amino acids to a solid support; pseudoproline positioning and reopening; and cleavage of the gram-positive class II bacteriocin or the variant thereof from the solid support to provide a linear gram-positive class II bacteriocin or variant thereof; and in situ disulfide bond formation. Various applications and uses of the synthetic bacteriocins are also disclosed. The synthetic process can also be used to synthesize variants of bacteriocins by the selective substitution of one or more amino acids and/or additions and/or deletions of selected amino acids.
专利号:US-7459443-B2 优先权日:1999-04-08 标 题 :Synthesis of biologically active compounds in cells 发明人:SERGEEV PAVEL 权利人:SERGEEV PAVEL 摘要:This invention relates to a new method of synthesis of biologically active substances of determined structure directly in the cells of living organisms containing specific RNA or DNA molecules of determined sequence. The method is based on the hybridization of two or more oligomers bound with biologically inactive precursors of biologically active substances to specific RNA or DNA in vivo in the cells of living organisms. After hybridization of the oligomers to RNA or DNA the biologically inactive precursors bound to the 5′ and/or 3′ ends of the oligomers can interact with each other to make biologically active form of the substances. This changing of properties is due to chemical reactions which bind the biologically inactive precursors through a chemical bond into a biologically active form of the whole compound.
专利号:WO-9105050-A1 优先权日:1989-09-29 标题 :Synthesis of mature human parathyroid hormone 发明人:SUNG WING L 权利人:CANADA MAJESTY IN RIGHT OF 摘要:A nucleotide coding sequence for human parathyroid hormone has been synthesized, which sequence results in a substantially higher yield of mature PTH than hitherto could be obtained. This is achieved by providing a synthesized nucleotide sequence coding for mature human PTH or a biologically active analog, wherein the amino terminal coding sequence is adenine-rich. A sequence wherein the degenerate codons for some or all of amino acids 1 through 5 are adenine-rich is preferred.
摘要:Kaneda, K.; Mitsudome, T., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 344. 参考文献:10.1038/s41467-021-24482-1 摘要:Wu P, Chen D, Ding W, Wu P, Hou H, Bai Y, Zhou Y, Li K, Xiang S, Liu P, Ju J, Guo E, Liu J, Yang B, Fan J, He L, Sun Z, Feng L, Wang J, Wu T, Wang H, Cheng J, Xing H, Meng Y, Li Y, Zhang Y, Luo H, Xie G, Lan X, Tao Y, Li J, Yuan H, Huang K, Sun W, Qian X, Li Z, Huang M, Ding P, Wang H, Qiu J, Wang F, Wang S, Zhu J, Ding X, Chai C, Liang L, Wang X, Luo L, Sun Y, Yang Y, Zhuang Z, Li T, Tian L, Zhang S, Zhu L, Chang A, Chen L, Wu Y, Ma X, Chen F, Ren Y, Xu X, Liu S, Wang J, Yang H, Wang L, Sun C, Ma D, Jin X, Chen G. The trans-omics landscape of COVID-19. Nature Communications. 2021 Jul 27;12(1):4543. doi: 10.1038/s41467-021-24482-1.