US 7,094,903 B2 · Processes for the preparation of substituted isoxazoles and 2-isoxazolines

Abstract

Provided are compounds, processes and synthetic intermediates useful for the preparation of compounds of the formula I and IX wherein R1 is selected from the group consisting of hydrogen, trihalomethyl, C1–C6 alkyl and substituted or unsubstituted phenyl; Y is a group of the formula wherein R2 is selected from the group consisting of C1–C6 alkyl, C1–C6 alkanoylamino and amino; and R5 is selected from the group consisting of hydrogen, amino, halogen, hydroxyl, nitro, C1–C6 alkyl, C1–C6 alkoxy, carboxy, C1–C6 trihaloalkyl, cyano, phosphonato, and hydroxyalkyl; and Z is selected from the group consisting of substituted and unsubstituted aryl. Also provided are certain N-acylated analogs of compounds of the formula I and IX, and processes for their preparation.

Claims22

Dependent claims

A compound of the formula IX

wherein R1 is selected from the group consisting of hydrogen, trihalomethyl, C1–C6 alkyl, and a group of the formula II
wherein
R3 and R4 are independently selected from the group consisting of hydrogen, amino, halogen, hydroxyl, nitro, C1–C6 alkyl, C1–C6 alkoxy, carboxy, C1–C6 trihaloalkyl, cyano, alkylsulfonyl, sulfamyl, phosphonato, and hydroxyalkyl;
Y is a group of the formula
wherein
R2 is selected from the group consisting of C1–C6 alkyl, C1–C6 alkanoylamino and amino;
and
R5 is selected from the group consisting of hydrogen, amino, halogen, hydroxyl, nitro, C1–C6 alkyl, C1–C6 alkoxy, carboxy, C1–C6 trihaloalkyl, cyano, phosphonato, and hydroxyalkyl;
and
Z is selected from the group consisting of substituted and unsubstituted carbocylic aromatic systems and heteroaryl;
or
a pharmaceutically acceptable salt thereof.

9 more elements

Dependencies are inferred from the claim text.

Processes for the preparation of substituted isoxazoles and 2-isoxazolines

Life of this patent

Processes for the preparation of substituted isoxazoles and 2-isoxazolines

Life of this patent

Abstract

Claims22