4-(三氟甲基)苯肼置于镍体系中,用 甲醇 作为反应溶剂,化学反应 1.0H,以to Give The Title Compound In 100% Yield的收率获得产物对三氟甲基苯胺 参考文献:Processes For Preparing Pesticidal Intermediates 标题:Processes For Preparing Pesticidal Intermediates 摘要:公式(i)的化合物是通过对公式(II)的氢解反应制备的:其中r1是卤代烷基,卤代烷氧基或−sf5;w是n或cr3;而r2和r3是h或cl.公式(i)的化合物可用作制备具有杀虫活性的芳基吡唑化合物的中间体.
专利号:US-11040938-B2 优先权日:2016-07-27 标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts 发明人:MA BING; PAN SHUAI 权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH 摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:WO-2016005407-A1 优先权日:2014-07-07 标 题:One-pot synthesis of squaramides 发明人:MÃ?RQUEZ LÓPEZ MARÃ?A EUGENIA; ALEGRE REQUENA JUAN VICENTE; PÉREZ HERRERA RAQUEL 权利人:UNIV ZARAGOZA; CONSEJO SUPERIOR INVESTIGACION 摘要:The present invention refers to the first one-pot synthesis of squaramides. The one-pot synthesis of squaramides described herein is an easy and straightforward procedure to obtain squaramide derivatives which saves energy, avoids time consuming purification steps, reduces costs and provides better yields as compared with those squaramides obtained through the traditional 'stop-and-go' approach. Moreover, the authors of the present invention herein demonstrate the efficiency of this one-pot process with the synthesis of three biologically active structures, improving in most of the cases the results of the previous stepwise syntheses.
专利号:US-2013338369-A1 优先权日:2011-03-07 标 题 :Process for the Synthesis of Aminobiphenylene 发明人:HEINRICH MARKUS; PRATSCH GERALD 权利人:HEINRICH MARKUS; PRATSCH GERALD; BASF SE 摘要:The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.
专利号:US-2025101045-A1 优先权日:2022-01-18 标题:Synthesis of boron-containing amidoxime reagents and their application to synthesize functionalized oxadiazole and quinazolinone derivatives 发明人:DAS BHASKAR 权利人:LONG ISLAND UNIV 摘要:The present disclosure is concerned with borylated amidoximes useful in the synthesis of biologically relevant drug-like molecules, including functionalized oxadizole and quinazolinone derivatives. Also disclosed are methods of making borylated amidoximes, methods of making functionalized oxadiazole and quinazolinone compounds using the amidoximes, and functionalized oxadiazole and quinazolinone compounds prepared from borylated amidoximes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:WO-2022123336-A1 优先权日:2020-12-07 标 题 :Chromeno [4,3-b] quinoline compounds and their synthesis by using silicotungstic acid [h4siw12o40] 发明人:HEGDE SUBRAMANYA GOPAL; LOKESH KOODLUR SANNEGOWDA; SHUBHA JAYACHAMARAJAPURA PRANESH; SUSHMA NURANI VISWANATHAN; BASAVARAJU GIRISH; DANAGOUDAR ANANDA; BODA VIJAY KUMAR 权利人:HEGDE SUBRAMANYA GOPAL; LOKESH KOODLUR SANNEGOWDA 摘要:The present invention relates to the development of novel compounds of chromeno [4,3-b] quinolone derivatives. It particularly relates to the development of novel compounds of thiochromeno [4,3-b] quinolone derivatives for the treatment of coronary artery diseases, dyslipidemia, and metabolic syndrome. The present invention also relates to the first synthesis of Silicotungstic -catalyzed Aza-Diels-Alder-reactions (ADAR) with s-prenyl derivatives of α-tetralone, 4-chromanone and Thiochroman-4-one and various substituted amines to deliver cycloadducts in good yield and excellent diastereoselectivity under mild reaction conditions. The invention further relates to the method for the treatment of coronary artery diseases, dyslipidemia, and metabolic syndrome by using synthesized compounds of thiochromeno [4,3-b] quinolone derivatives. The present invention provides the use of Silicotungstic acid as Lewis acid for Aza-Diels-Alder-reactions to get a mixture of diastereomers are the first examples. In addition to its efficiency, simplicity, and mild reaction conditions, the catalyst is very cheap and only a small amount (10 mol%) is needed. Intramolecular cyclization was carried out very conveniently as a one-pot reaction starting from the S-prenyl chromene-3-carbaldehyde and arylamines without isolation of the intermediate imines.
[参考文献]: A M Jones, Et Al. Mapping Of The Human Ribosomal Small Subunit Protein Gene Rps24 To The Chromosome 10Q22-Q23 Boundary. Genomics. 1997 Jan 1;39(1):121-2. [参考文献]: B A Maguire, Et Al. Mutations In The Rpmbg Operon Of Escherichia Coli That Affect Ribosome Assembly. J Bacteriol. 1997 Apr;179(8):2486-93. [参考文献]: J Seifert, Et Al. Trifluoromethylanilines--Their Effect On Dna Synthesis And Proliferative Activity In Parenchymal Organs Of Rats. Toxicology. 1993 Oct 25;83(1-3):49-59. [参考文献]: L Sebestová, Et Al. Effects Of Trifluoromethylaniline Isomers On Enzyme Activities In Lymphatic Organs And Hematology Of The Rat. Toxicology. 1994 Sep 6;92(1-3):27-38. [参考文献]: S J Brown, Et Al. A Cdna Encoding Human Ribosomal Protein S24. Gene. 1990 Jul 16;91(2):293-6.
合成参考文献
摘要:Vrána, J.; Růžička, A., Science of Synthesis Knowledge Updates, (2021) 2, 31. 摘要:Lubell, W. D.; St-Cyr, D. J.; Dufour-Gallant, J.; Hopewell, R.; Boutard, N.; Kassem, T.; Dörr, A.; Zelli, R., Science of Synthesis Knowledge Updates, (2013) 1, 176. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 149. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 257. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 113.