Compound 1 Amine Solvate Purification and Stable Polymorphs

The patent changes the physical-chemical parameters of the compound by forming amine solvates, which alters the purification mechanism from chromatographic separation based on adsorption to crystallization-based separation based on solubility differences. This enables high-purity product obtention through simple filtration and washing operations, eliminating the need for complex column chromatography while maintaining regulatory purity requirements

The patent introduces amine solvates as an intermediary form of the compound during the purification process. The amine solvate acts as a temporary intermediate that facilitates impurity removal through differential solubility and crystallization, allowing the main compound to be purified without direct use of complex chromatographic systems. After purification, the solvate can be removed to yield the final pure product

The patent employs inexpensive, readily available amine solvents that can be easily removed after serving their purification function. These solvates act as temporary, disposable intermediaries that enable low-cost purification through simple crystallization and filtration operations, replacing expensive column chromatography equipment and materials. The amine solvents are typically removed by evaporation or simple washing, leaving the purified product without requiring costly chromatographic media

By changing the compound into an amine solvate form, the patent exploits differences in solubility parameters between the solvate and impurities, enabling inexpensive filtration-based purification. This parameter change allows the use of simple, low-cost separation techniques rather than expensive chromatography, significantly reducing manufacturing costs while maintaining high purity levels required for pharmaceutical production

The patent converts the harmful effect of impurity generation into a beneficial purification mechanism. By forming amine solvates, the patent creates a situation where impurities remain in the mother liquor while the main compound crystallizes out in pure form. The impurities that were previously problematic become the basis for separation, allowing the synthesis process to yield high-purity product directly without requiring extensive additional purification steps

The patent performs preliminary action by forming the amine solvate during or immediately after the synthesis step, before final product isolation. This preliminary solvate formation prepares the mixture for efficient separation, allowing impurities to be removed in subsequent simple filtration or washing operations. The preliminary action of solvate formation enables the synthesis process to be more efficient overall by incorporating purification functionality into the synthesis workflow itself