摘要:
Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.
摘要:
Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.
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:
A process for making a compound of formula I and intermediate compounds thereof, wherein R1 is CN, F or Cl; R2 is H or Br; and R3 and R4 are each independently H or F. The compounds of formula I are useful in the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.
摘要:
A process for making a compound of formula I and intermediate compounds thereof, wherein R1 is CN, F or Cl; R2 is H or Br; and R3 and R4 are each independently H or F. The compounds of formula I are useful in the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.
摘要:
The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.
摘要:
The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is 0 or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.