专利号:US-2009253913-A1 优先权日:2008-03-06 标题:Process for the preparation of sorafenib and salts thereof 发明人:ROSSETTO PIERLUIGI; MACDONALD PETER LINDSAY; CANAVESI AUGUSTO 权利人:ROSSETTO PIERLUIGI; MACDONALD PETER LINDSAY; CANAVESI AUGUSTO 摘要:Methods for the synthesis of the N-carbamoyl imidazole (I) and its 1:1 adduct with imidazole are provided. Methods for the preparation of these crystalline intermediates in a high state of purity are also provided. These intermediates react cleanly under mild conditions to produce sorafenib in high yield and purity, without generating difficult-to-remove impurities.
专利号:US-7897762-B2 优先权日:2006-09-14 标 题:Kinase inhibitors useful for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:DECIPHERA PHARMACEUTICALS LLC 摘要:The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-3594426-A 优先权日:1966-02-03 标题 :Process for the preparation of tri-organo-boron compounds 发明人:SALVEMINI ANTONIO; SMAI FRANCO 权利人:MONTEDISON SPA 摘要:PROCESS FOR THE PREPARATION OF ORGANOBORON COMPOUNDS OF THE GENERAL FORMULA BR3, WHEREIN R IS AN ALKYL, ARYL, CYCLOALKYL OR ARALKYL RADICAL, FOR USING IN CATALYSTS FOR THE POLYMERIZATION OF VINYL COMPOUNDS IN ORGANIC SYNTHESIS, ETC., BY REACTING THE COMPONENTS OF A GRIGNARD REAGENT OF THE GENERAL FORMULA R.MG.X, WHERE R IS THE AFOREMENTIONED RADICAL AND X IS A HALOGEN FROM THE GROUP OF CHLORINE, BROMINE AND IODINE, WITH A POLYBORATE BORON DERIVATIVE OF THE GENERAL FORMULA (R''O)3B.NB2O3 (WHERE R'' IS AN ALKYL RADICAL HAVING A STRAIGHT OR BRANCHED CHAIN CONTAINING FROM 2 TO 6 CARBON ATOMS, A PHENYL, AN ALKYL SUBSTITUTED-PHENYL OR PHENYL SUBSTITUTED ALKYL, AND N IS A NUMBER EQUAL TO OR UPWARDS OF 1, BUT PREFERABLY LESS THAN 2). THIS GRIGNARD REAGENT IS PREPARED FROM AN RX TYPE COMPOUND AND A SUSPENSION OF MAGNESIUM IN AN INERT ORGANIC HYDROCARBON SOLVENT CONTAINING ONLY CATALYTIC QUANTITIES OF AN ETHER SUCH THAT THE MOLAR RATIO OF ETHERS TO THE RX COMPOUND RANGES SUBSTANTIALLY FROM 0.01 TO 0.5. THE MAGNESIUM MAY BE ACTIVATED WITH SMALL QUANTITIES OF ETHYL IODIDE PRIOR TO ITS INCORPORATION IN THE SUSPENSION.
专利号:CN-102485714-A 优先权日:2011-10-09 标题:Method for synthesis of sorafenib through carbonylation
专利号:CN-102190616-B 优先权日:2010-03-18 标 题:A kind of deuterated synthesis of ω-diphenyl urea and the Method and process of production
[参考文献]: Sara Van Poecke, Et Al. Synthesis And Inhibitory Activity Of Thymidine Analogues Targeting Mycobacterium Tuberculosis Thymidine Monophosphate Kinase. Bioorg Med Chem. 2011 Dec 15;19(24):7603-11. [参考文献]: Sung Hee Hwang, Et Al. Synthesis And Biological Evaluation Of Sorafenib- And Regorafenib-Like Seh Inhibitors. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3732-7.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).