CAS: 10457-90-6; Bromperidol

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CAS号114361-10-3 4-[4-hydroxy-4-... | CAS号366-77-8 3-(4-氟苯甲酰)丙酸

4-<4-<4-(Trimethylstannyl)Phenyl>-4-Hydroxypiperidino>-4'-Fluorobutyrophenone置于溴体系中,用 氯仿 用作溶剂,化学反应 0.5H,以79%的收率获得溴哌利多
参考文献:Synthesis Of High Specific Activity [75Br]-And [77Br]Bromperidol And Tissue Distribution Studies In The Rat
标题:Synthesis Of High Specific Activity [75Br]-And [77Br]Bromperidol And Tissue Distribution Studies In The Rat
摘要:A Rapid Synthesis Of [75Br]-And [77Br]Bromperidol With Specific Activity Exceeding 10000 Ci/mmol Is Described In Which A Trimethylstannylated Analogue Of Bromperidol Is Used As A Substrate For Regiospecific No-Carrier-Added Radiobromination. 4-[4-[4-(Trimethylstannyl)Phenyl]-4-Hydroxypiperidino]-4'-Fluorobutyrophenone Was Synthesized By The Reaction Of (Trimethylstannyl)Sodium With Haloperidol And Purified By Preparative HPLC. Subsequent Radiobromination With No-Carrier-Added 75Br-Or 77Br-And In Situ Oxidation Using H2O2/ch3Cooh Gave A Corrected Radiochemical Yield Of 35% With A 30-Min Preparation Time. Tissue Distribution Studies In The Rat Show A Rapid And Prolonged Uptake Into The Brain,Liver,And Kidneys And Consistently Low Blood Concentrations That Differ Quantitatively From Previous Studies Using Relatively Low Specific Activity Bromperidol. Potential Clinical Applications For This High Specific Activity Radiobrominated Neuroleptic Are Discussed.
Doi:10.1021/jm00147A035

专利信息

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

专利号:US-8143437-B2
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
发明人：GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

专利号:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

专利号:US-2005239725-A1
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof

专利号:US-2023271983-A1
优先权日:2020-07-29
标题 :Functionalized isonitriles and products, preparation and uses thereof
发明人：SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
权利人:UNIV SANTIAGO COMPOSTELA
摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.