Crystalline Forms of Methyl Isoxazole Herbicide for Stability and Activity

The patent applies parameter changes by transitioning from an amorphous solid form to a crystalline form of the active ingredient. This phase change fundamentally alters the physical and chemical properties, enabling the material to simultaneously achieve high storage stability characteristic of solids and high herbicidal activity through the specific crystalline structure that facilitates better solubility and bioavailability.

The invention utilizes phase transitions by discovering and characterizing a specific crystalline form of the active ingredient. The transition from amorphous to crystalline state provides a stable solid formulation that maintains enhanced herbicidal activity, resolving the contradiction between storage stability and activity by achieving both through the optimized crystal structure.

The patent changes the critical parameter of crystal structure by identifying and characterizing a previously unknown crystalline form with specific X-ray diffraction patterns. This structural parameter change results in a formulation that maintains stability while exhibiting superior herbicidal activity and synergistic effects compared to known crystalline forms.

The invention creates a composite effect by combining the specific crystalline form with a synergistic mixture of stereoisomers (R,R and S,S forms). This composite approach at the molecular level enhances both formulation stability and herbicidal activity, achieving performance beyond what single isomers or amorphous forms can provide.

The patent resolves this contradiction through phase transition from amorphous to crystalline state. The discovered crystalline form maintains the high herbicidal activity associated with the amorphous form while providing the storage stability characteristic of crystalline structures, effectively combining the advantages of both phases.

By changing the physical state parameter from amorphous to crystalline, the invention achieves a formulation that retains the high bioavailability and activity of the amorphous form while gaining the storage stability of crystalline materials through the specific crystal lattice structure.