CAS: 103745-39-7; 5-((1,4-Diazepan-1-yl)Sulfonyl)Isoquinoline

该化合物是一种药剂,主要因其作为包括滑动肌肉收缩和细胞迁移在内的各种细胞过程的酶,包括滑动肌肉收缩和细胞迁移,具有选择性抑制力的作用而得到公认,其化学配方为C14H18N4O2,被归类为小分子.Fasudil经常用于治疗脑血管血管血管出血等情况,在包括心血管疾病和...

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CAS号505-66-8 高哌嗪 | CAS号84468-15-5 异喹啉-5-磺酰氯 | CAS号105627-79-0 异喹啉-5-磺酰氯盐酸盐 | CAS号105628-07-7 盐酸法舒地尔

合成工艺路线路线简述

    5-异喹啉磺酸置于氯化亚砜体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 5.5H,反应生成法舒地尔
    参考文献:使用 1-重氮萘醌的 Cu(II)-催化构建杂二芳基化合物:合成 Quinox 和相关 P,N 配体的一般策略
    标题:使用 1-重氮萘醌的 Cu(II)-催化构建杂二芳基化合物:合成 Quinox 和相关 P,N 配体的一般策略
    摘要:开发了一种有效且直接的方法,用于在廉价的 Cu(II) 催化下使用容易获得的n-氧化物和重氮萘醌合成杂二芳基化合物.所开发的方法以简单的方式提供了 Quinox 和相关同类物.以高位点选择性实现了范围广泛的重要杂二芳基化合物.合成的萘酚被转化为特权相关的 P,N 配体.合适的拆分方法可以直接提供相应的轴向手性杂二芳基化合物.
    Doi:10.1021/acs.Orglett.2C00127

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:US-12180182-B2
    优先权日:2021-12-01
    标题 :(Di)amination of activated allene compounds, derivatives thereof, and methods for synthesis of the same
    发明人:DAI MINGJI
    权利人:PURDUE RESEARCH FOUNDATION
    摘要:One-pot synthesis methods for producing amines from activated allenes and derivatives thereof are provided, as well as the compounds produced thereby.

    专利号:WO-2025056767-A1
    优先权日:2023-09-15
    标题 :Process for the preparation of enantiomerically enriched aliphatic amines
    发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS
    权利人:SYNGENTA CROP PROTECTION AG
    摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.

    专利号:US-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:WO-2009094569-A2
    优先权日:2008-01-25
    标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

    专利号:WO-2021074309-A1
    优先权日:2019-10-16
    标 题:1-(3-quinolyl)-3,4-dihydroisoquinoline derivatives as fungicides for combating specific phytopathogens
    发明人:WEISS MATTHIAS; QUARANTA LAURA; BOU HAMDAN FARHAN; MAHAJAN ATUL; WILLIAMS SIMON; KILARU JAGADEESH; SEN INDIRA; BIERI STEPHANE; DIGGELMANN MARTIN
    权利人:SYNGENTA CROP PROTECTION AG
    摘要:1-(3-quinolyl)-3,4-dihydroisoquinoline derivatives of formula (I) as well as a method of combating, preventing or controlling the phytopathogens Mycosphaerella graminicola (Septoria tritici), Fusarium culmorum, Gibberella zeae (Fusarium graminearum) and Monographella nivalis (Microdochium nivale), which comprises applying to the phytopathogen, to the locus of the phytopathogen, or to a plant susceptible to attack by the phytopathogen, or to propagation material thereof, a fungicidally effective amount of a 1-(3-quinolyl)-3,4-dihydroisoquinoline derivative of formula (I). The present description discloses the synthesis of exemplary compounds, formulation examples, relevant biological data (antifungal activity against Mycosphaerella graminicola (Septoria tritici), Fusarium culmorum, Gibberella zeae (Fusarium graminearum) and Monographella nivalis (Microdochium nivale) when spayed on plants), as well as comparative data against three prior art compounds (e.g. pages 52 to 85; formulation examples; examples A1 to A3; table E; compounds E.01 to E.187; biological examples). Exemplary compounds are e.g.: 5-bromo-1-(8-fluoro-3-quinolyl)spiro[4H-isoquinoline-3,1'- cyclopropane] (example A1) 5-bromo-1-(8-fluoro-3-quinolyl)-3,3-dimethyl-4H-isoquinoline (example A2) 1-(8-fluoro-3-quinolyl)-3,3-dimethyl-4H-isoquinoline-5-carbonitrile (example A3)
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    主要参考文献


