(S)-3-(4-Thiazolyl)-2-Benzoylaminopropanoic Acid置于盐酸体系中,化学反应 20.0H,以0.24 G的收率获得l-4-噻唑丙氨酸 参考文献:Enantioselective Synthesis Of (S)-3-(4-Thiazolyl)-2-Tert-Butoxycarbonyl-Aminopropionic Acid: A Chiral Building Block For Renin Inhibitor 标题:Enantioselective Synthesis Of (S)-3-(4-Thiazolyl)-2-Tert-Butoxycarbonyl-Aminopropionic Acid: A Chiral Building Block For Renin Inhibitor 摘要:(S)-3-(4-Thiazolyl)-2-Tert-Butoxycarbonylaminopropionic Acid (6),An Important Structural Constituent Of The Renin Inhibitor,Has Been Synthesized From (Z)-3-(4-Thiazolyl)-2-Benzoylaminoprop-2-Enoic Acid (4B) By Enantioselective Hydrogenation Using The Ru-(S)-P-Tolyl-Binap Complex As The Key Step,And Then Followed By Acid Hydrolysis And Tert-Butoxycarbonylation. Doi:10.3987/com-04-10178
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-9475837-B2 优先权日:2011-12-23 标题 :Process for the synthesis of therapeutic peptides 发明人:HURLEY FIONN; WEGNER KATARZYNA; FOLEY PATRICK 权利人:IPSEN MFG IRELAND LTD 摘要:The present invention relates to a process for the large-scale synthesis of therapeutic peptides using a Sieber Amide resin, which comprises solid-phase Fmoc-chemistry.
专利号:US-2024400608-A1 优先权日:2021-09-03 标题:Synthesis of bicycle toxin conjugates, and intermediates thereof 发明人:WITTY DAVID; LIMB DARREN; MIN BYOUNG JOON; HE LIWEN; SANDERS WILLIAM J; NNANABU ERNEST OBINNA 权利人:BRICYCLETX LTD 摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.
专利号:US-9574189-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries 发明人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK 权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS 摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
专利号:US-8932838-B2 优先权日:2010-06-17 标 题 :Biocatalysts and methods for the synthesis of (S)-3-(1-aminoethyl)-phenol 发明人:CABIROL FABIEN LOUIS; GOHEL ANUPAM; OH SEONG HO; SMITH DEREK J; WONG BRIAN; LALONDE JAMES J 权利人:CODEXIS INC 摘要:The present disclosure provides engineered transaminase polypeptides having improved properties as compared to naturally occurring transaminases including the ability of converting the substrate, 3′-hydroxyacetophenone to (S)-3-(1-aminoethyl)-phenol in enantiomeric excess and high percentage conversion. Also provided are polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to synthesize (S)-3-(1-aminoethyl)-phenol and related compounds useful in the production of active pharmaceutical ingredients.
专利号:US-8932836-B2 优先权日:2010-08-16 标 题:Biocatalysts and methods for the synthesis of (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine 发明人:LIMANTO JOHN; BEUTNER GREGORY; GRAU BRENDAN; JANEY JACOB; KLAPARS ARTIS; ASHLEY ERIC R; STROTMAN HALLENA R; TRUPPO MATTHEW D; HUGHES GREGORY; CABIROL FABIEN; GOHEL ANUPAM; COLLIER STEVEN J; LIANG JACK; MOCK MARISSA; MUNDORFF EMILY; NOVICK SCOTT; SMITH DEREK 权利人:LIMANTO JOHN; BEUTNER GREGORY; GRAU BRENDAN; JANEY JACOB; KLAPARS ARTIS; ASHLEY ERIC R; STROTMAN HALLENA R; TRUPPO MATTHEW D; HUGHES GREGORY; CABIROL FABIEN; GOHEL ANUPAM; COLLIER STEVEN J; LIANG JACK; MOCK MARISSA; MUNDORFF EMILY; NOVICK SCOTT; SMITH DEREK; CODEXIS INC 摘要:The disclosure provides transaminase polypeptides capable of converting the substrate, 2-(3,4-dimethoxyphenethoxy)cyclohexanone to the trans diastereomer product (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine in at least a 2:1 diastereomeric ratio relative to the cis diastereomer (1R,2S)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine. The disclosure also provides polynucleotides, vectors, host cells, and methods of making and using the transaminase polypeptides in processes for preparing (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine and its analogs, which can product compounds can be further used to prepare the aminocyclohexylether compound, (3R)-1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]pyrrolidin-3-ol, which is an ion channel blocker.
1: Mennen SM, Blank JT, Tran-Dubé MB, Imbriglio JE, Miller SJ. A peptide-catalyzed asymmetric Stetter reaction. Chem Commun (Camb). 2005 Jan 14;(2):195-7. Epub 2004 Nov 29.
合成参考文献
参考文献:10.1038/s42004-022-00625-3 摘要:Zhang G, Brown JS, Quartararo AJ, Li C, Tan X, Hanna S, Antilla S, Cowfer AE, Loas A, Pentelute BL. Rapid de novo discovery of peptidomimetic affinity reagents for human angiotensin converting enzyme 2. Communications Chemistry. 2022 Jan 19;5(1):8. doi: 10.1038/s42004-022-00625-3.