Abstract: The present invention provides a compound of formula 1: wherein R1 is CF3, R2 is H? R3 is H.

Abstract: Processes are provided for purifying a compound of the structure (I): wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.

Abstract: The present invention provides a compound of formula 1: wherein R1 is CF3, R2 is H, R3 is H, and R4 is H.

Abstract: The present invention provides method for making a compound of formula 1: comprising the steps of reacting compounds of formulas 2 and 3: to produce a compound of formula 4: wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula 4 is then converted to the compound of formula 1. The invention further comprises compounds of formulas 3 and 4 and methods for making compounds of formulas 3 and 4.

Abstract: The present invention provides method for making a compound of formula 1: comprising the steps of reacting compounds of formulas 2 and 3: to produce a compound of formula 4: wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula 4 is then converted to the compound of formula 1. The invention further comprises compounds of formulas 3 and 4 and methods for making compounds of formulas 3 and 4.

Abstract: The present invention provides method for making a compound of formula 1: comprising the steps of reacting compounds of formulas 2 and 3: to produce a compound of formula 4: wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula 4 is then converted to the compound of formula 1. The invention further comprises compounds of formulas 3 and 4 and methods for making compounds of formulas 3 and 4.

Abstract: 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.

Abstract: The present invention provides N?-(2-halobenzylidene)sulfonylhydrazides of formula I Compounds of formula I are useful for the manufacture of 1-arylsulfonylindazole 5-HT6 ligands.

Abstract: The present invention provides a process for the manufacture of an arylmethyl-sulfonylarene, R1CH2SO2R2, wherein R1 and R2 are each independently an optionally substituted phenyl or naphthyl group which process comprises reacting an arylmethylhalide, R1CH2-Hal wherein R1 is as defined hereinabove and Hal is Cl, Br or I with a sodium arylsulfinate R2SO2Na wherein R2 is as defined hereinabove in the presence of a base optionally in the presence of a solvent. Also provided is the use of the inventive process in the manufacture of a 3-arylsulfonylindazole 5-HT6 ligand.

Abstract: 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.

Abstract: The present invention provides processes for the preparation of arylalkylsulfonyl halides and heteroarylalkylsufonyl halides of Formula I: Ar—R—SO2—X, that are useful as intermediates in the preparation of pharmaceuticals.

Abstract: Processes are provided for purifying a compound of the structure: wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.

Abstract: The present invention provides method for making a compound of formula 1: comprising the steps of reacting compounds of formulas 2 and 3: to produce a compound of formula 4: wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula 4 is then converted to the compound of formula 1. The invention further comprises compounds of formulas 3 and 4 and methods for making compounds of formulas 3 and 4.

Abstract: The present invention provides processes for the preparation of arylalkylsulfonyl halides and heteroarylalkylsufonyl halides of Formula I: Ar—R—SO2—X, that are useful as intermediates in the preparation of pharmaceuticals.

Abstract: 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.

Abstract: A method for preparing 2,2'-methylene-bis-[6-(2H)-benzotriazol-2-yl)-4-hydrocarbyl phenols] is disclosed. According to the process(i) formaldehyde, a dialkylamine and a 4-hydrocarbyl-6-benzotriazolyl phenol as monomer are mixed;(ii) the mixture is heated to a temperature high enough to remove the water produced by the reaction of the mixture;(iii) thereafter an alkaline catalyst is added with heating for several hours;(iv) the phenol compound precipitates when the reaction mixture is neutralized and solvent for the salt product of the neutralization reaction is added in an amount sufficient to permit stirring.The solid product produced is 2,2'-methylene-bis-[6-(2H-benzotriazol-2-yl)-4-hydrocarbyl phenol] having the formula I: ##STR1## in which each R group is an alkyl group of one to twelve carbons or a cycloalkyl group of five to eight carbons and X is chloro or hydrogen.

Abstract: A method is described for preparing compounds of Formula I and Formula II: ##STR1## R.sub.1 is an alkyl group of one to twelve carbon atoms or a cycloalkyl group of five to eight carbons, X is chloro or hydrogen, and R.sub.2 is an alkoxy group having one to twelve carbons. In accordance with the method:(a) a bis(dialkylamino)methane is formed, preferably by reacting a dialkylamine of the formula HNR.sub.3 R.sub.4 (wherein R.sub.3 and R.sub.4 are independently alkyl groups having three or more carbons) and a solid formaldehyde material to produce the corresponding bis(dialkylamino)methane,(b) a monomer of Formula III or IV ##STR2## in which R.sub.1 is an alkyl group of one to twelve carbons or a cycloalkyl group of five to eight carbons, X is chloro or hydrogen and R.sub.