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CAS号79-08-3 溴乙酸 | CAS号13094-51-4 溴代乙酸酐 | CAS号368-44-5 phenyldichlorof... | CAS号98-88-4 苯甲酰氯 | CAS号17759-85-2 1-Bromo-1-chlor... | CAS号5439-13-4 2-溴-n-(4-溴苯基)乙酰胺 | CAS号34680-81-4 2-溴-N-甲基乙酰胺 | CAS号40299-87-4 2-溴-1-(4-吗啉)乙酮 | CAS号5468-77-9 N,N-二甲基-溴乙酰胺 | CAS号3823-19-6 2-溴-N-(4-(三氟甲基)... | CAS号57339-11-4 2-溴-N-(3,5-二氯苯基)乙酰胺 | CAS号32433-61-7 2-溴-N-(2,6-二甲苯基)乙酰胺 | CAS号5439-17-8 2-溴-n-(3-甲基苯基)乙酰胺 | CAS号151427-19-9 2-溴-1-(2,3-二氢-1... | CAS号144581-86-2 2-溴-N-(4-甲氧基苄基)乙酰胺

溴乙酸置于草酰氯体系中,用 二氯甲烷 用作溶剂,化学反应 3.0H,反应生成溴乙酰氯
参考文献:发现 Cdk12 和 Cdk13 的高效,选择性双 Protac 降解剂
标题:发现 Cdk12 和 Cdk13 的高效,选择性双 Protac 降解剂
摘要:细胞周期蛋白依赖性激酶 12 和 13 (Cdk12/13) 的选择性降解为三阴性乳腺癌 (Tnbc) 提供了新的治疗机会,但仍然缺乏双 Cdk12/13 降解剂.在此,我们报告了通过采用蛋白水解靶向嵌合体 (Protac) 技术发现的第一系列高效,选择性双 Cdk12/13 降解剂.在mda-Mb-231乳腺癌细胞中,最佳化合物7F可有效降解cdk12和cdk13,Dc 50值分别为2.2和2.1 Nm.整体蛋白质组分析证明了7F的靶标选择性.在体外,7F以时间和剂量依赖性方式抑制核心 Dna 损伤反应 (Ddr) 基因的表达.此外,7F显着抑制包括 Mfm223 在内的多种 Tnbc 细胞系的增殖,Ic 50值为 47 Nm.重要的是,与结构相似的抑制剂4相比,7F显示出显着改善的抗增殖活性,这表明 Cdk12/13 降解剂对于 Tnbc 靶向治疗的潜在优势.
Doi:10.1021/acs.Jmedchem.2C00384

专利信息

专利号:US-10189803-B2
优先权日:2008-02-22
标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions
发明人：CHONG HYUN-SOON
权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH
摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

专利号:WO-2024036115-A1
优先权日:2022-08-08
标题:Continuous flow synthesis of lorazepam
发明人：THOMPSON DAVID; BIYANI SHRUTI; HYUN SEOK-HEE; MCGUIRE MICHAEL
权利人:PURDUE RESEARCH FOUNDATION; CONTINUITY PHARMA LLC
摘要:A method for synthesis of Lorazepam in a continuous flow using continuous flow reactor, in which method comprises five steps including N-acylation, diazepine ring closure, imine N- oxidation, Polonovski-type rearrangement, and ester hydrolysis; a green reagent comprising a peroxide reagent and rhenium oxide catalyst for N-oxidation of delorazepam; and an ammonium source combination for the synthesis of delorazepam.

专利号:WO-9000622-A1
优先权日:1988-07-08
标题 :Oligonucleotide hybridization probes and means for the synthesis of the most preferred probes
发明人：KWIATKOWSKI MAREK; SUND CHRISTIAN; HURSKAINEN PERTTI
权利人:WALLAC OY; PHARMACIA AB
摘要:Oligonucleotide probe labeled at one of its teminal positions with a non-linear branched polymer carrying a plurality of negatively charged groups, preferably phosphodiester groups, and optionally also analytically indicatable groups covalently linked to terminal ends of the branches of said polymer. The preferred indicatable groups are lanthanide chelates. A compound that can be used for the synthesis of the probe is also disclosed. The compound has formula (I), where R1 and R2 are lower alkyl; R3 is lower alkyl (C1-C7), or aryl each of which optionally being provided with electron-withdrawing substituents; and A1, A2 and A3 are hydrogen, A'-O-B, A''-O-B or A'''-O-B, at most one of A1-3 being hydrogen and A', A'' and A''' being a hydrocarbon chain providing a distance of 5-9 atoms between the phosphorous atom and the oxygen directly bound to B, and B being a protecting group. In the preferred compound at least two of A1-3 are identical while the other is hydrogen.

专利号:US-6756199-B1
优先权日:1994-02-23
标题:Peptide nucleic acid combinatorial libraries and improved methods of synthesis
发明人：COOK PHILLIP DAN; KIELY JOHN; SPRANKLE KELLY
权利人:ISIS PHARMACEUTICALS INC
摘要:New sub-monomer synthetic methods for the preparation of peptide nucleic acid oligomeric structures are disclosed that provide for the synthesis of both predefined sequence peptide nucleic acid oligomers as well as random sequence peptide nucleic acid oligomers. Further these methods also provide for the incorporation of peptide nucleic acid units or strings of such units with amino acids or strings of amino acids in chimeric peptide nucleic acid-amino acid compounds. Further disclosed are method of making random libraries of peptide nucleic acids using the fully preformed monomers. Chimeric oligomers and libraries of the same are also disclosed.

专利号:US-5783577-A
优先权日:1995-09-15
标题 :Synthesis of quinazolinone libraries and derivatives thereof
发明人：HOUGHTEN RICHARD A; OSTRESH JOHN M
权利人:TREGA BIOSCIENCES INC
摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.

专利号:US-11555047-B2
优先权日:2019-10-31
标题:One-step synthesis of phosphate-based inhibitors and applications thereof
发明人：D'ANTONIO EDWARD; PIERCE JOSHUA
权利人:UNIV SOUTH CAROLINA; UNIV NORTH CAROLINA STATE
摘要:One-step methods for forming phosphate-based enzyme inhibitors are disclosed. Methods include reacting o-phosphorylethanolamine with an acyl chloride at acidic conditions. Acyl chlorides can be derivatized. The phosphate-based enzyme inhibitors can inhibit enzymes of the pentose phosphate pathway including D-ribose-5-phosphate aldose-ketose isomerase enzymes such as T. cruzi ribose 5-phosphate isomerase type B and D-ribulose-5-phosphate 3-epimerase enzymes. Methods can be used in forming pharmaceutical compositions for use in treatment of disease caused by kinetoplastid parasites including T. cruzi, T. brucei, and Leishmania spp.