CAS: 1469-70-1; Carbonicacidallylethylester

相似化合物

15022-08-9 35466-83-2 35179-98-7

上下游产品

CAS号541-41-3 氯甲酸乙酯 | CAS号107-18-6 烯丙醇 | CAS号64-17-5 乙醇 | CAS号15022-08-9 碳酸二烯丙酯 | CAS号2937-50-0 氯甲酸烯丙酯 | CAS号124-38-9 二氧化碳 | CAS号121-44-8 三乙胺 | CAS号4743-74-2 2-苯基-4-五亚乙基六胺-2-醇 | CAS号538-08-9 二烯丙基代氰氨 | CAS号2049-80-1 烯丙基丙二酸二乙酯 | CAS号3195-24-2 二烯丙基丙二酸二乙酯 | CAS号21997-30-8 1-ALLYL-2(1H)-P... | CAS号64-17-5 乙醇 | CAS号107-18-6 烯丙醇 | CAS号105-58-8 碳酸二乙酯 | CAS号875-79-6 1,2-二甲基吲哚 | CAS号696-57-1 N-烯丙基吗啉

氯甲酸乙酯,烯丙醇置于吡啶,4-二甲氨基吡啶体系中,用 二氯甲烷 用作溶剂,以99%的收率获得碳酸丙烯乙酯
参考文献:设计,合成和构象活性的非天然桥接双环二肽作为高强度缺氧诱导因子-1抑制剂和抗肿瘤剂.
标题:设计,合成和构象活性的非天然桥接双环二肽作为高强度缺氧诱导因子-1抑制剂和抗肿瘤剂.
摘要:通过基于棘霉素的双环肽结构进行结构修饰,我们成功合成了各种强大的抗肿瘤衍生物.通过与非天然键的交联限制了所得化合物中的环构象.所制备的衍生物被证明能强烈抑制缺氧诱导因子(hif)-1的转录激活和hif-1蛋白表达的缺氧诱导.特别是,烯烃桥连衍生物12表现出显着的细胞毒性(在mcf-7细胞系上,Ic50 = 0.22 Nm)和hif-1抑制(ic50 = 0.09 Nm),大大超过了棘霉素.构象分析和分子模型研究表明,通过构象限制,通过代谢稳定和刚性的桥键交联,生物活性得到增强.此外,我们提出了一种新的通过分子内π堆积稳定的球状构象,该构象可以促进双环二肽的生物效应.本研究中提出的进展为扩大药物发现中肽的化学空间提供了有用的指导.
Doi:10.1021/acs.Jmedchem.9B02039

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: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: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-9688644-B2
优先权日:2009-04-30
标 题 :Synthesis of Tetracyclines and intermediates thereto
发明人：MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M
权利人:HARVARD COLLEGE
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 substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.

专利号:US-9884830-B2
优先权日:2004-05-21
标题 :Synthesis of tetracyclines and analogues thereof
发明人：MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R
权利人:HARVARD COLLEGE
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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

专利号:US-8907104-B2
优先权日:2006-10-11
标 题 :Synthesis of enone intermediate
发明人：MYERS ANDREW G; BRUBAKER JASON D
权利人:HARVARD COLLEGE
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 a more efficient route for preparing the enone intermediate.