CAS: 73231-34-2; 2,2-Dichloro-N-((1R,2S)-3-Fluoro-1-Hydroxy-1-(4-(Methylsulfonyl)Phenyl)Propan-2-yl)Acetamide

该化合物是一种抗生素,对各种动物物种中的克菌阳性细菌和克菌阴性细菌都有效,其广谱活动和强效杀菌特性使其适合治疗家禽,牲畜和伴动物的细菌感染. 该产品在管理途径上提供了灵活性,包括水药和注射.

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欧盟法规

ECHA物质C&L通报

上下游产品

CAS号535-15-9 二氯乙酸乙酯 | CAS号116-54-1 二氯乙酸甲酯 | CAS号76639-93-5 氟甲砜霉素胺 | CAS号51458-28-7 甲砜霉素杂质 1 | CAS号79-36-7 二氯乙酰氯 | CAS号1069118-16-6 3-(dichloroacet... | CAS号1106981-80-9 3-(dichloroacet... | CAS号1106981-83-2 3-(dichloroacet...

合成工艺路线路线简述

  • 合成目标产物 Florfenicol 主要起始原料 Oxazole, 2-(Dichloromethyl)-4-(Fluoromethyl)-4,5-Dihydro-5-[4-(Methylsulfonyl)Phenyl]-, (4S,5R)-
  • (文献来源)合成步骤主要原料 Oxazole, 2-(Dichloromethyl)-4-(Fluoromethyl)-4,5-Dihydro-5-[4-(Methylsulfonyl)Phenyl]-, (4S,5R)-
甲砜霉素置于氯化亚砜,Triethylamine Tris(Hydrogen Fluoride),三乙胺体系中,用 二氯甲烷,1,2-二氯乙烷 作为反应溶剂,化学反应 13.0H,反应生成 氟苯尼考
参考文献:酮还原酶的动态还原动力学拆分不对称合成氟苯尼考
标题:酮还原酶的动态还原动力学拆分不对称合成氟苯尼考
摘要:化学酶促合成:氟苯尼考的制备方法是利用酶促动态还原动力学拆分(dyrkr)来建立顺式1,2-氨基醇中间体的两个立体中心,其ee大于99%,非对映体比率(dr)为99% .用et 3 N-3Hf处理氮丙啶和环硫酸盐可以高区域选择性地引入氟原子.
DOI:10.1002/ejoc.201800658

海关参考信息

专利信息


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.
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主要参考文献


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.

合成参考文献


参考文献:10.1155/2011/824104
摘要:Cao H, He S, Wei R, Diong M, Lu L. Bacillus amyloliquefaciens G1: A Potential Antagonistic Bacterium against Eel‐Pathogenic Aeromonas hydrophila. Evidence-Based Complementary and Alternative Medicine. 2011 Jan;2011(1). doi: 10.1155/2011/824104.
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