CAS: 298-57-7; 1-Benzhydryl-4-Cinnamylpiperazine

该化合物是一种化学化合物,被归类为氟他利衍生物,主要用作抗口炎和抗乳素,其化学配方为C26H28N2, 其结构复杂,包括二苯甲基组和氟他利环.辛那利因具有抑制钙渠道的能力,有助于有效治疗运动病和脊椎病,表现出中度的亲脂性,允许其跨过血液脑屏障,这对...

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3-Phenylpropenol diphenylmethylpiperazine 3-phenyl-propenal 1-phenylpropadienecinnarizin * γ-cyclodextrin complex 1-benzhydryl-4-(3,3-diphenyl-propyl)-piperazine 36H39Cl3N4O4SC36H39Cl3N4O4S 36H39Cl3N4O4SC36H39Cl3N4O4S

合成工艺路线路线简述

  • 合成目标产物 Stugeron 主要起始原料 Cinnamyl Alcohol And 1-Benzhydrylpiperazine
  • (文献来源)合成步骤主要原料 Cinnamyl Alcohol 和 1-Benzhydrylpiperazine
肉桂醛置于triscarbonyl-(η4-3,4-Bis(4-Methoxyphenyl)-2,5-Diphenylcyclopenta-2,4-Dienone)Iron,氢气体系中,用 硝基甲烷,乙醇,甲苯 用作溶剂,80.0~130.0 °C,506.66 Kpa 条件下,反应 60.0H,反应生成桂利嗪
参考文献:直接从烯丙醇中进行铁催化的烯丙基胺化反应
标题:直接从烯丙醇中进行铁催化的烯丙基胺化反应
摘要:已经证明,使用有效且区域特异性的分子铁催化剂,无需任何路易斯酸活化剂即可直接从醇中进行烯丙基胺化反应.使用各种胺和醇,并且反应通过氧化/还原(氧化还原)途径进行.从肉桂醇生产出的副产品中显示了肉桂醇和萘替芬等普通药物的直接一步合成.
Doi:10.1002/chem.201505214

海关参考信息

专利信息


专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:WO-2025136243-A1
优先权日:2023-12-20
标题:Mechanochemical synthesis of histamine h1-receptor antagonists
发明人:AYDONAT SIMAY; OZEL MERTCAN; YIGITBASI JOANNA MARIANNA; BAYTEKIN BILGE; COLACINO EVELINA
权利人:IHSAN DOGRAMACI BILKENT UNIV; CENTRE NAT RECH SCIENT
摘要:The present invention relates to mechanochemical synthesis of histamine antagonists which are benzhydryl ethers and unsymmetrically disubstitutes piperazines and salts thereof. Said antihistamine active pharmaceutical ingredients can be diphenhydramine hydrochloride, cyclizine hydrochloride and diphenylpyraline hydrochloride. These antihistamines are used in the treatment of allergies, hives, hay fever (allergic rhinitis), conjunctivitis, reactions to insect bites and sings, nausea, motion sickness, insomnia.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人:MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-6603003-B2
优先权日:2000-11-07
标 题 :Method for the preparation of piperazine and its derivatives
发明人:SEBASTIAN SONNY; PATEL HETAL VIRENDRA; THENNATI RAJAMANNAR
权利人:SUN PHARMACEUTICAL IND LTD
摘要:A novel method for the synthesis of piperazine and its derivatives of formula 1,wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms;R1 is selected from hydrogen, a methyl group, a phenyl group optionally substituted with an alkyl group having 1 to 6 carbon atoms, or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; andR2 is selected from hydrogen, or a methyl group, or a fluoromethyl group;comprising the steps:a. reacting an ester of formula 11 with substituted or unsubstituted ethylenediamine of formula 7 to give 3,4-dehydropiperazine-2-one and its derivatives of formula 12, wherein R, R1, R2 are as defined above and R6 is a C1 to C4 linear or branched alkyl group; andb. reacting the 3,4-dehydro-piperazine-2-one and its derivatives of formula 12 with a reducing agent to yield the piperazine and its derivatives of formula 1.

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人:DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
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主要参考文献


1: Lamie NT, Monir HH. Simultaneous Determination of Cinnarizine and Dimenhydrinate in Binary Mixture Using Chromatographic Methods. J Chromatogr Sci. 2016 Jan;54(1):36-42. doi: 10.1093/chromsci/bmv103. Epub 2015 Sep 8. doi: 10.1021/acs.molpharmaceut.5b00498. Epub 2015 Sep 30. doi: 10.1016/j.saa.2015.05.048. Epub 2015 May 27. doi: 10.1007/s10072-015-2270-6. Epub 2015 Jun 3. doi: 10.1016/j.saa.2015.01.033. Epub 2015 Jan 28. doi: 10.1159/000438705. Epub 2015 Aug 12. doi: 10.1016/bs.podrm.2015.01.001. Epub 2015 Apr 1. Review. doi: 10.1016/j.ejpb.2014.08.011. Epub 2014 Sep 6. Review.
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合成参考文献


参考文献:10.1038/ncb3255
摘要:Lin R, Elf S, Shan C, Kang HB, Ji Q, Zhou L, Hitosugi T, Zhang L, Zhang S, Seo JH, Xie J, Tucker M, Gu TL, Sudderth J, Jiang L, Mitsche M, DeBerardinis RJ, Wu S, Li Y, Mao H, Chen PR, Wang D, Chen GZ, Hurwitz SJ, Lonial S, Arellano ML, Khoury HJ, Khuri FR, Lee BH, Lei Q, Brat DJ, Ye K, Boggon TJ, He C, Kang S, Fan J, Chen J. 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. Nat Cell Biol. 2015 Nov;17(11):1484–96.
摘要:Ross et al. JASMS 2022; 33; 1061-1072. DOI:10.1021/jasms.2c00111
摘要:https://pubs.acs.org/doi/abs/10.1021/acs.analchem.7b01709
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