1,3-Dimethyl-5-Bromo-6-Methylaminopyrimidine-2,4-Dione置于sodium Azide体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,以47%的收率获得产物茶碱 参考文献:A High Chemical Reactivity Of 5-Azidouracils And Its Synthetic Application: Novel Synthesis Of 8-Substituted 1,3-Dimethylxanthine Derivatives 标题:A High Chemical Reactivity Of 5-Azidouracils And Its Synthetic Application: Novel Synthesis Of 8-Substituted 1,3-Dimethylxanthine Derivatives 摘要:A Novel Method For The Preparation Of 8-Substituted 1,3-Dimethylxanthine Derivatives (7 Or 8) Is Described: Treatment Of 6-Alkylamino-5-Bromo-1,3-Dimethyluracils (6A-E),Easily Prepared By Bromination Of The Corresponding 6-Alkylamino-1,3-Dimethyluracils (5),With Sodium Azide In Dmf At Ambient Temperature Allowed The Direct Formation Of The 8-Substituted 1,3-Dimethylxanthines (7) Proceeding Via A Transient Formation Of The Corresponding 5-Azido-1,3-Dimethyluracils. The 5-Bromo-1,3-Dimethyluracils (6F,G) Possessing An Ct-Branched Alkylamino Group At The 6-Position Similarly React With Sodium Azide To Afford 8,8-Disubstituted 1,3-Dimethyl-8H-Xanthines (8,8-Disubstituted 1,3-Dimethyl-3,G-Dihydropurine-2,6-Diones)(8). DOI:10.3987/com-97-S68
专利信息
专利号:US-11542269-B2 优先权日:2018-01-03 标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHOI HYEONG-WOOK; FANG FRANCIS G 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:US-10913749-B2 优先权日:2015-05-07 标 题 :Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:US-11136335-B2 优先权日:2016-06-30 标题:Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHASE CHARLES E; CHOI HYEONG-WOOK; ENDO ATSUSHI; FANG FRANCIS G; KIM DAE-SHIK 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
专利号:US-8957230-B2 优先权日:2011-06-30 标 题 :Synthesis of cleistanthin A and derivatives thereof 发明人:MULIK NILESH SHRIDHAR; PANGHAVANE KAILASH DATTATRAYA 权利人:MULIK NILESH SHRIDHAR; PANGHAVANE KAILASH DATTATRAYA 摘要:The present invention provides a method for preparing Cleistanthin A, a diphyllin glycoside, derivatives thereof and intermediates thereto. In particular the present invention provides in one of the aspect a method for synthesis of compound of formula D a key intermediate of diphyllin, which can be carried out in a shorter duration and at an ordinary temperature.
专利号:US-2025235415-A1 优先权日:2022-02-23 标 题:Modulation of human breast milk composition 发明人:ROSS MICHAEL G; DESAI MINA 权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER 摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.
专利号:US-5955083-A 优先权日:1996-01-03 标 题 :Use of eriobotrya japonica extract, in particular in cosmetics for stimulating glycosaminoglycan synthesis 发明人:BONTE FREDERIC; DUMAS MARC 权利人:LVMH RECH 摘要:PCT No. PCT/FR97/00009 Sec. 371 Date Aug. 28, 1997 Sec. 102(e) Date Aug. 28, 1997 PCT Filed Jan. 3, 1997 PCT Pub. No. WO97/06659 PCT Pub. Date Feb. 27, 1997The invention concerns novel uses of an Eriobotrya japonica extract, in particular in cosmetics or pharmaceutics. This extract permits stimulation of glycosaminoglycan synthesis, in particular of hyaluronic acid, thus imparting to the cosmetic compositions containing this extract the properties of improving the firmness and suppleness of the skin, combating the formation of wrinkles or lessening the depth thereof, smoothing the surface of the skin by means of a tightening effect, or moisturizing the skin. The invention further concerns the use of these extracts for stimulating the synthesis of glycosaminoglycans from a cell culture medium, in particular fibroblasts or keratinocytes.
[参考文献]: Barnes Pj. Theophylline. Am J Respir Crit Care Med. 2013 Oct 15;188(8):901-6. [参考文献]: Ichiyama T, Et, Al. Theophylline Inhibits Nf-Kappa B Activation And I Kappa B Alpha Degradation In Human Pulmonary Epithelial Cells. Naunyn Schmiedebergs Arch Pharmacol. 2001 Dec;364(6):558-61. [参考文献]: Ito K, Et, Al, Adcock Im, Barnes Pj. A Molecular Mechanism Of Action Of Theophylline: Induction Of Histone Deacetylase Activity To Decrease Inflammatory Gene Expression. Proc Natl Acad Sci U S A. 2002 Jun 25;99(13):8921-6. [参考文献]: Németh Zh, Et, Al. Amrinone And Theophylline Differentially Regulate Cytokine And Nitric Oxide Production In Endotoxemic Mice. Shock. 1997 May;7(5):371-5. [参考文献]: Rabe Kf, Et, Al. Theophylline And Selective Pde Inhibitors As Bronchodilators And Smooth Muscle Relaxants. Eur Respir J. 1995 Apr;8(4):637-42.
合成参考文献
参考文献:10.1007/s11095-009-0039-4 摘要:Ji JA, Liu J, Shire SJ, Kamerzell TJ, Hong S, Billeci K, Shen Y, Wang YJ. Characteristics of rhVEGF Release from Topical Hydrogel Formulations. Pharmaceutical Research. 2010 Feb 13;27(4):644–54. doi: 10.1007/s11095-009-0039-4. 参考文献:10.1007/s11418-010-0396-7 摘要:Kusuma IW, Arung ET, Rosamah E, Purwatiningsih S, Kuspradini H, Syafrizal, Astuti J, Kim Y, Shimizu K. Antidermatophyte and antimelanogenesis compound from Eleutherine americana grown in Indonesia. Journal of Natural Medicines. 2010 Feb 13;64(2):223–6. doi: 10.1007/s11418-010-0396-7. 参考文献:10.1007/s00216-010-3506-1 摘要:Carvalho JJ, Weller MG, Panne U, Schneider RJ. A highly sensitive caffeine immunoassay based on a monoclonal antibody. Analytical and Bioanalytical Chemistry. 2010 Feb 16;396(7):2617–28. doi: 10.1007/s00216-010-3506-1. 参考文献:10.1186/2047-783x-14-s4-108 摘要:Holownia A, Mroz RM, Kolodziejczyk A, Chyczewska E, Braszko JJ. Increased FKBP51 in induced sputum cells of chronic obstructive pulmonary disease patients after therapy. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):108. doi: 10.1186/2047-783x-14-s4-108. 参考文献:10.1186/2047-783x-14-s4-205 摘要:Rantzsch U, Vacca G, Dück R, Gillissen A. Anti-inflammatory effects of myrtol standardized and other essential oils on alveolar macrophages from patients with chronic obstructive pulmonary disease. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):205. doi: 10.1186/2047-783x-14-s4-205.