专利号:WO-2008151306-A1 优先权日:2007-06-05 标题 :Synthesis of cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity 发明人:PETTIT GEORGE R; SMITH THOMAS H; FENG SONG 权利人:UNIV ARIZONA; PETTIT GEORGE R; SMITH THOMAS H; FENG SONG 摘要:The present invention is directed to effective methods of synthesizing cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity. Total syntheses of the eighteen-membered ring cyclodepsipeptides kitastatin (1a) and respirantin (1b) are taught. One important step in the synthesis is an intramolecular transesterification of the ?-ketoester alcohol 6 to afford the protected macrocycle 5. The synthetic products were shown to be identical to the natural products and the absolute stereochemistry of 6 of the 7 asymmetric centers of cyclodepsipeptide 1b was unequivocally established. Kitastatin (1a) and respirantin (1b) were found to be remarkable inhibitors of cancer cell growth and are related to the antimycin family of antibiotics.
专利号:US-2009123983-A1 优先权日:2007-10-03 标 题:Processes for preparing an intermediate of sitagliptin via enzymatic reduction 发明人:NIDDAM-HILDESHEIM VALERIE 权利人:NIDDAM-HILDESHEIM VALERIE 摘要:The invention provides enzymatic reduction processes for the preparation of 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate, particularly, (S)-methyl 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate, a key intermediate in the synthesis of Sitagliptin, and the (S)- and (R)-enantiomers of methyl 4-(2,4,5-trifluorophenyl)-3-hydroxybutanoate in high enantiomeric purity.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-12157908-B2 优先权日:2019-02-25 标 题:Cell-free protein synthesis platforms derived from clostridia extracts 发明人:JEWETT MICHAEL CHRISTOPHER; KRUGER-GERICKE ANTJE; MUELLER ALEXANDER PAUL; KOEPKE MICHAEL 权利人:UNIV NORTHWESTERN; LANZATECH INC 摘要:Disclosed are compositions, methods, and kits for performing cell-free RNA transcription and/or cell-free protein synthesis (CFPS). The disclosed compositions, methods, and kits include or utilize components prepared from a species of Clostridia such as cellular extracts from Clostridium autoethanogenum.
专利号:EP-0830136-B1 优先权日:1995-03-07 标 题:New cryptophycins from synthesis 发明人:MOORE RICHARD E; TIUS MARCUS A; BARROW RUSSELL A; LIANG JIAN; CORBETT THOMAS H; VALERIOTE FREDERICK A; HEMSCHEIDT THOMAS K; GOLAKOTI TRIMURTULU 权利人:UNIV HAWAII; UNIV WAYNE STATE 摘要:Novel cryptophycin compounds are disclosed, together with methods of producing cryptophycins by total synthesis and methods for the use of such cryptophycins in pharmaceuticals to inhibit the proliferation of mammalian cells and to treat neoplasia.
专利号:US-6013626-A 优先权日:1993-12-21 标题 :Cryptophycins from synthesis 发明人:MOORE RICHARD E; TIUS MARCUS A; BARROW RUSSELL A; LIANG JIAN; CORBETT THOMAS H; VALERIOTE FREDERICK A; GOLAKOTI TRIMURTULU; HEMSCHEIDT THOMAS K 权利人:UNIV HAWAII; UNIV WAYNE STATE 摘要:A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods of producing cryptophycins by total synthesis and methods of using cryptophycins in pharmaceuticals. It is a further object of this invention to use cryptophycins to inhibit the proliferation of mammalian cells. Moreover, methods of using cryptophycins to treat neoplasia is also provided.
参考标题:First Total Synthesis Of Cyclic Pentadepsipeptides Hikiamides A-C 作者:Donglin Fu,Xuemin Rao,Jinyi Xu,Genzoh Tanabe,Osamu Muraoka,Xiaoming Wu,Weijia Xie |发布日期:2018.7 摘要:The First Total Syntheses Of Naturally Occurring Cyclodepsipeptides Hikiamides A-C Are Described. The Key Linear Pentapeptide Precursors, Prepared Efficiently Via Fmoc-Solid-Phase Synthesis, Were Cyclized In Dilute Solution To Provide The Target Hikiamides A-C. The Structures Of The Synthetic Hikiamides A-C Were Characterized By Nmr And Hrms Spectroscopy Which Were In Agreement With Those Of Natural
合成参考文献
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