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-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.
专利号:US-9567308-B1 优先权日:2015-07-23 标 题:Process for the synthesis of chlorzoxazone 发明人:BOGOGNA LUIGI; CICIONE LAVINIA; BAROZZA ALESSANDRO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of chlorzoxazone (1) from 4-chloro-2-aminophenol and ethyl chloroformate in the presence of a base. n n n n n n n n n n The process is particularly advantageous because it uses ethyl chloroformate instead of triphosgene, a highly dangerous reagent that releases phosgene and must be handled with extremely strict procedures to guarantee the safety of operators in industrial facilities. n Ethyl chloroformate allows the possibility of working with a number of solvents, including water. n The yield and purity of the product obtained are very high.
专利号:US-2014378538-A1 优先权日:2011-12-14 标 题:Methods of responding to a biothreat 发明人:BANCEL STEPHANE 权利人:MODERMA THERAPEUTICS INC 摘要:The present disclosure provides for devices, in particular mobile devices, which may be used in the synthesis of modified nucleic acid molecules, in particular modified mRNA molecules. The device for making the modified nucleosides, modified nucleotides and modified nucleic acids (e.g., mRNA) disclosed herein may be mobile devices comprising at least one sample block for insertion of one or more sample vessels, a device base with electronic control units for the sample block, a voltage supply, and one or more reagent(s) for the synthesis of at least one nucleic acid.
专利号:US-2021062179-A1 优先权日:2015-02-26 标题 :Microsomal bioreactor for synthesis of drug metabolites 发明人:KRISHNAN SADAGOPAN; WALGAMA CHARUKSHA THAMEERA; NERIMETLA RAJASEKHARA REDDY 权利人:UNIV OKLAHOMA STATE 摘要:Reusable microsomal biocatalytic systems (bioreactors) constructed on carbon nanostructure modified electrodes are provided. The bioreactors comprise stable, biologically active immobilized enzymes such as human cytochromes P 450 (CYPs) and their redox partner proteins, e.g. CYP-NADPH (reduced nicotinamide adenine dinucleotide phosphate) reductases (CPR), on the carbon nanostructure surface. The immobilized enzymes may be present in liver microsomes, such as human liver microsomes (HLM) or as bactosomes, S9 fractions, etc. The bioreactors are used, for example, for synthesizing metabolites of interest from compounds such as drugs that are catabolized by the enzymes.
1: Bedada SK, Neerati P. Resveratrol Pretreatment Affects CYP2E1 Activity of Chlorzoxazone in Healthy Human Volunteers. Phytother Res. 2015 Dec 17. doi: 10.1002/ptr.5549. [Epub ahead of print] doi: 10.4103/2230-973X.167689. 3: Tang P, Li S, Wang L, Yang H, Yan J, Li H. Inclusion complexes of chlorzoxazone with β- and hydroxypropyl-β-cyclodextrin: Characterization, dissolution, and cytotoxicity. Carbohydr Polym. 2015 Oct 20;131:297-305. doi: 10.1016/j.carbpol.2015.05.055. Epub 2015 Jun 4. doi: 10.3109/00498254.2014.985760. Epub 2014 Nov 19. doi: 10.4103/2229-516X.136789. 6: Yurdakul S, Yurdakul M. FT-IR, FT-Raman spectra, and DFT computations of the vibrational spectra and molecular geometry of chlorzoxazone. Spectrochim Acta A Mol Biomol Spectrosc. 2014 May 21;126:339-48. doi: 10.1016/j.saa.2014.02.156. Epub 2014 Mar 12. doi: 10.1016/j.talanta.2013.06.058. Epub 2013 Jul 4. doi: 10.1212/WNL.0b013e3182a55f6d. Epub 2013 Aug 23. doi: 10.1093/chromsci/bms125. Epub 2012 Jul 26. doi: 10.1371/journal.pone.0053038. Epub 2013 Jan 2.
合成参考文献
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