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:WO-2013035102-A1 优先权日:2011-09-05 标 题 :Processes for the preparation of imatinib base and intermediates thereof 发明人:KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD; KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY 摘要:The invention relates to an improved process for the preparation of highly pure imatinib base (99.99% HPLC purity) of formula (I) and the pharmaceutically acceptable acid addition salts thereof. This invention also relates to processes for the preparation of the intermediates in the synthesis of imatinib base.
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:WO-2012022217-A1 优先权日:2010-08-20 标 题 :N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)phenyl]benzamide derivatives, a preparation method and use for synthesis of imatinib thereof
专利号:WO-2021074138-A1 优先权日:2019-10-14 标题:Synthesis of 6-methyl-n1-(4-(pyridin-3-yl)pyrimidin-2-yl)benzene-1,3-diamine
专利号:EP-3333162-A1 优先权日:2016-12-12 标题 :Metod for preparing n-(2-methyl-5-nitrophenyl)-4-(pyridin-3-yl)pyrimidin-2-amine 发明人:NIKLEWICZ PAWEL GRZEGORZ; LAPCZYNSKI RADOSLAW MIECZYSLAW; PLUTA JANUSZ; OWCZAREK ARTUR; KAROLEWICZ BOZENA 权利人:SILESIAN CATALYSTS SP Z O O 摘要:The invention relates to a method for preparing N-(2-Methyl-5-nitrophenyl)-4-(pyridin-3-yl)pyrimidin-2-amine, a compound from the group of 2-aminopyrimidine derivatives, which is the precursor of active pharmaceutical ingredients, in particular imatinib. n The method of production of N-(2-methyl-5-nitrophenyl)-4-(pyridin-3-yl)pyrimidin-2-amine or other 2-pyrimidineamine lies in that 3-(dimethylamino)-1-(3-pyridyl)prop-2-en-1-one, after being mixed with 1-(2-methyl-5-nitrophenyl)-guanidine nitrate and an alkali hydroxide, preferably sodium hydroxide dissolved in a solvent in the form of dimethyl sulfoxide (DMSO), is subjected to coupling reaction under a pressure from 1 to 50 MPa in a rotating microwave field, with an absorbed microwave power volumetric density contained in the range from 1 W/cm 3 to 1 MW/cm 3 . The coupling process is preferably conducted at a temperature from 300 to 773K, wherein the volumetric density of microwave power absorbed by the reaction system under isothermal process conditions is controlled during the synthesis process. n In a variant of the method, the reagents are subjected to coupling reaction in a microwave reactor, in which the reaction vessel is placed in a container equipped with at least two microwave ports supplying microwave energy to the reagents positioned in the reaction vessel by means of electrodes that are isolated from the reagents by a dielectric layer and play the role of coupling elements.