专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-11512303-B2 优先权日:2017-05-27 标 题 :Engineered polypeptides and their applications in the synthesis of beta-hydroxy-alpha-amino acids 发明人:CHEN HAIBIN; BONG YONG KOY; XU QING; ZHOU AMENG; SHEN TIANRAN; YANG JIADONG; YANG ZHUHONG 权利人:ENZYMASTER NINGBO BIO ENG CO LTD 摘要:The present invention provides engineered polypeptides that are useful for the asymmetric synthesis of β-hydroxy-α-amino acids under industrial-relevant conditions. The engineered polypeptides disclosed in this invention were developed through directed evolution based on the ability of catalytic synthesis of (2S, 3R)-2-amino-3-hydroxy-3-(4-nitrophenyl) propanoic acid. The present disclosure also provides polynucleotides encoding engineered polypeptides, host cells capable of expressing engineered polypeptides, and methods of producing β-hydroxy-α-amino acids using engineered polypeptides. Compared to other processes of preparation, the use of the engineered polypeptides of the present invention for the preparation of β-hydroxy-α-amino acids results in high purity of the desired stereoisomers, mild reaction conditions, low pollution and low energy consumption. So, it has good industrial application prospects.
专利号:US-11542269-B2 优先权日:2018-01-03 标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHOI HYEONG-WOOK; FANG FRANCIS G 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:US-8410320-B2 优先权日:2010-12-07 标 题 :Method for synthesis of secondary alcohols 发明人:CHENG CHIEN-HONG; KARTHIKEYAN JAGANATHAN; HUANG PANG-CHI 权利人:CHENG CHIEN-HONG; KARTHIKEYAN JAGANATHAN; HUANG PANG-CHI; NAT UNIV TSING HUA 摘要:A method for synthesis of secondary alcohols is provided for pharmaceutical secondary alcohol by addition of organoboronic acids with aldehydes in presence of the cobalt ion and bidentate ligands as the catalyst. In addition, an enantioselective synthesis method for secondary alcohols is also herein provided in the present invention. The present invention has advantages in using less expensive cobalt ion and commercially available chiral ligands as the catalyst, wide scope of organoboronic acids and aldehydes compatible with this catalytic reaction and achieving excellent yields and/or enantiomeric excess.
专利号:US-10913749-B2 优先权日:2015-05-07 标 题 :Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:US-11136335-B2 优先权日:2016-06-30 标题:Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHASE CHARLES E; CHOI HYEONG-WOOK; ENDO ATSUSHI; FANG FRANCIS G; KIM DAE-SHIK 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
参考文献:10.1007/s10895-011-0919-y 摘要:Shanker N, Dilek O, Mukherjee K, McGee DW, Bane SL. Aurones: Small Molecule Visible Range Fluorescent Probes Suitable for Biomacromolecules. Journal of Fluorescence. 2011 Jul 12;21(6):2173. doi: 10.1007/s10895-011-0919-y.