CAS: 55314-16-4; 1-(3-Pyridyl)-3-(Dimethylamino)-2-Propen-1-One

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123367-26-0 123367-27-1 75415-01-9

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CAS号350-03-8 3-乙酰吡啶 | CAS号4637-24-5 N,N-二甲基甲酰胺二甲基缩醛 | CAS号68-12-2 N,N-二甲基甲酰胺 | CAS号5762-56-1 三(二甲氨基)甲烷 | CAS号5815-08-7 叔丁氧基双(二甲胺基)甲烷 | CAS号6006-65-1 N,N -二甲基甲酰胺二丙缩醛... | CAS号1188-33-6 N,N-二甲基甲酰胺二乙基缩醛 | CAS号404844-11-7 N-[4-甲基-3-(4-吡啶... | CAS号143101-63-7 3-ethoxy-1-pyri... | CAS号45887-08-9 3-(1H-吡唑-3-基)吡啶 | CAS号917392-54-2 4-甲基-3-[[4-(3-吡... | CAS号641569-94-0 4-甲基-3-[[4-(3-吡... | CAS号726169-73-9 阿比特龙 | CAS号66521-66-2 4-(3-吡啶基)-2-嘧啶胺 | CAS号641571-10-0 尼罗替尼 | CAS号152459-95-5 伊马替尼 | CAS号108-78-1 三聚氰胺

3-乙酰基吡啶,N,N-二甲基甲酰胺二乙基缩醛 以 邻二甲苯 作为反应溶剂,化学反应 6.0H,以85%的收率获得产物1-(3-吡啶基)-3-(二甲氨基)-2-丙烯-1-酮
参考文献:伊马替尼中间体和类似物合成的优化方法† ‡
标题:伊马替尼中间体和类似物合成的优化方法† ‡
摘要:我们回顾了伊马替尼合成的经典合成方法,为制备一系列新的伊马替尼类似物提供了一种改进和优化的方法.所提出的方法有效地克服了某些有问题的步骤,节省了时间和劳力,提供了很高的产率和纯度,并具有用于合成许多类似物的潜力.所需胍盐4的形成,是伊马替尼合成的关键步骤之一,几乎是通过合适的苯胺3的盐酸盐与过量的熔融氰胺在没有任何溶剂的情况下反应而定量进行的.纯芳基胺中间体6A-d在亚当催化剂上用氢气将中间体嘧啶5A-D的硝基还原后,可以在很短的反应时间内定量获得.此外,这种优化方法的应用可以扩展到尼罗替尼及其类似物中间体的合成中.
DOI:10.1039/c6Ra09812F

专利信息

专利号:US-8334381-B2
优先权日:2006-11-16
标题 :Process for the preparation of intermediates useful in the synthesis of imatinib
发明人：FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO
权利人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO; ITALIANA SINT SPA
摘要:It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.

专利号:US-5064963-A
优先权日:1990-04-25
标 题 :Process for the synthesis of n-(3-(1h-imidazol-1-yl)phenyl-4-(substituted)-2-pyrimidinamines
发明人：DEAN WILLIAM D
权利人:AMERICAN CYANAMID CO
摘要:The invention provides a novel process for producing N-[3-(1H-imidazol-1-yl)phenyl]-4-(substituted)-2 pyrimidinamine compounds in which the substituent is a 2-pyridinyl, 3-pyrindinyl, 4-pyridinyl, 2-furanyl or 2-thienyl group. The process includes the steps of (1) reacting a 3-(1H-imidazol-1-yl)benzamine with cyanamide and a halogen acid while controlling the pH of the reaction between pH about 2 to abourt 3.5 and recovering a [3-(1H-imidazol-1-yl)phenyl] guanidine dihydrohalide and (2) reacting the [3-(1H-imidazol-1-yl)phenyl] guanidine dihydrohalide so recovered with an appropriately substituted 3-dimethylamino-1-(substituted)-2-propen-1-one and a base at a pH of from about 10.5 to about 11.5 and recovering the N-[3-(1H-imidazol-1-yl)phenyl-4-(substituted)-2-pyrimidamine compound so produced. The novel process provides improved yield and purity by adhering to the stated crucial pH ranges.

专利号:US-2023065387-A1
优先权日:2019-10-14
标题:Synthesis of tyrosine kinase inhibitors

专利号:US-2011097268-A1
优先权日:2006-08-23
标 题 :Radiohaloimatinibs and methods of their synthesis and use in pet imaging of cancers
发明人：BORNMANN WILLIAM; ALAUDDIN MIAN; GELOVANI JURI; GHOSH PRADIP; GUO LIWEI; HAN DONGMEI; MAXWELL DAVID; MUKHOPADHYAY UDAY; PENG ZHENGHONG; SHAVRIN ALEKSANDR; YING YUNMING
权利人:UNIV TEXAS
摘要:We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells.

专利号:CN-108884047-B
优先权日:2016-03-25
标 题 :Intermediates for the synthesis of aryl or heteroaryl substituted 5-hydroxy-1, 7-naphthyridine compounds and methods for their preparation

专利号:US-10738028-B2
优先权日:2016-05-11
标题:Spiro three-membered ring, spiro five-membered ring peptide deformylase inhibitor and use thereof in antibacteria and anti-tumor
发明人：HU WENHAO; LV FENGPING; TANG YANG; LI ZIYAN; CHEN CHEN; WEI JIANHAI; DONG SUZHEN; QIAN YU
权利人:RUDONG RUIEN PHARMACEUTICAL TECH CO LTD
摘要:Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, can affect the energy balance of the cancer cells through inhibiting the peptide deformylase of the mitochondria in the cells, so that the mitochondrial membrane is depolarized, ATP is exhausted and cell apoptosis is promoted, and has good inhibitory activities on many cancer cell strains such as colorectal cancer, leukemia, lung cancer, gastric cancer, cervical cancer, breast cancer, prostatic cancer, liver cancer and osteosarcoma at relatively lower concentrations. The structure of exemplary invention spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitors are represented by one or more of: