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Preparation of a MEK Inhibitor and preparation containing same
专利权人:
NOVARTIS AG;ARRAY BIOPHARMA INC.
发明人:
PAUL NICHOLS,PETER J. STENGEL,WEIDONG LIU,DANIEL ZIMMERMANN,MARIE WOLF,WERNER HEINZ CHRISTINE - PACHINGER,DANIEL ANDREAS NIEDERER,MARIAN MISUN,CHRISTOPH MAX KRELL
申请号:
ARP130103796
公开号:
AR099630A1
申请日:
2013.10.18
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
1. Characteristic 1: preparation of (2-hydroxy) - 6 - (4-bromo-2-fluorooffenilamino) - 7-fluoro-3-methyl-3h-benzoic acid-5-compound a (4) carboxylic acid;This process includes the following steps: (a) making a formula compound (1) react and have an appropriate basis for forming an intermediate; (b) making the intermediate react with a formula compound (2) in order to provide a formula compound (3) or a formula hydrate, in which P1 is a protection group; and (c) dissolving the compound so that it becomes Formula (3) or such hydrate in an appropriate solvent or solvent system; and (d) do not protect formula compound (3) or such hydrate containing an appropriate unprotected reagent, in which P1 may be the same or different and an appropriate protective group,a. Claim 12: the procedure of claim 1, which also includes (a) various stages of dissolving compounds, including (I) a solvent system, including an ether and an optional alcohol, and (II) water to provide a solution; (b) Add a crystal bacteria suspension agent to the solution to provide a suspension agent mixture; (c) cool the suspension agent mixture to provide a cooling suspension agent mixture; (d) add water to the cooling suspension agent mixture to provide a treated mixture;(e) Cool the treated mixture to provide a crystalline compound. Requirement 24: preparation of (2-hydroxyoxygen) - 6 - (4-bromo-2-fluorooffenilamino) - 7-fluoro-3-methyl-3h-benzodiazepine-5-carboxyl (compound a);This process includes (a) the steps of dissolving compound A, including (I) a solvent system, which contains an ether, optionally an alcohol, and (II) water to provide a solution; (b) adding a crystalline bacterial suspension to the solution to provide a mixed suspension; (c) Cooling the mixed suspension to provide a cooling suspension mixture; (d) adding water to the cooling suspension mixture to provide a treated mixture; And (E) cooling the treated mixture to provide (2-hydroxyoxygen) - 6 - (4-bromo-2-fluorooffenilamino) - 7-fluo
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