CAS: 24729-96-2; (2R,3R,4S,5R,6R)-6-((1S,2S)-2-Chloro-1-((2S,4R)-1-Methyl-4-Propylpyrrolidine-2-Carboxamido)Propyl)-4,5-Dihydroxy-2-(Methylthio)Tetrahydro-2H-Pyran-3-Yl Dihydrogen Phosphate

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CAS号21462-39-5 盐酸克林霉素

以 水 用作溶剂,化学反应 8.0H,以92%的收率获得克林霉素磷酸酯
参考文献:三氮唑在合成克林霉素磷酸酯中的应用
标题:三氮唑在合成克林霉素磷酸酯中的应用
摘要:本发明涉及一种三氮唑在合成克林霉素磷酸酯中的应用,该应用中用三氮唑代替吡啶和三乙胺,使三氮唑,三氯氧磷和式i化合物在溶剂中进行磷酯化反应获得式ii化合物溶液.三氮唑的应用使合成克林霉素磷酸酯的方法更高效,成本低,节能环保,所得克林霉素磷酸酯的收率高,纯度高.

专利信息

专利号:US-2015182634-A1
优先权日:2012-12-28
标 题:Molecular Design and Chemical Synthesis of Pharmaceutical-Ligands and Pharmaceutical-Pharmaceutical Analogs with Multiple Mechanisms of Action
发明人：COYNE CODY P; BEAR RYAN; JONES TONI
权利人:COYNE CODY P; BEAR RYAN; JONES TONI
摘要:Multi-phase and single-phase chemical reaction schemes have been developed for the synthesis of pharmaceutical-ligand analogs, pharmaceutical-pharmaceutical analogs, and similar molecular-molecular analogs that possess multiple mechanisms of action. The multi-phase organic chemical reaction schemes include relatively mild reaction conditions, high end product yields, and comparatively rapid completion of chemical reactions, which are all of particular utility for the synthesis of preparations including covalent pharmaceutical-receptor ligand or pharmaceutical-immunoglobulin analogs. Examples of pharmaceutical-ligand preparations that can be synthesized utilizing the multi-step chemical reaction schemes include covalent chemotherapeutic-ligand agents that possess selective targeted delivery properties and a capacity to exert additive and synergistic levels of cytotoxic anti-neoplastic potency. Pharmaceutical-pharmaceutical analogs, including chemotherapeutic-chemotherapeutic analogs that are capable of exerting multiple mechanisms of action, can be synthesized using either of the described multi-phase or single-phase organic chemistry reaction schemes. Each of these representative examples has utility against a spectrum of disease states including, for example, neoplastic conditions such as mammary adenocarcinoma/carcinoma, ovarian carcinoma, prostatic carcinoma, intestinal carcinoma, melanoma, leukemia, myeloma, and lymphoma.

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人：CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

专利号:US-10933051-B2
优先权日:2017-06-09
标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
发明人：CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
权利人:FOB SYNTHESIS INC
摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

专利号:US-9693999-B2
优先权日:2011-01-26
标题:Small molecule RNase inhibitors and methods of use
发明人：DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

专利号:US-6106846-A
优先权日:1995-09-19
标题 :Use of at least one thermal spring water from Vichy as a substance P antagonist
发明人：BRETON LIONEL; LECLAIRE JACQUES; DE LACHARRIERE OLIVIER
权利人:SOCIETEL OREAL S A
摘要:The present invention relates to the use of at least one thermal spring water from the Vichy basin as substance P antagonist in a cosmetic composition or for the preparation of a pharmaceutical composition. The invention also relates to the use of at least one thermal spring water from the Vichy basin in a cosmetic composition or for the preparation of a pharmaceutical composition, more especially a dermatological composition, intended for treating disorders associated with excessive synthesis and/or release of substance P.