氯甲酸甲酯置于potassium Hydrogencarbonate体系中,用 水 作为反应溶剂,化学反应生成 氨基甲酸甲酯 参考文献:Efficient Synthesis Of A 1,4-Dihydro2H-3,1-Benzoxazin-2-One 标题:Efficient Synthesis Of A 1,4-Dihydro2H-3,1-Benzoxazin-2-One 摘要:一种高效的方法,用氨基醇中间体与烷基或芳基氯甲酸酯和碱进行环化反应,制备一种名为dmp-266的化合物(-)-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并噁嗪-2-酮,也称为一种逆转录酶抑制剂.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
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-10253153-B2 优先权日:2015-04-24 标题 :Linker and support for solid phase synthesis of nucleic acid, and production method of nucleic acid using said support 发明人:MAETA ERI; MORI KENJIRO; HORIE SHOHEI; ITO TAKAHIKO; SAITO SHOICHIRO; NAGAO RYUHEI 权利人:NITTO DENKO CORP 摘要:The present invention provides a linker for solid phase synthesis of nucleic acid, which consists of a compound represented by the formula (I) or the formula (II), a support for solid phase synthesis of nucleic acid, which has a structure represented by the formula (III), and a production method of a nucleic acid, which uses the support: n nwherein each symbol is as defined in the SPECIFICATION.
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:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-8445713-B2 优先权日:2007-10-22 标 题 :Catalyst for the synthesis of organic carbonates, process for preparing the same and application thereof 发明人:WERSHOFEN STEFAN; KLEIN STEPHAN; ZHOU ZHIPING; WANG XINKUI; WANG JUNWEI; KANG MAOQING 权利人:WERSHOFEN STEFAN; KLEIN STEPHAN; ZHOU ZHIPING; WANG XINKUI; WANG JUNWEI; KANG MAOQING; BAYER MATERIALSCIENCE AG 摘要:The present invention relates to a catalyst for the synthesis of organic carbonates, the preparation of the catalyst and the application of this catalyst in the synthesis of organic carbonates from reacting urea and hydroxyl group containing compounds. The catalyst provided in this invention is a calcinate of hydrous salt containing rare earth element at a moderate calcining temperature.
[参考文献]: Anton I Rosenbaum, Et Al. Thiadiazole Carbamates: Potent Inhibitors Of Lysosomal Acid Lipase And Potential Niemann-Pick Type C Disease Therapeutics. J Med Chem. 2010 Jul 22;53(14):5281-9. [参考文献]: Catharina Wesseling, Et Al. Symptoms Of Psychological Distress And Suicidal Ideation Among Banana Workers With A History Of Poisoning By Organophosphate Or N-Methyl Carbamate Pesticides. Occup Environ Med. 2010 Nov;67(11):778-84. [参考文献]: F K Zimmermann, Et Al. Formaldehyde, Glyoxal, Urethane, Methyl Carbamate, 2,3-Butanedione, 2,3-Hexanedione, Ethyl Acrylate, Dibromoacetonitrile And 2-Hydroxypropionitrile Induce Chromosome Loss In Saccharomyces Cerevisiae. Mutat Res. 1992 Nov 16;270(2):151-66. [参考文献]: Geun-Hye Gang, Et Al. Analysis Of Fungicide Sensitivity And Genetic Diversity Among Colletotrichum Species In Sweet Persimmon. Plant Pathol J. 2015 Jun;31(2):115-22. [参考文献]: Jean Demaison, Et Al. Equilibrium Vs Ground-State Planarity Of The Conh Linkage. J Phys Chem A. 2007 Apr 5;111(13):2574-86.
合成参考文献
摘要:Chen, P.; Liu, G.; Engle, K. M.; Yu, J.-Q., Science of Synthesis Knowledge Updates, (2013) 2, 77. 摘要:Khartulyari, A.; Maier, M. E., Science of Synthesis Knowledge Updates, (2010) 3, 114. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 262. 摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2018) 4, 140. 摘要:Aitken, R. A.; Boubalouta, Y., Science of Synthesis Knowledge Updates, (2013) 4, 141.