CAS: 548-73-2; 1-(1-(4-(4-Fluorophenyl)-4-Oxobutyl)-1,2,3,6-Tetrahydropyridin-4-yl)-1H-Benzo[d]Imidazol-2(3H)-One

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CAS号60373-72-0 1-(p-Fluorophen...

📜3-[1-[3-[2-(4-Fluorophenyl)-1,3-Dioxolan-2-Yl]Propyl]-3,6-Dihydro-2H-Pyridin-4-Yl]-1H-Benzimidazol-2-One置于盐酸体系中,用 甲醇 作为反应溶剂,化学反应 1.5H,以300 Mg的收率获得产物氟哌利多
参考文献:Rearrangement Of Spiro-Benzimidazolines: Preparation Of N-Alkenyl-And N-Alkyl-Benzimidazol-2-Ones
标题:Rearrangement Of Spiro-Benzimidazolines: Preparation Of N-Alkenyl-And N-Alkyl-Benzimidazol-2-Ones
摘要:A Synthetically Useful Protocol Has Been Developed For The Preparation Of Highly Functionalized N-Alkenyl-Benzimidazol-2-Ones. Reaction Of Commercially Available O-Phenylenediamines With Variously Substituted Cyclic Ketones Provides Spiro-Benzimidazolines. Treatment Of These Spiro-Benzimidazolines With Triphosgene In The Presence Of Potassium Carbonate Results In Rapid Rearrangement And Formation Of N-Alkenyl-Benzimidazol-2-Ones In Modest To Excellent Yield For The Two-Step Sequence. Extension Of This Methodology Toward The Preparation Of A M Opiate Receptor Antagonist And Droperidol,A Potent Antiemetic And Antipsychotic Agent,Currently A Marketed Pharmaceutical Is Also Described. Upon Treatment Of Spiro-Benzimidazolines With Triphosgene In The Presence Of Sodium Triacetoxyborohydride,N-Alkyl-Benzimidazol-2-Ones Were Formed. (C) 2007 Merck & Co.,Inc. Published By Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Tet.2007.06.106

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-4310535-A
优先权日:1976-11-30
标题:Combination of drugs and a method for the selective control of the immune reactions evoked in a host by the administration of antigens
发明人：PIERPAOLI WALTER
权利人:PIERPAOLI WALTER
摘要:The invention concerns a new composition or combination of drugs effective to selectively control the immune reactions which are evoked in a host by the administration of antigens. It comprises active components capable of simultaneously blocking the alpha -adrenergic receptors of the cells for catecholamine, blocking the dopaminergic receptors of the cells and increasing the synthesis of serotonin. Preferred drug combinations according to the invention contain in association phentolamine, haloperidol, L-5-hydroxy-tryptophane and possibly dopamine.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:WO-9925385-A1
优先权日:1997-11-17
标 题:A method of increasing nucleic acid synthesis with ultrasound
发明人：UNGER EVAN C; MCCREERY THOMAS; SADEWASSER DAVID
权利人:IMARX PHARMACEUTICAL CORP
摘要:The present invention is directed to a method of increasing nucleic acid synthesis in a cell comprising administering to the cell a therapeutically effective amount of ultrasound for a therapeutically effective time such that said administration of said ultrasound results in said increased nucleic acid synthesis. The nucleic acid sequence may comprise an endogenous sequence or an exogenous sequence.

专利号:US-9365532-B1
优先权日:2011-02-14
标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines
发明人：ISAACMAN STEVEN
权利人:ISAACMAN STEVEN; NANOMETICS LLC
摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.

专利号:US-2019031650-A1
优先权日:2016-01-29
标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies
发明人：HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN
权利人:UNIV YALE
摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.