A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I]

##STR00001##

wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.

The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I]

##STR00001##

wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.

Disclosed is a method for refining 5-fluorouracil, comprising the following steps: dissolving 5-fluorouracil in an organic solvent, preferably DMSO, heating and stirring until dissolved; naturally cooling the filtrate until a crystal is precipitated; filtering, washing a filter cake using a polar solvent, and draining and drying under reduced pressure. By using the new refining method, the content of impurities in 5-fluorouracil may be reduced to less than 0.01%, the product purity is more than 99.98%, and the refining yield is higher than 70%. In addition, the refining method of the present invention has a simple process, convenient operation, low production costs, high product purity, a stable process, and is suitable for industrial production.

Disclosed is a method for refining 5-fluorouracil, comprising the following steps: dissolving 5-fluorouracil in an organic solvent, preferably DMSO, heating and stirring until dissolved; naturally cooling the filtrate until a crystal is precipitated; filtering, washing a filter cake using a polar solvent, and draining and drying under reduced pressure. By using the new refining method, the content of impurities in 5-fluorouracil may be reduced to less than 0.01%, the product purity is more than 99.98%, and the refining yield is higher than 70%. In addition, the refining method of the present invention has a simple process, convenient operation, low production costs, high product purity, a stable process, and is suitable for industrial production.

Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease.

Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease.

The present invention provides a process for the preparation of Tipiracil HCl of Formula (I) and intermediate thereof with improved yields and purities.

##STR00001##

The present invention provides a process for the preparation of Tipiracil HCl of Formula (I) and intermediate thereof with improved yields and purities.

##STR00001##