专利号:US-10768157-B2 优先权日:2015-10-20 标 题:Materials and methods for the detection of trace amounts of substances in biological and environmental samples 发明人:KABIR ABUZAR; FURTON KENNETH G 权利人:KABIR ABUZAR; FURTON KENNETH G; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides chemical compositions and synthesis strategies to create molecularly imprinted polymers (MIPs) via sol-gel processes. In a specific embodiment, the subject invention utilizes a(n) organic, inorganic, or metallic template analyte to create a hybrid organic-inorganic or inorganic three-dimensional network possessing cavities complementary to the shape, size, and functional orientation of the template molecule or ions. The subject invention further pertains to the use of the novel MIPs as selective solid phase extraction (SPE) sorbents for pre-concentration and clean-up of trace substances in biological and environmental samples. Synthesis of other molecularly imprinted polymers with environmental, pharmaceutical, chemical, clinical, toxicological, and national security implications can be conducted in accordance with the teachings of the subject invention.
专利号:US-9772338-B2 优先权日:2015-10-20 标题 :Materials and methods for the detection of trace amounts of substances in biological and environmental samples 发明人:KABIR ABUZAR; FURTON KENNETH G 权利人:KABIR ABUZAR; FURTON KENNETH G; UNIV FLORIDA INT 摘要:The subject invention provides chemical compositions and synthesis strategies to create molecularly imprinted polymers (MIPs) via sol-gel processes. In a specific embodiment, the subject invention utilizes a(n) organic, inorganic, or metallic template analyte to create a hybrid organic-inorganic or inorganic three-dimensional network possessing cavities complementary to the shape, size, and functional orientation of the template molecule or ions. The subject invention further pertains to the use of the novel MIPs as selective solid phase extraction (SPE) sorbents for pre-concentration and clean-up of trace substances in biological and environmental samples. Synthesis of other molecularly imprinted polymers with environmental, pharmaceutical, chemical, clinical, toxicological, and national security implications can be conducted in accordance with the teachings of the subject invention.
专利号:US-2023183175-A1 优先权日:2020-03-16 标 题:Method for preparing intermediate for use in synthesis of florfenicol and compounds prepared thereby 发明人:LI WENSEN; ZHANG WENQI 权利人:HEADING NANJING PHARMTECHNOLOGIES CO LTD 摘要:The present invention provides a method for preparing an intermediate of florfenicol, comprising: reacting p-methylthiobenzaldehyde with isocyanoacetate under catalysis of a chiral catalyst. In the reaction, the chiral product is oxidized to form a methylsulfone-substituted product which is subsequently deformylized to obtain the intermediate. In the method of the present invention, the chiral center of the intermediate is directly generated in the first step of reaction, and the yield of the first step reaches 75%-80%, which is significantly higher than the conventional chiral resolution methods (about 40% yield), and the product has high chiral purity. The method of the present invention does not use anhydrous copper sulfate that pollutes the environment, which reduces the environmental pressure. The compound of p-methylthiobenzaldehyde and the compound of isocyanoacetate are used to react to form a chiral intermediate, which has higher material availability and efficiency than linear synthesis methods.
专利号:WO-2025056767-A1 优先权日:2023-09-15 标题 :Process for the preparation of enantiomerically enriched aliphatic amines 发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS 权利人:SYNGENTA CROP PROTECTION AG 摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.
专利号:US-5401852-A 优先权日:1989-10-20 标 题:Process for the stereochemical inversion of (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R) enantiomers 发明人:VILLA MARCO; GIORDANO CLAUDIO; CAVICCHIOLI SILVIA; LEVI SILVIO 权利人:ZAMBON SPA 摘要:Intermediates for transforming (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R)-enantiomers are described. The final compounds are useful intermediates for the synthesis of antibiotics like chloramphenicol, Thiamphenicol and Florfenicol.
专利号:US-5789599-A 优先权日:1994-05-06 标题:Aziridine compounds, methods of preparation and reactions thereof 发明人:DAVIS FRANKLIN A; ZHOU PING; REDDY GADDAMPALLY VENKAT 权利人:UNIV DREXEL 摘要:Novel N-sulfinyl-2-carboxyaziridine compounds and novel N-hydrogen-2-hydroxymethylaziridine compounds are provided. The asymmetric synthesis of N-sulfinylaziridines is readily accomplished in high diastereomeric purity and good yield by the Darzens-type reaction of the metal enolate of an α-haloester and an enantiopure sulfinimine. Ring-opening of these aziridines affords α-amino acids and the otherwise difficult to prepare syn-β-hydroxy-α-amino acids, both key structural units found in many bioactive materials. The N-sulfinyl radical may be selectively removed from the novel aziridine compounds by treatment with acid or base. Alternatively, the N-sulfinyl radical may be oxidized to provide the corresponding N-sulfonyl-aziridine, or reduced to form the corresponding 1H-2-hydroxymethylaziridine, either of which may subsequently be ring-opened to provide precursors to bioactive compounds.
1: Sandoval R, Oliver C, Valdivia S, Valenzuela K, Haro RE, Sánchez P, Olavarría VH, Valenzuela P, Avendaño-Herrera R, Romero A, Cárcamo JG, Figueroa JE, Yáñez AJ. Resistance-nodulation-division efflux pump acrAB is modulated by florfenicol and contributes to drug resistance in the fish pathogen Piscirickettsia salmonis. FEMS Microbiol Lett. 2016 Jun;363(11). pii: fnw102. doi: 10.1093/femsle/fnw102. Epub 2016 Apr 15. doi: 10.1016/j.chemosphere.2016.04.072. Epub 2016 May 6. doi: 10.1016/j.chroma.2016.04.024. Epub 2016 Apr 16. doi: 10.1080/00071668.2016.1148263. doi: 10.3389/fmicb.2016.00389. eCollection 2016. 7: Faulkner D, Cantley M, Walker M, Crooks S, Kennedy D, Elliott C. Evidence of non-extractable florfenicol residues: development and validation of a confirmatory method for total florfenicol content in kidney by UPLC-MS/MS. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2016 Jun;33(6):983-94. doi: 10.1080/19440049.2016.1175187. Epub 2016 May 20. doi: 10.1016/j.colsurfb.2016.02.027. Epub 2016 Feb 12. doi: 10.1371/journal.pone.0149100. eCollection 2016. 10: Wei CF, Chang SK, Shien JH, Kuo HC, Chen WY, Chou CC. Synergism between two amphenicol of antibiotics, florfenicol and thiamphenicol, against Staphylococcus aureus. Vet Rec. 2016 Mar 26;178(13):319. doi: 10.1136/vr.103554. Epub 2016 Feb 10. doi: 10.1016/j.talanta.2015.12.045. Epub 2015 Dec 18. doi: 10.1016/j.saa.2016.01.043. Epub 2016 Jan 25. doi: 10.1007/s11356-015-5897-1. Epub 2015 Dec 26. doi: 10.1049/iet-nbt.2015.0012. doi: 10.1136/vr.103320. Epub 2015 Dec 8. doi: 10.1111/jfd.12416. Epub 2015 Nov 3. doi: 10.1016/j.chroma.2015.09.047. Epub 2015 Sep 24. doi: 10.2460/ajvr.76.10.860. doi: 10.1111/avj.12364. Epub 2015 Sep 27.
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