Process for the preparation of phenyl 2-pyrimidinyl ketones and their novel intermediates
View Patent ↗A process for the preparation of the compounds of the formula (I), or salts thereof, wherein R represents a hydrogen atom or difluoromethanesulfonyl, characterized in that compounds of the formula (II), or salts thereof, wherein R has the same definition as aforementioned, and n represents 0 or 1, are reacted in the presence of hydrogen peroxide and acetic acid.
1. A process for the preparation of a compound of formula (I) or a salt thereof,
wherein
R is a hydrogen atom or difluoromethanesulfonyl, comprising:
reacting hydrogen peroxide and acetic acid with a compound of formula (II) or a salt thereof,
wherein
R is defined as in the compound of formula (I), and n is 0 or 1.
2. A process according to claim 1 , wherein R is a hydrogen atom.
3. A process according to claim 1 , wherein R is difluoromethanesulfonyl.
4. A process according to claim 1 , wherein said hydrogen peroxide is aqueous.
5. A process according to claim 1 , wherein said acetic acid is 96 to 99.5% aqueous acetic acid.
6. A process according to claim 1 , wherein a compound of formula (II) is reacted with hydrogen peroxide in a ratio of 1 mole of compound (II) to 1 to 5 moles of hydrogen peroxide.
7. A process according to claim l, wherein the reaction is conducted at temperatures in the range of 15° C. to 1200° C.
8. A compound of formula (II) or a salt thereof,
wherein
R is a hydrogen atom or difluoromethanesulfonyl, and n is 0 or 1.
9. A compound in according to claim 8 , wherein R is a hydrogen atom and n is 0.
10. A compound according to claim 8 , wherein R is a hydrogen atom and n is 1.
11. A compound in according to claim 8 , wherein R is difluoromethanesulfonyl and n is 0.
12. A compound according to claim 8 , wherein R is difluoromethanesulfonyl and n is 1.