The present application relates to novel 3-phenylpropionic acid derivatives which carry a branched or cyclic alkyl substituent in the 3-position, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.

A method for the manufacture of a bis(ether anhydride) comprises contacting an N-substituted bis(ether phthalimide) with a base under conditions effective to ring open the imides to provide a ring-opened product; and contacting the ring-opened product with an acid under conditions effective to provide a composition comprising the bis(ether anhydride).

A method for the manufacture of a bis(ether anhydride) comprises contacting an N-substituted bis(ether phthalimide) with a base under conditions effective to ring open the imides to provide a ring-opened product; and contacting the ring-opened product with an acid under conditions effective to provide a composition comprising the bis(ether anhydride).

The present invention discloses a pyrazolamide compound of General Formula I having an insecticidal activity and an intermediate of General Formula II used to preparing the compound of General Formula I, wherein R.sub.1 is selected from chloro or CN, R.sub.2 is selected from H, C.sub.1-C.sub.3 alkyl, C.sub.1-C.sub.3 haloalkyl or C.sub.1-C.sub.5 alkoxyalkyl, R.sub.3 is selected from halo or C.sub.1-C.sub.3 haloalkyl, R.sub.4 is selected from halo, and R.sub.5 is selected from H or halo. Compared with the compounds in the prior art, the compound of General Formula I of the present invention has a higher activity at a low concentration. This reduces the amount of the compound used and the residue of the compound in farmland, and is thus environmentally friendly.

A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base:

##STR00001##

In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R.sup.2, G is an electron-withdrawing group, R.sup.1 is hydrogen or a substituent, and two of R.sup.1, R.sup.2 and G may joint together to form a ring. In formula (II), R.sup.3 and R.sup.4 are independently hydrogen or a substituent, R.sup.5 is an electron-withdrawing group, and two of R.sup.3, R.sup.4 and R.sup.5 may joint together to form a ring. The conjugate acid of the base has a pK.sub.a in the range of 1 to 15.

A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base:

##STR00001##

In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R.sup.2, G is an electron-withdrawing group, R.sup.1 is hydrogen or a substituent, and two of R.sup.1, R.sup.2 and G may joint together to form a ring. In formula (II), R.sup.3 and R.sup.4 are independently hydrogen or a substituent, R.sup.5 is an electron-withdrawing group, and two of R.sup.3, R.sup.4 and R.sup.5 may joint together to form a ring. The conjugate acid of the base has a pK.sub.a in the range of 1 to 15.

Disclosed are a compound represented by Formula (1), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, tautomer, enantiomer, or pharmaceutically acceptable diastereomer thereof, a method of preparing the same, and a pharmaceutical composition, which have effects for treatment or prevention of metabolic syndromes, comprising the same: wherein R.sub.1 to R.sub.6, X.sub.1 to X.sub.4, and n are the same as defined in claim 1.

Disclosed are a compound represented by Formula (1), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, tautomer, enantiomer, or pharmaceutically acceptable diastereomer thereof, a method of preparing the same, and a pharmaceutical composition, which have effects for treatment or prevention of metabolic syndromes, comprising the same: wherein R.sub.1 to R.sub.6, X.sub.1 to X.sub.4, and n are the same as defined in claim 1.

The present invention relates to a process for synthesis of a compound according to Formula (A): wherein R.sub.1 is a substituted or unsubstituted aryl having 6 to 20 carbon atoms; preferably substituted or unsubstituted phenyl; R.sub.2 is a straight or branched alkyl having 1 to 12 carbon atoms; and R.sub.3 is a straight or branched alkyl having 1 to 12 carbon atoms; starting from a di-keto compound according to Formula (B) wherein R.sub.3 is as shown above, which compound is converted into a ketoenamine compound according to Formula (C) wherein R.sub.2 and R.sub.3 are as shown above, which ketoenamine compound is then reduced to an amino alcohol according to Formula (D), wherein R.sub.2 and R.sub.3 are as shown above, that is subsequently converted into a compound according to Formula (A): characterized in that the ketoenamine is reduced into an amino alcohol using a nickel aluminium alloy in an aqueous solution of an inorganic base. ##STR00001##

The present invention relates to a process for synthesis of a compound according to Formula (A): wherein R.sub.1 is a substituted or unsubstituted aryl having 6 to 20 carbon atoms; preferably substituted or unsubstituted phenyl; R.sub.2 is a straight or branched alkyl having 1 to 12 carbon atoms; and R.sub.3 is a straight or branched alkyl having 1 to 12 carbon atoms; starting from a di-keto compound according to Formula (B) wherein R.sub.3 is as shown above, which compound is converted into a ketoenamine compound according to Formula (C) wherein R.sub.2 and R.sub.3 are as shown above, which ketoenamine compound is then reduced to an amino alcohol according to Formula (D), wherein R.sub.2 and R.sub.3 are as shown above, that is subsequently converted into a compound according to Formula (A): characterized in that the ketoenamine is reduced into an amino alcohol using a nickel aluminium alloy in an aqueous solution of an inorganic base. ##STR00001##