摘要:
Processes for preparing oxindoles, which can be utilized in the preparation of a variety of useful compounds, and methods for minimizing or preventing N-alkylation of amide containing compounds, including oxindoles, are provided. Also provided is a compound of the following structure:
摘要:
Processes for preparing oxindoles, which can be utilized in the preparation of a variety of useful compounds, and methods for minimizing or preventing N-alkylation of amide containing compounds, including oxindoles, are provided. Also provided is a compound of the following structure:
摘要:
Methods and kits for preventing or minimizing the formation of isatin oximes during formation of an isatin from an isonitrosoacetanilide are provided. Also provided are methods and kits for preventing or minimizing the formation of isatin oxime impurities after formation of an isatin from an isonitrosoacetanilide by using a decoy agent in the quenching and/or extraction steps. The isatins can be prepared using a decoy agent and desirably a strong acid. Further provided are methods for preparing isatin oximes.
摘要:
Processes are disclosed for preparing indolinone phenylaminopropanol derivatives, particularly chiral indolinone phenylaminopropanol derivatives of the general formula: The processes disclosed may be used to prepare, inter alia, 7-fluoro-1-[(1S, 2R)-1-(3-fluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one and 7-fluoro-1-[(1S, 2R)-1-(3,5-difluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one. Intermediates of the processes are also disclosed.
摘要:
A novel trifluoroacetylating agent, i.e., N-trifluoroacetylmorpholine, is described. This reagent is useful in the preparation of phenyl and heterocyclic sulfonamide compounds. Methods are therefore described for preparing sulfonamide compounds of the following structure, wherein R1 and R2 are defined herein, using N-trifluoroacetylmorpholine. The sulfonamide compounds that may be prepared as described herein include 5-chloro-thiophene-2-sulfonic acid [(1S,2R)-2-(3,5-difluoro-phenyl)-3,3,3-trifluoro-1-hydroxymethyl-propyl]-amide using N-trifluoroacetylmorpholine.
摘要:
The present invention provides processes for the preparation of compounds of Formula III that are useful in the preparation of pharmaceuticals for the treatment of inflammatory diseases.
摘要:
The present invention concerns processes for the production and purification of compounds of the formula: where R1-R10 are as defined in the specification. Preferred processes of the invention utilize a lithium bis(trimethylsilyl)amide, lithium dicyclohexylamide, or potassium bis(trimethylsilyl)amide base and a R1—X alkylating agent where X is as described in the specification. An alcohol preferably is added to the product solution is used to promote crystallization of the desired product.