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2,6-Dibromopyridine 2-amino-4,6-dibromopyridine N-(6-bromo-pyridin-2-yl)acetamide tert-butyl 6-bromopyridin-2-ylcarbamate 3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-6'-ylamine 6-bromo-2-hydroxypyridine 2-amino-6-methoxypyridine 6-ethoxypyridin-2-amine 合成工艺路线路线简述
- 合成目标产物 2-Amino-6-Bromopyridine 主要起始原料 2-Bromo-6-Fluoropyridine
- (文献来源)合成步骤主要原料 2-Bromo-6-Fluoropyridine
2,6-二溴吡啶置于ammonium Hydroxide体系中,用85%的收率获得2-氨基-6-溴吡啶
参考文献:经典和弱氢键对自组装β-Turn模拟物的金属诱导结构的协同作用
标题:经典和弱氢键对自组装β-Turn模拟物的金属诱导结构的协同作用
摘要:通过前所未有的多重非共价相互作用(经典氢键,弱氢键,金属配位,π堆积相互作用),开发并研究了一种新颖的金属诱导模板,用于两个独立的膦配体的自组装.我们的结果解决了弱氢键(whbs)的重要性和能力,这是基于分子识别的自组装过程中重要的有吸引力的相互作用.Whb与经典的氢键一起,可作为将互补单体膦配体特异自组装成超分子杂化结构的促进剂.分子间c的形成通过x射线晶体分析,质谱和NMR光谱分析研究了h...n氢键及其在固态和溶液中的持久性.Dft计算证明了进一步的证据,该计算为提出的构象提供了特定的几何参数,并使我们能够估计参与分子识别过程的氢键所涉及的能量.所提出的模板可以看作是一种新型的自组装β-Turn模拟物或超分子假氨基酸,用于在连接寡肽时使β-Sheet结构成核.
Doi:10.1002/chem.200900662
专利信息
专利号:WO-2021161084-A1
优先权日:2020-02-16
标题 :N-(4-fluorophenyl)-5-phenyl-[1,2,4] triazolo [1,5-a] pyridine-2-carboxamide derivatives and their synthesis thereof
发明人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP
权利人:NINGEGOWDA RAGHU; BANUPRAKASH GOVINDAPPA; CHANDRASHEKHARAPPA SANDEEP
摘要:The present invention relates to the development of novel N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for their different pharmacological activities. It particularly relates to the development of N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives as antiviral, anticancer, antifungal, hypoglycemic, anti-tubercular, sedative, anti-type 2 diabetes activity. It specifically relates to the N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for treatment of H37Rv and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). The present invention also relates to the process for synthesis of N-(4-fluorophenyl)- 5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives. The invention further relates to method for treatment of method for treatment of diseases such as tuberculosis, type 2 diabetes, bacterial, viral and fungal infections. Invention addresses the challenges in working with chemical processes and products by inventing novel reaction methodology that can maximize the desired products and minimize by-products, designing new synthetic schemes that can simplify operations in chemical productions and seeking nontoxic reagent that are inherently environmentally and ecologically benign. Synthesis of novel N-(4- fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives is being employed to develop a novel synthetic methodology and their pharmacological applications. Novel series of N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[l,5-a]pyridine-2-carboxamide derivatives were designed synthesized evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of mycobacterium tuberculosis (MTB). All the synthesized compounds were characterized by spectroscopic methods like Mass, NMR and elemental analysis.
专利号:WO-2024103458-A1
优先权日:2022-11-18
标题 :Ligand and metal iridium complex having proton response function, preparation method therefor, and use thereof
发明人:YIN QIN; RONG NIANXIN
权利人:SHENZHEN INST ADV TECH; SHENZHEN INST OF ADV TECH CAS
摘要:Disclosed are a ligand and a metal iridium complex having proton response function, a preparation method therefor, and use thereof. The ligand having proton response function has a structure represented by formula L below. The metal iridium complex having proton response function can be easily and quickly prepared from simple, easily available starting materials. The complex can be dearomatized and rearomatized in situ during the reaction. This eliminates the need to prepare dearomatization type ligands in advance, thereby reducing the number of synthesis steps and simplifying the process; moreover, the synthesis of such ligands is simple and modular, which is conducive to the establishment of libraries of ligands and complexes. The disclosed metal iridium complex exhibits relatively high catalytic performance in 'hydrogen borrowing' hydrogen transfer reactions.
专利号:US-12172977-B2
优先权日:2019-07-01
标题:2,2-dimethyl-n-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propionamide, method for preparing (6-amino-pyridin-2-yl)-(1-methyl-piperidin-4-yl)-methanone using said compound, and use of said compound in the preparation of lasmiditan
发明人:ARE CELESTE; SÃ?NCHEZ CASALS CARLES; DOBARRO RODRÃ?GUEZ ALICIA
权利人:MOEHS IBERICA SL
摘要:The present invention relates to a new intermediate, (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide) useful in the synthesis of lasmiditan, to a method for obtaining same, to the use of said intermediate for preparing lasmiditan, to a method for preparing lasmiditan making use of said intermediate, and to a method for preparing an intermediate ((6-amino-pyridin-2-yl)-(1-methyl-piperidin-4-yl)-methanone) from (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide).
专利号:US-7884125-B2
优先权日:2008-04-30
标 题:Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues
发明人:STEVENS CHRISTIAN; HEUGEBAERT THOMAS
权利人:UNIV GENT
摘要:The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
专利号:WO-2018151830-A1
优先权日:2017-02-17
标 题:Pyridinyl based apoptosis signal-regulation kinase inhibitors
发明人:JIN BOHAN; DONG QING; HUNG GENE
权利人:FRONTHERA U S PHARMACEUTICALS LLC
摘要:Apoptosis signal-regulating kinase 1 (ASK1) activation and signaling have been reported to play an important role in a broad range of diseases including neurodegenerative, cardiovascular, inflammatory, autoimmunity and metabolic disorders. Disclosed herein is the synthesis of pyridinyl derived therapeutic agents that function as inhibitors of ASK 1 as well as their pharmaceutical compositions and methods of use.
专利号:US-2009275616-A1
优先权日:2008-04-30
标 题 :Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues