The present invention provides processes for the preparation of ivacaftor using novel intermediates and a process for its preparation.

The present invention provides processes for the preparation of ivacaftor using novel intermediates and a process for its preparation.

Non-lactone carbocyclic modulators of bacterial quorum sensing. Pharmaceutical composition containing such modulators. Methods employing such modulators for modulation of quorum sensing. Compounds are exemplified by those of formula:
A-[Z].sub.n-L1-[Y]NH-L2-HG,
where A is an optionally substituted aryl or heteroaryl group having one or two 5- or 6-member rings with up to 1-3 heteroatoms in a ring, or a substituted or unsubstituted C1-C12 acyclic aliphatic group and HG is an optionally substituted cyclopentyl group. Compounds include those where n is 1 or 0, Z is CO, OCO, COO, NHCO, CONH, NHCONH, O, S, or NH.sub.2, Y is NHCO, COCH.sub.2C(Y1)-, or SO.sub.2, where Y1 is OH, SH, NH.sub.2 or F; and L1 and L2 independently are [CH.sub.2]p1- and [CH.sub.2]p2-, where p1 and p2, independently, are 0 or integers ranging from 1-3.

Non-lactone carbocyclic modulators of bacterial quorum sensing. Pharmaceutical composition containing such modulators. Methods employing such modulators for modulation of quorum sensing. Compounds are exemplified by those of formula:
A-[Z].sub.n-L1-[Y]NH-L2-HG,
where A is an optionally substituted aryl or heteroaryl group having one or two 5- or 6-member rings with up to 1-3 heteroatoms in a ring, or a substituted or unsubstituted C1-C12 acyclic aliphatic group and HG is an optionally substituted cyclopentyl group. Compounds include those where n is 1 or 0, Z is CO, OCO, COO, NHCO, CONH, NHCONH, O, S, or NH.sub.2, Y is NHCO, COCH.sub.2C(Y1)-, or SO.sub.2, where Y1 is OH, SH, NH.sub.2 or F; and L1 and L2 independently are [CH.sub.2]p1- and [CH.sub.2]p2-, where p1 and p2, independently, are 0 or integers ranging from 1-3.

Methods of making compounds of Formula I are disclosed:

##STR00001##

Methods of making compounds of Formula I are disclosed:

##STR00001##

Methods of making compounds of Formula I are disclosed:

##STR00001##

A method for preparing a pyrimidone compound and an important intermediate in which raw materials of the preparation method are cheap, the reaction condition of preparation method is mild, the preparation method is simple to operate, and is safe and controllable, has high total yield, and thus is suitable for industrial production.

A method for preparing a pyrimidone compound and an important intermediate in which raw materials of the preparation method are cheap, the reaction condition of preparation method is mild, the preparation method is simple to operate, and is safe and controllable, has high total yield, and thus is suitable for industrial production.

Methods of making compounds of Formula I are disclosed: ##STR00001##