    1: Li YH, Liu CY, Zhang PJ, Yu JZ, Ji N, Yan YY, Feng L, Zhang HF, Xiao BG, Ma CG. [Effect of Fasudil on miroglia and astrocytes in experimental autoimmune encephalomyelitis mice]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2012 Dec;28(12):1242-5. Chinese. eCollection 2015.
    3: Fukuda T, Narahara Y, Kanazawa H, Matsushita Y, Kidokoro H, Itokawa N, Kondo C, Atsukawa M, Nakatsuka K, Sakamoto C. Effects of fasudil on the portal and systemic hemodynamics of patients with cirrhosis. J Gastroenterol Hepatol. 2014 Feb;29(2):325-9. doi: 10.1111/jgh.12360. Chinese. doi: 10.1097/IMI.0000000000000178. doi: 10.1097/NEN.0000000000000095. doi: 10.3892/mmr.2013.1818. Epub 2013 Nov 20. doi: 10.1002/acr.21622. Epub 2012 Jan 24.
    9: Guo R, Su Y, Yan J, Sun H, Wu J, Liu W, Xu Y. Fasudil improves short-term echocardiographic parameters of diastolic function in patients with type 2 diabetes with preserved left ventricular ejection fraction: a pilot study. Heart Vessels. 2015 Jan;30(1):89-97. doi: 10.1007/s00380-013-0458-3. Epub 2014 Jan 5. doi: 10.1016/j.ijcard.2014.09.101. Epub 2014 Sep 28. eCollection 2015.

    合成参考文献


    参考文献:10.1507/endocrj.k09e-328
    摘要:Kanazawa I, Yamaguchi T, Yano S, Yamauchi M, Sugimoto T. Fasudil hydrochloride induces osteoblastic differentiation of stromal cell lines, C3H10T1/2 and ST2, via bone morphogenetic protein-2 expression. Endocr J. 2010;57(5):415–21. doi: 10.1507/endocrj.k09e-328.
    参考文献:10.1253/circj.cj-11-0567
    摘要:Fukumoto Y, Shimokawa H. Recent progress in the management of pulmonary hypertension. Circ J. 2011;75(8):1801–10. doi: 10.1253/circj.cj-11-0567.
    参考文献:10.4103/2152-7806.81968
    摘要:Shirao S, Yoneda H, Ishihara H, Kajiwara K, Suzuki M; Survey Study Members of Japan Neurosurgical Society. A proposed definition of symptomatic vasospasm based on treatment of cerebral vasospasm after subarachnoid hemorrhage in Japan: Consensus 2009, a project of the 25 Spasm Symposium. Surg Neurol Int. 2011;2():74.
    参考文献:10.3892/ijmm.2011.747
    摘要:Kato K, Otsuka T, Matsushima-Nishiwaki R, Natsume H, Kozawa O, Tokuda H. Rho-kinase regulates thrombin-stimulated interleukin-6 synthesis via p38 mitogen-activated protein kinase in osteoblasts. Int J Mol Med. 2011 Oct;28(4):653–8. doi: 10.3892/ijmm.2011.747.
    参考文献:10.1016/j.jhep.2011.04.029
    摘要:Kuroda S, Tashiro H, Igarashi Y, Tanimoto Y, Nambu J, Oshita A, Kobayashi T, Amano H, Tanaka Y, Ohdan H. Rho inhibitor prevents ischemia-reperfusion injury in rat steatotic liver. J Hepatol. 2012 Jan;56(1):146–52. doi: 10.1016/j.jhep.2011.04.029.
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