专利号:WO-2019202611-A1 优先权日:2018-04-21 标题:An improved process for the synthesis of ivabradine and its pharmaceutically acceptable salts 发明人:NANDEPU Venkateswara Rao; BOPPANA DURGA PRASAD 权利人:METROCHEM API PVT 摘要:: Disclosed herein is an improved process for the preparation of Ivabradine and pharmaceutically acceptable salts thereof. The invention more particularly disclosesthe synthesis of key intermediates viz.,(S)-N-[(4,5-dimethoxybenzocydobut-l-yl)-methyl]-N- (methyl)amine hydrochloride of Formula-II and 3-(3-Iodopropyl)-7,8-dimethoxy-1,3-dihydro-2H-3-benzapin-2-one of Formula-III, and its use in industrial synthesis of Ivabradine and pharmaceutically acceptable salts thereof.
专利号:US-12162849-B2 优先权日:2018-12-21 标题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:The present invention relates to a method of synthesis of compound (I), wherein R1 represents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant.
专利号:US-11427530-B2 优先权日:2018-02-09 标 题 :Synthesis of 4-chlorokynurenines and intermediates 发明人:LEVIN DANIEL; LEEMING PETER; EISENREICH EMERICH; LIU XUEJUN KARL 权利人:VISTAGEN THERAPEUTICS INC 摘要:The invention relates to an overall enantio-specific synthesis of 4-chlorokynurenine compounds, in particular L-4-chlorokynurenine, with improved yields. Large-scale syntheses are disclosed. The invention also relates to novel intermediates in the synthesis of L-4-chlorokynurenine.
专利号:WO-2024012791-A1 优先权日:2022-07-11 标题 :Electrochemical synthesis of pyrazolines and pyrazoles 发明人:BÄR ROBIN MAXIMILIAN; FORD MARK JAMES; KALDAS SHERIF JAMES; WALDVOGEL SIEGFRIED; HOFMANN SILJA; LINDEN MARTIN 权利人:BAYER AG 摘要:The present invention relates to an electrochemical process for the synthesis of pyrazolines and pyrazoles of formula (I). The process can be especially used for the synthesis of the herbicide safener mefenpyr-diethyl.
专利号:WO-2025134140-A1 优先权日:2023-12-19 标题:A method for the synthesis of substituted anthranilic amide compounds, intermediates and salts thereof 发明人:MALVIYA NITIN JAIKANT; SINGH VIPENDER; SHAH JIGARKUMAR HARKISHANDAS; KALE MANOJ GANPAT; KAVITAKE SANTOSH GIRIDHAR; BORHADE AJIT SAHEBRAO; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD 摘要:The present invention discloses a method for the synthesis of compounds of formula (I) or a salt thereof, wherein, R is selected from hydrogen, halogen, cyano, C1-C12 alkyl, C1-C12 haloalkyl, C1-C12 alkoxy, C1-C12 haloalkoxy, or C3-C8 cycloalkyl; R4 is selected from hydrogen, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C1-C12 haloalkyl, C2-C12 haloalkenyl, C2-C12 haloalkynyl, C1-C12 alkoxy, C1-C12 haloalkoxy, C3-C8 cycloalkyl, or C3-C8 cycloalkyl-C1-C10 alkyl; and n represents an integer selected from 0-4. The method further comprises the synthesis of an anthranilic diamide compound of formula (A).
专利号:US-2025205370-A1 优先权日:2022-03-19 标 题:Synthesis of toluidine blue o and a kit for mucosal application 发明人:PANDA SWAGATIKA 权利人:PANDA SWAGATIKA 摘要:The present invention describes synthesis of Toluidine blue O for a formulation to be used for screening and biopsy site identification in oral cancer. The invention discloses two formulations and a method of delivery of the said formulations via a kit. The method described is a reproducible method of synthesis of pharmaceutical grade Toluidine blue O of acceptable purity and good colorimetric value. The present invention also discloses a kit that includes one formulation of a cleaning solution containing an organic acid and another formulation that is a vital stain formulation. The kit is packaged as a dual chamber sprayer having two pump dispensers, that facilitates ready to use, convenient dental chair side delivery, and allows mass screening.
[参考文献]: Anna Baewicz, Et Al. Determination Of Total Iodine In Serum And Urine Samples By Ion Chromatography With Pulsed Amperometric Detection - Studies On Analyte Loss, Optimization Of Sample Preparation Procedures, And Validation Of Analytical Method. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Jul 1:962:141-146. [参考文献]: Bruno Gabriel Lucca, Et Al. Electrodeposition Of Reduced Graphene Oxide On A Pt Electrode And Its Use As Amperometric Sensor In Microchip Electrophoresis. Electrophoresis. 2015 Aug;36(16):1886-93. [参考文献]: Inês C Santos, Et Al. Paired-Ion Electrospray Ionization--Triple Quadrupole Tandem Mass Spectrometry For Quantification Of Anionic Surfactants In Waters. Talanta. 2015 Oct 1:143:320-327. [参考文献]: Jiannan Sun, Et Al. Use Of Ion-Pairing Reagent For Improving Iodine Speciation Analysis In Seaweed By Pressure-Driven Capillary Electrophoresis And Ultraviolet Detection. J Chromatogr A. 2015 Jan 30:1379:112-7. [参考文献]: Leslie J Loh, Et Al. Detection Of Water Contamination From Hydraulic Fracturing Wastewater: A μpad For Bromide Analysis In Natural Waters. Analyst. 2015 Aug 21;140(16):5501-7.
合成参考文献
参考文献:10.1007/s00436-010-1781-6 摘要:Paraud C, Pors I, Rehby L, Chartier C. Absence of ivermectin resistance in a survey on dairy goat nematodes in France. Parasitol Res. 2010 May;106(6):1475–9. doi: 10.1007/s00436-010-1781-6. 参考文献:10.1007/s00415-011-6163-1 摘要:Kahraman D, Eggers C, Schicha H, Timmermann L, Schmidt M. Visual assessment of dopaminergic degeneration pattern in 123I-FP-CIT SPECT differentiates patients with atypical parkinsonian syndromes and idiopathic Parkinson's disease. J Neurol. 2012 Feb;259(2):251–60. doi: 10.1007/s00415-011-6163-1. 参考文献:10.1007/bf00485779 摘要:Headings VE, Tashian RE. A radioimmunoassay for quantifying carbonic anhydrase isozymes in crude lysates. Biochem Genet. 1970 Apr;4(2):285–95. doi: 10.1007/bf00485779. 参考文献:10.7326/0003-4819-155-2-201107190-00017 摘要:Shimazawa R, Ikeda M. Medical management of the acute radiation syndrome. Ann Intern Med. 2011 Jul 19;155(2):135–6. doi: 10.7326/0003-4819-155-2-201107190-00017. 参考文献:10.1007/978-1-61779-252-6_19 摘要:Maghelli N, Tolić-Nørrelykke IM. Laser ablation of the microtubule cytoskeleton: setting up and working with an ablation system. Methods Mol Biol. 2011;777():261–71. doi: 10.1007/978-1-61779-252-6_19.