CAS: 19774-82-4; (2-Butylbenzofuran-3-yl)(4-(2-(Diethylamino)Ethoxy)-3,5-Diiodophenyl)Methanone Hydrochloride

该化合物是一种强效的三级抗心律剂,主要用于治疗严重的心血管和超子体心律不齐,其化学结构包括碘,具有独特的药理特性,包括长期行动潜在时间和耐腐期,化合物显示钠和钾渠道被封锁,以及无竞争力的肾上腺抑制,其高脂溶解性导致组织分布广泛,长期消除半衰期,从而能够产生持续的治疗效果.氨碘酸盐因其在生殖性心律不齐症(包括结构性心脏病)中的功效而特别受到重视.然而,由于甲状腺机能障碍和肺毒性等潜在不利影响,其使用需要仔细监测.适当的剂量和病人评估对于取得最佳效果至关重要.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

2-chloro-N,N-diethylethylamine hydr°Chloride 2-n-butyl-3-(3',5'-diiodo-4'-hydroxybenzoyl)benzofuran 2-n-butylbenzo[b]furan methyl 2-(2-formylphenoxy)hexanoate4-Hydroxyamiodarone (+/-)-{4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl}[2-(3-hydroxybutyl)benzofuran-3-yl]methanone hydr°Chloride

合成工艺路线路线简述

  • 合成目标产物 Amiodarone Hydrochloride 主要起始原料 2-Diethylaminoethylchloride Hydrochloride And 2-Butyl-3-(3,5-Diiodo-4-Hydroxy Benzoyl) Benzofuran
  • (文献来源)合成步骤主要原料 2-Diethylaminoethylchloride Hydrochloride 和 2-Butyl-3-(3,5-Diiodo-4-Hydroxy Benzoyl) Benzofuran
2-丁基苯并呋喃置于甲醇,Iron(III) Chloride,碘,Potassium Carbonate,Sodium Hydroxide体系中,用 水,1,2-二氯乙烷,甲苯 用作溶剂,化学反应 17.0H,反应生成盐酸胺碘酮
参考文献:一种制备盐酸胺碘酮的方法
标题:一种制备盐酸胺碘酮的方法
摘要:本发明公开一种制备盐酸胺碘酮的方法,包括:以2‑丁基苯并呋喃和对乙酰氧基苯甲醛为原料,在lewis酸催化以及加热条件下发生aldol反应,产物在碘和碱存在的条件下同时发生羟基氧化,脱乙酰基以及碘代反应,之后产物和n,N‑二乙基氯乙胺反应,成盐,得到盐酸胺碘酮.该方法只需要催化量lewis酸的使用,不需要强酸性氯化铝的参与,反应条件更加温和,副产物少,易于后处理,三废大大减少;整个路线的操作简单,所用试剂都便宜易得,无毒害,非常适用于工业化生产.

海关参考信息

专利信息


专利号:US-11390890-B2
优先权日:2015-02-15
标 题:Dibasic organic acid producing strain and preparation and application of same
发明人:TIAN CHAOGUANG; LI JINGEN; LONG CHUANNAN; SUN TAO; LIN LIANGCAI; XU JING; LIU QIAN; JI JINGXIAO; SUN WENLIANG; MA YANHE
权利人:TIANJIN INST IND BIOTECHNOLOGY CAS
摘要:Provided are an engineered strain for synthesizing a dibasic organic acid and preparation and application of same. The engineered strain introduces or up-regulates expression of a positive regulator gene for synthesis of a dibasic organic acid, and/or down-regulates expression of a negative regulator gene for synthesis of a dibasic organic acid, as compared with the origin strain of the engineered strain, the producing capability for producing the dibasic organic acid is improved. The dibasic organic acid comprises malic acid, succinic acid, fumaric acid, oxaloacetic acid, glutaric acid, and adipic acid; the expression product of the positive regulator gene comprises aspartate aminotransferase, glutamic acid-aspartate transporter, C4-dicarboxylic acid transporter, pyruvate carboxylase and malate dehydrogenase, glucose transporter; the expression product of the negative regulatory gene comprises succinyl-CoA synthase, and malic acid-alpha ketoglutarate transporter, and the original strain comprises Myceliophthora thermophila, Thielavia terrestris, Aspergillus , and Rhizopus.

专利号:US-6187756-B1
优先权日:1996-09-05
标 题 :Composition and methods for treatment of neurological disorders and neurodegenerative diseases
发明人:LEE ROBERT K K; WURTMAN RICHARD J
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:It has been discovered that the stimulation of β-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising β-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by β-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E 2 (PG E 2 ), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of β-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E 2 , forskolin, or nicotine ditartrate is inhibited by immunosuppressants or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.

专利号:US-6469055-B2
优先权日:1996-09-05
标题 :Compositions and methods for treatment of neurological disorders and neurodegenerative diseases
发明人:LEE ROBERT K K; WURTMAN RICHARD J
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:It has been discovered that the stimulation of β-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising β-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by β-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E 2 (PG E 2 ), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of β-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E 2 , or forskolin is inhibited by immunosuppressants, immunophilin ligands, or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.

专利号:US-2007203079-A1
优先权日:2005-11-21
标题:Methods of using small molecule compounds for neuroprotection
发明人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG
权利人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG
摘要:Methods are provided for preventing neurodegeneration and neuronal loss by administering compositions comprising small molecule compounds with the effect of preventing neurodegeneration and neuronal loss. In one aspect of the invention, the methods and compositions are also useful for treating neurodegenerative diseases. Small molecule compounds provide an important treatment option because of their stability, ease of use in both manufacture and formulation, ease of administration, and patient compliance. The small molecule compound compositions of the present invention may include topoisomerase II inhibitors, bacterial transpeptidase inhibitors, calcium channel antagonists, cyclooxygenase inhibitors, folic acid synthesis inhibitors, or sodium channel blockers and functional analogues thereof that have an effect on neurodegeneration. The compositions of the present invention may be administered prophylactically before the onset of clinical symptoms or after clinical symptoms of a neurodegenerative disease have manifested.

专利号:CN-114671836-B
优先权日:2021-12-30
标题 :Synthesis method of amiodarone impurity C

专利号:CN-111747913-A
优先权日:2020-07-15
标 题 :Synthesis method of deuterated amiodarone hydrochloride
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✅ COA系统入驻 | 共享模式

主要参考文献


1: Karkhanis A, Tram NDT, Chan ECY. Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acids. Biochem Pharmacol. 2017 Dec 15;146:188-198. doi: 10.1016/j.bcp.2017.09.012. Epub 2017 Sep 25. doi: 10.1007/s00228-017-2195-5. Epub 2017 Jan 12.

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.
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