Patent ID: 7741483
Filing Date: 2010-06-22
Classification: A61P,C07C,C07D

Abstract:
1. A process for preparing a compound of Formula I: wherein R 1 is C 1 -C 4 branched or straight chain alkyl; R R R R R R or their pharmaceutically acceptable salts, the process comprising reacting compound IE with compound IF: wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined above, in an inert solvent in the presence of an organic base as a catalyst as well as an acid neutralizer at −20° C. to 80° C., to obtain compound ID: heating compound ID in an acidic aqueous solution to obtain the compound IA: wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined above, carrying out a cyclization reaction of compound IA by heating and refluxing in an appropriate solution under acidic, basic or neutral condition to obtain compounds of-Formula I: wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined above; or, compounds of Formula I are obtained directly by cyclization of the corresponding compound ID under conditions as follows: a) heating to 100-300° C. in mixture of phosphorus pentoxide, water and tertiary amine, or, b) reacting at room temperature or reacting by heating in basic hydrogen peroxide aqueous solution, or, c) reacting at room temperature or reacting by heating under acidic hydrous or anhydrous condition; or, specific example of compounds of Formula I wherein R compound IC is obtained by reaction between compound IF and compound IE wherein R wherein R 1 , R 2 , R 3 and R 4 are as defined above, then compound IB is obtained by reacting compound IC with chlorosulfonic acid alone or in dichloromethane, chloroform, and other inert or polar non-proton solvents—, wherein R 1 , R 2 , R 3 and R 4 are as defined above, and then acylation reaction occurs between compound IB and proper amines in dichloromethane, chloroform, tertiary amine or other inert or polar non-proton solvents at −78° C. to 100° C. to obtain compounds of Formula I wherein R or, compounds of Formula I are obtained by reacting compound IG with compound IH in the solvents of polar non-proton solvents in the presence of the base as catalyst, wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined above and X represents Cl, Br or I; and optionally, converting the compounds of Formula I into the corresponding salts thereof by reacting with pharmaceutically acceptable acids.