CAS: 68206-45-1; 3-Nitro-2-Pyridinesulfenylchloride

该化合物是一种有机化合物,其特点是其独特的结构,包括一个由硝基组和硫化氯功能组替代的环,该化合物一般是黄色至橙固态或液体,视其纯度和形态而定;以其反应性而著称,特别是由于硫基氯化物组的存在可参与核生殖替代反应;硝基罗组有助于化合物的电子提取特性,影响其再活动性和稳定性.3-Nitro-2-pyridinefenyl 氯经常用于有机合成,特别是用于制造各种含有硫化合物的化合物和化学反应中的试剂.必须谨慎处理该化合物,因为它可能有毒,而且一旦与皮肤或粘膜接触,可能会引起刺激.在实验室环境中与该物质打交道时,应当遵循适当的安全议定书.

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38240-29-8 130156-01-3 68118-07-0

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CAS号69212-31-3 2-苄硫基-3-硝基吡啶 | CAS号5470-18-8 2-氯-3-硝基吡啶 | CAS号153815-22-6 2-[(4-methoxyph... | CAS号76880-29-0 (R)-2-((叔丁氧基羰基)...

合成工艺路线路线简述

    📜4-Methoxybenzyl 3-Nitro-2-Pyridyl Sulfide置于磺酰氯体系中,用 二氯甲烷 作为反应溶剂,化学反应 0.33H,反应生成 3-硝基-2-吡啶硫酰氯
    参考文献:A New Method For The Preparation Of 3-Nitro-2-Pyridinesulfenyl Chloride And One-Pot Syntheses Ofn(α)-Tert-Butoxycarbonyl-S-3-Nitro-2-Pyridinesulfenyl Derivatives Of Cysteine And D-Penicillamine
    标题:A New Method For The Preparation Of 3-Nitro-2-Pyridinesulfenyl Chloride And One-Pot Syntheses Ofn(α)-Tert-Butoxycarbonyl-S-3-Nitro-2-Pyridinesulfenyl Derivatives Of Cysteine And D-Penicillamine
    摘要:通过 3-硝基-2-吡啶苄基硫化物与硫酰氯的反应制备了 3-硝基-2-吡啶硫酰氯.使用 4-甲氧基苄基 3-硝基-2-吡啶硫化物完成了半胱氨酸和 D-青霉胺的 N (δ)-叔丁氧羰基-S-3-硝基-2-吡啶亚磺酰基衍生物的一锅合成.
    DOI:10.1055/s-1994-25394

    海关参考信息

    专利信息


    专利号:US-2006287520-A1
    优先权日:2005-05-16
    标 题 :Synthesis of salinosporamide A and analogues thereof
    发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI
    权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI
    摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.

    专利号:WO-2012047907-A9
    优先权日:2010-10-04
    标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto
    发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
    权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
    摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.

    专利号:US-2009221568-A1
    优先权日:2005-11-04
    标题:Synthesis of Inhibitors of FtsZ
    发明人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY
    权利人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY
    摘要:FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.

    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-7576234-B2
    优先权日:2002-05-15
    标题 :Synthesis of 2-alkyl amino acids
    发明人:CHORGHADE MUKUND S; GURJAR MUKUND K; MOHAPATRA DEBENDRA K
    权利人:GENZYME CORP
    摘要:Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.

    专利号:US-7414106-B2
    优先权日:2003-06-19
    标 题 :Synthesis of peptide α-thioesters
    发明人:CAMARERO JULIO A; MITCHELL ALEXANDER R; DE YOREO JAMES J
    权利人:L LIVERMORE NAT SECURITY LLC
    摘要:Disclosed herein is a new method for the solid phase peptide synthesis (SPPS) of C-terminal peptide α thioesters using Fmoc/t-Bu chemistry. This method is based on the use of an aryl hydrazine linker, which is totally stable to conditions required for Fmoc-SPPS. When the peptide synthesis has been completed, activation of the linker is achieved by mild oxidation. The oxidation step converts the acyl-hydrazine group into a highly reactive acyl-diazene intermediate which reacts with an α-amino acid alkylthioester (H-AA-SR) to yield the corresponding peptide α-thioester in good yield. A variety of peptide thioesters, cyclic peptides and a fully functional Src homology 3 (SH3) protein domain have been successfully prepared.

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    主要参考文献

    [参考文献]: K C Pugh, Et Al. Synthesis And Stability Of 3-Nitro-2-Pyridinesulfenyl Chloride (Npyscl). Int J Pept Protein Res. 1993 Aug;42(2):159-64.
    [参考文献]: O Rosen, Et Al. Thiolysis Of The 3-Nitro-2-Pyridinesulfenyl (Npys) Protecting Group. An Approach Towards A General Deprotection Scheme In Peptide Synthesis. Int J Pept Protein Res. 1990 Jun;35(6):545-9.
    [参考文献]: R G Simmonds, Et Al. Synthesis Of Disulfide-Bridged Fragments Of Omega-Conotoxins Gvia And Mviia. Use Of Npys As A Protecting/activating Group For Cysteine In Fmoc Syntheses. Int J Pept Protein Res. 1994 Apr;43(4):363-6.
    [参考文献]: R Matsueda, Et Al. Compatibility Of The S-(3-Nitro-2-Pyridinesulfenyl) Protecting Group With Dcc/hobt Coupling Chemistry. Pept Res. 1992 Sep-Oct;5(5):262-4.
    [参考文献]: R Matsueda, Et Al. Design And Synthesis Of A Kininogen-Based Selective Inhibitor Of Thrombin-Induced Platelet Aggregation. Pept Res. 1994 Jan-Feb;7(1):32-5.

    合成参考文献


    参考文献:10.1055/s-0035-1560537
    摘要:Poulsen T, Olsen F, Tsakos M. Npys-Mediated Elimination Reactions of Alcohols and Thiols: A Facile Route to Dehydroalanine and Dehydrobutyrine Building Blocks. Synlett. 2015 Nov 06;26(19):2697–701. doi: 10.1055/s-0035-1560537.
    摘要:Matsueda R, Umeyama H, Puri RN, Bradford HN, Colman RW. Design and synthesis of a kininogen-based selective inhibitor of thrombin-induced platelet aggregation. Pept Res. 1994 Jan;7(1):32–5.
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