📜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
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.
[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.