胞嘧啶置于sodium Hydroxide体系中,用 水 作为反应溶剂,以65%的收率获得产物5-氟脲嘧啶 参考文献:Process For Production Of 5-Fluorouracil And Its Derivatives 标题:Process For Production Of 5-Fluorouracil And Its Derivatives 摘要:生产5-氟尿嘧啶及其衍生物的方法包括在水性介质中将具有以下结构的胞嘧啶化合物:##str1## 其中r是氢原子或糖苷基与氟或氟磺酸氟酸酯(foso.Sub.2 F)反应,以得到相应的具有以下结构的5-氟尿嘧啶化合物:##str2## 其中r如上所定义.
专利信息
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-10167308-B2 优先权日:2013-09-14 标题:Highly efficient synthesis of long RNA using reverse direction approach 发明人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P 权利人:CHEMGENES CORP 摘要:The present invention relates to novel process of reverse 5′→3′ directed synthesis of RNA oligomers in the range of about 100-mer to about 200-mer has been developed and disclosed. Using that method demonstrated high quality RNA synthesis with coupling efficiency approaching 99%.
专利号:WO-2024201393-A1 优先权日:2023-03-29 标 题:Methods for the synthesis of nucleoside analogues and nucleosides analogues derived therefrom 发明人:BRITTON ROBERT; Muir Garrett; ANKETELL MATTHEW JAMES; HUXLEY COHAN; BAIKABI SUPING 权利人:UNIV FRASER SIMON 摘要:The present invention relates to methods for the synthesis of nucleoside analogues. More specifically, the present invention relates to methods for the synthesis of C4' substituted nucleoside analogues via the reaction of a soft nucleophile with a halohydrin ketone.
专利号:US-7229797-B1 优先权日:1999-08-20 标 题:Enzymatic synthesis of deoxyribonucleosides 发明人:TISCHER WILHELM; IHLENFELDT HANS-GEORG; BARZU OCTAVIAN; SAKAMOTO HIROSHI; PISTOTNIK ELISABETH; MARLIERE PHILIPPE; POCHET SYLVIE 权利人:PASTEUR INSTITUT 摘要:The present invention relates to a method for the in vitro enzymatic synthesis of deoxyribonucleosides and enzymes suitable for this method.
专利号:WO-2024104433-A9 优先权日:2022-11-16 标 题:Use of galectin-1 as immune checkpoint in preparation of tumor immunotherapy medicament and medicament 发明人:ZHANG YU; HONG YU; SI XIAOFANG; LIU WENJING; MAI XUEYING 权利人:NAT INSTITUTE OF BIOLOGICAL SCIENCES BEIJING 摘要:Provided are use of galectin-1 (Gal-1) as an immune checkpoint in the preparation of a tumor immunotherapy medicament and the medicament, and provided is a new tumor immunotherapy strategy targeting the new immune checkpoint. Lactose and a derivative thereof can inhibit the immune checkpoint by competing Gal-1 on the surfaces of a cancer cell and an immune cell, and do not have significant toxic and side effects. Knocking out B4GATL1 to reduce protein galactosylation can significantly reduce the level of Gal-1 transferred from a tumor to a T cell, thereby enhancing the activation and function of the T cell. In addition, a lactose synthetase component LALBA is overexpressed in a mouse tumor, and de novo synthesis of lactose in a tumor microenvironment can be realized, such that an immune response mediated by a CD8+ T cell is enhanced. In combination with the anti-tumor effect and economic cost of lactose, a wide and feasible idea is provided for cancer treatment.
专利号:WO-2024163733-A1 优先权日:2023-02-01 标题:Electrochemical synthesis with redox stable nucleotides 发明人:WU TIANDI; LACKEY JEREMY; LIN YANYOU; PITSCH STEFAN 权利人:TWIST BIOSCIENCE CORP 摘要:Provided herein are compositions, devices, systems and methods for constructing and storing polynucleotides encoding information with redox resistant bases. The compositions, devices, systems, and methods described herein provide for storage or synthesis of a library comprising a plurality of polynucleotides with one or more redox resistance bases. Further provided herein are methods to increase DNA synthesis yield and fidelity.
1: Shah VV, Aldahan AS, Mlacker S, Alsaidan M, Samarkandy S, Nouri K. 5-Fluorouracil in the Treatment of Keloids and Hypertrophic Scars: A Comprehensive Review of the Literature. Dermatol Ther (Heidelb). 2016 Apr 22. [Epub ahead of print] Review. doi: 10.1007/s12291-015-0482-4. Epub 2015 Feb 15. Review. 3: Metterle L, Nelson C, Patel N. Intralesional 5-fluorouracil (FU) as a treatment for nonmelanoma skin cancer (NMSC): A review. J Am Acad Dermatol. 2016 Mar;74(3):552-7. doi: 10.1016/j.jaad.2015.09.040. Epub 2015 Nov 11. Review. doi: 10.1002/14651858.CD006259.pub2. Review. Review. Japanese. doi: 10.1155/2014/827989. Epub 2014 Dec 28. Review. 7: Ye J, Chen J, Ge L, Liu A, Zhou S. Effectiveness and safety of s-1-based therapy compared with 5-Fluorouracil-based therapy for advanced colorectal cancer: a meta-analysis. Gastroenterol Res Pract. 2014;2014:146530. doi: 10.1155/2014/146530. Epub 2014 Nov 30. Review.
合成参考文献
参考文献:10.1016/j.canlet.2010.01.006 摘要:Pan J, Cheng C, Verstovsek S, Chen Q, Jin Y, Cao Q. The BH3-mimetic GX15-070 induces autophagy, potentiates the cytotoxicity of carboplatin and 5-fluorouracil in esophageal carcinoma cells. Cancer Lett. 2010 Jul 28;293(2):167–74. doi: 10.1016/j.canlet.2010.01.006. 参考文献:10.1016/j.colsurfb.2010.01.030 摘要:Arias JL, López-Viota M, Delgado AV, Ruiz MA. Iron/ethylcellulose (core/shell) nanoplatform loaded with 5-fluorouracil for cancer targeting. Colloids Surf B Biointerfaces. 2010 May 01;77(1):111–6. doi: 10.1016/j.colsurfb.2010.01.030. 摘要:Yanagisawa S, Tsuchiya S, Kaiho T, Togawa A, Shinmura K, Okamoto R, Nishimura M, Nomura S, Nobumoto D, Miyazaki M. [Histological complete response in a case of primary squamous cell carcinoma of the stomach treated by chemotherapy with docetaxel and cisplatin plus 5-fluorouracil]. Gan To Kagaku Ryoho. 2010 Feb;37(2):307–10. 摘要:Furumoto K, Kojima H, Takaya H, Okuno M, Fuji H, Mizuno R, Mori T, Ito D, Kogire M. [A case of advanced ascending colon cancer, curatively resected after complete response in left supraclavicular and paraaortic lymph nodes and liver metastases to FOLFOX4 therapy]. Gan To Kagaku Ryoho. 2010 Feb;37(2):323–6. 摘要:Yasue H, Hanyu N, Usuba T, Abe M. [A case successfully treated with total pelvic exenteration after preoperative chemotherapy FOLFOX4 plus bevacizumab for unresectable sigmoid colon cancer with extramural progression]. Gan To Kagaku Ryoho. 2010 Feb;37(2):327–9.