- Preparation method of sorafenib compound
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The invention discloses a preparation method of a sorafenib compound. The preparation method comprises the following steps of: adopting reaction of 2-chloro-5-aminotrifluorotoluene and sodium cyanateto prepare a compound III, reaction of 4-bromophenol (compound IV) and a compound V to prepare a compound VI, and reaction of the compound VI and the compound III to obtain a final product, i.e., sorafenib (I). The preparation method disclosed by the invention has the beneficial effects that raw materials for reaction are low in cost and easy in obtaining, the process route is simple, the total yield is high, the side products are fewer, so that the preparation method is suitable for industrial production.
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Paragraph 0015; 0028-0036
(2018/09/08)
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- Synthesis of unsymmetrical diarylureas via Pd-catalyzed C-N cross-coupling reactions
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A facile synthesis of unsymmetrical N,N′-diarylureas is described. The utilization of the Pd-catalyzed arylation of ureas enables the synthesis of an array of diarylureas in good to excellent yields from benzylurea via a one-pot arylation-deprotection protocol, followed by a second arylation.
- Breitler, Simon,Oldenhuis, Nathan J.,Fors, Brett P.,Buchwald, Stephen L.
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p. 3262 - 3265
(2011/08/07)
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- Process for the Preparation of a RAF Kinase Inhibitor and Intermediates for Use in the Process
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There is provided a process for preparing sorafenib or a salt thereof comprising the use of a compound of formula (A) wherein R′ is selected from the group consisting of hydrogen, —C(O)OA, —C(O)CX3, —C(O)NH2, —C(O)—NHOH or There is also provided intermediate compounds of general formula (A), N-methyl-4-(4-ureidophenoxy)picolinamide, 4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenylcarbamate derivative and N-methyl-4-(4-(2,2,2-trihaloacetamido)phenoxy)picolinamide, processes for their preparation and their use in the preparation of sorafenib.
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Page/Page column 21
(2010/12/29)
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- PROCESS FOR THE PREPARATION OF A RAF KINASE INHIBITOR AND INTERMEDIATES FOR USE IN THE PROCESS
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There is provided a process for preparing sorafenib or a salt thereof comprising the use of a compound of formula (A), wherein R' is selected from the group consisting of hydrogen, -C(O)OA, -C(O)CX3, - OH C(O)NH2, -C(O)-NHOH or (a). There is also provided intermediate compounds of general formula (A), N-methyl-4-(4-ureidophenoxy)picolinamide, 4-(2- (methylcarbamoyl)pyridin-4-yloxy)phenylcarbamate derivative and N-methyl-4-(4-(2,2,2- trihaloacetamido)phenoxy)picolinamide, processes for their preparation and their use in the preparation of sorafenib.
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Page/Page column 47-48; 54
(2009/04/25)
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