CAS: 42399-41-7; (2S,3S)-5-(2-(Dimethylamino)Ethyl)-2-(4-Methoxyphenyl)-4-Oxo-2,3,4,5-Tetrahydrobenzo[b][1,4]Thiazepin-3-Yl Acetate

该化合物是一种主要用于治疗高血压和腹肌切除物的钙管阻塞器,其功能是阻止钙离子流入心脏和光滑肌肉细胞,导致血管变异和心率下降.Dltiazem被归类为苯并亚津衍生物,并表现出抗anginal和抗血压性能.该物质通常在各种配方中施用,包括口服药片和静脉注射.其药用动力学涉及广泛的肝代谢,其半衰期相对较短,需要多剂量才能产生持续治疗效果.常见副作用可能包括眩晕,头痛和胃肠炎.Dltiazem在患有严重低温或心脏病等某些症状的病人中具有反射作用.

结构式图片

上下游产品

CAS号42399-40-6 去乙酰地尔硫卓 | CAS号108-24-7 乙酸酐 | CAS号4584-46-7 二甲氨基氯乙烷盐酸 | CAS号33286-22-5 盐酸地尔硫卓 | CAS号99109-07-6 methyl (2S,3S)-... | CAS号696-62-8 4-碘苯甲醚 | CAS号24393-56-4 对甲氧基肉桂酸乙酯 | CAS号137-07-5 2-氨基苯硫酚 | CAS号182268-43-5 Ethyl threo-3-(... | CAS号42399-40-6 去乙酰地尔硫卓 | CAS号84903-82-2 去乙酰-O-去甲基地尔硫卓

合成工艺路线路线简述

  • 合成目标产物 Diltiazem 主要起始原料 Ethyl 4-Methoxycinnamate
  • (文献来源)合成步骤主要原料 Ethyl 4-Methoxycinnamate

海关参考信息

专利信息


专利号:US-10889599-B2
优先权日:2018-02-27
标 题:1,1-diborylalkyl-1-metal compounds, preparation method thereof, and their applications toward synthesis of 1,1-diboronate ester compounds
发明人:CHO SEUNG HWAN; LEE YEOSAN
权利人:POSTECH ACAD IND FOUND
摘要:The present invention relates to a 1,1-diborylalkyl-1-metal compound including one metal group together with two identical boron groups at the sp3 carbon center, and its use. Specifically, the present invention relates to development of novel organic reactions, synthesis of functional molecules, and synthesis of new drugs by applying the novel 1,1-diboryl-1-metal substituted alkyl compounds to various molecular libraries which could not be synthesized by conventional methodologies.

专利号:US-7452994-B2
优先权日:2001-09-12
标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
发明人:MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN
权利人:ANORMED INC
摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.

专利号:US-5545568-A
优先权日:1992-09-14
标题:Solid phase and combinatorial synthesis of compounds on a solid support
发明人:ELLMAN JONATHAN A
权利人:UNIV CALIFORNIA
摘要:Methods, compositions, and devices for synthesizing combinatorial libraries of various useful compounds, such as benzodiazepines, prostaglandins, β-turn mimetics and glycerol-derived drugs is described. In order to expediently synthesize such combinatorial libraries of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. This disclosure thus also describes an important extension of solid phase synthesis methods to nonpolymeric organic compounds.

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:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-4937334-A
优先权日:1988-07-26
标题:Process for the preparation of intermediates for the synthesis of diltiazem
发明人:CAVICCHIOLI SILVIA; PAIOCCHI MAURIZIO; GIORDANO CLAUDIO
权利人:ZAMBON SPA
摘要:A process for the preparation of the compound (2S,3S)(+)-3-hydroxy-2,3-dihydro-2-(4-methoxyphenyl)-5-(2-dimethylaminoethyl)-1, 5-benzothiazepin-4(5H)-one is described. Said compound is an intermediate useful in the synthesis of Diltiazem.
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主要参考文献


1: Wang L, Cheng Z, Gu Y, Peng D. Short-Term Effects of Verapamil and Diltiazem in the Treatment of No Reflow Phenomenon: A Meta-Analysis of Randomized Controlled Trials. Biomed Res Int. 2015;2015:382086. doi: 10.1155/2015/382086. Epub 2015 Oct 4. Review.
2: Sajid MS, Whitehouse PA, Sains P, Baig MK. Systematic review of the use of topical diltiazem compared with glyceryltrinitrate for the nonoperative management of chronic anal fissure. Colorectal Dis. 2013 Jan;15(1):19-26. doi: 10.1111/j.1463-1318.2012.03042.x. Review. doi: 10.1111/j.1346-8138.2010.00858.x. Review. Review. Review. Spanish. doi: 10.1517/14656560802694739 . Review. Epub 2007 Sep 11. Review. Review. Review. Italian. Review. Review. Review. Review. Russian. Review. Review. Review. Review. Review. Review.
20: Beleslin DB, Prostran MS, Jovanović-Mićić D. [Pharmacology--new therapy. Calcium channel blockers: new aspects of therapeutic use of diltiazem]. Srp Arh Celok Lek. 1992 May-Jun;120(5-6):188-92. Review. Serbian.

合成参考文献


参考文献:10.1177/0961203309355298
摘要:Llamas-Velasco M, Eguren C, Santiago D, García-García C, Fraga J, García-Diez A. Calcinosis cutis and Sjögren's syndrome. Lupus. 2010 May;19(6):762–4. doi: 10.1177/0961203309355298.
摘要:Shayeda, Gannu R, Palem CR, Rao YM. Development of novel bioadhesive buccal formulation of diltiazem: in vitro and in vivo characterization. PDA J Pharm Sci Technol. 2009 Sep;63(5):401–8.
参考文献:10.4061/2011/132405
摘要:Tedla FM, Brar A, Browne R, Brown C. Hypertension in Chronic Kidney Disease: Navigating the Evidence. International Journal of Hypertension. 2011;2011():1–9. doi: 10.4061/2011/132405.
参考文献:10.1111/j.2042-7158.2010.01224.x
摘要:Sarti F, Barthelmes J, Iqbal J, Hintzen F, Bernkop-Schnürch A. Intestinal enzymatic metabolism of drugs. J Pharm Pharmacol. 2011 Mar;63(3):392–9. doi: 10.1111/j.2042-7158.2010.01224.x.
参考文献:10.2147/tcrm.s12701
摘要:Samalin L, Garnier M, Llorca PM. Clinical potential of lurasidone in the management of schizophrenia. Ther Clin Risk Manag. 2011;7():239–50.
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