An object of the present invention is to provide a method for producing a fluorinated organic compound, whereby an iodosylbenzene derivative can be easily separated and recovered. The above object can be achieved by a method for producing a fluorinated organic compound, comprising step A of fluorinating an organic compound (1) by reaction with a fluorine source (3) in the presence of a hypervalent iodine aromatic ring compound (2a), or in the presence of an iodine aromatic ring compound (2b) and an oxidant (2bo); wherein the fluorine source (3) is a fluorine source (3a) represented by formula: MF.sub.n, wherein M is H, a metal of Group 1 of the periodic table, or a metal of Group 2 of the periodic table; and n is 1 or 2; and step B of separating the iodine aromatic ring compound from a reaction liquid after step A is started.

An object of the present invention is to provide a method for producing a fluorinated organic compound, whereby an iodosylbenzene derivative can be easily separated and recovered. The above object can be achieved by a method for producing a fluorinated organic compound, comprising step A of fluorinating an organic compound (1) by reaction with a fluorine source (3) in the presence of a hypervalent iodine aromatic ring compound (2a), or in the presence of an iodine aromatic ring compound (2b) and an oxidant (2bo); wherein the fluorine source (3) is a fluorine source (3a) represented by formula: MF.sub.n, wherein M is H, a metal of Group 1 of the periodic table, or a metal of Group 2 of the periodic table; and n is 1 or 2; and step B of separating the iodine aromatic ring compound from a reaction liquid after step A is started.

The invention relates to a process for the preparation of a compound of formula I comprising a) reacting a compound of formula II in the presence of magnesium or an organometallic reagent of formula III R.sub.1M.sup.2X (III), wherein R.sub.1 is C.sub.I-C.sub.4alkyl; M.sup.2 is Li or Mg and X is halogen or absent; with a compound of formula IV CF.sub.3-C(O)-R.sub.2 (IV), wherein R.sub.2 is halogen, hydroxyl, C.sub.I-C.sub.4alkoxy, (di-C.sub.I-C.sub.4alkyl)amino, OC(O)CF.sub.3, phenoxy or OM.sup.1; wherein M.sup.1 is Lithium, Magnesium, Sodium or Potassium; to a compound of formula V, and b) reacting the compound of formula V with alkali metal fluoride in the presence of catalytic amounts of a phase transfer catalyst in the presence of a polar solvent to the compound of formula I.

##STR00001##

The invention relates to a process for the preparation of a compound of formula I comprising a) reacting a compound of formula II in the presence of magnesium or an organometallic reagent of formula III R.sub.1M.sup.2X (III), wherein R.sub.1 is C.sub.I-C.sub.4alkyl; M.sup.2 is Li or Mg and X is halogen or absent; with a compound of formula IV CF.sub.3-C(O)-R.sub.2 (IV), wherein R.sub.2 is halogen, hydroxyl, C.sub.I-C.sub.4alkoxy, (di-C.sub.I-C.sub.4alkyl)amino, OC(O)CF.sub.3, phenoxy or OM.sup.1; wherein M.sup.1 is Lithium, Magnesium, Sodium or Potassium; to a compound of formula V, and b) reacting the compound of formula V with alkali metal fluoride in the presence of catalytic amounts of a phase transfer catalyst in the presence of a polar solvent to the compound of formula I.

##STR00001##

The invention relates to a process for the preparation of a compound of formula I comprising a) reacting a compound of formula II in the presence of magnesium or an organometallic reagent of formula III R.sub.1M.sup.2X (III), wherein R.sub.1 is C.sub.I-C.sub.4alkyl; M.sup.2 is Li or Mg and X is halogen or absent; with a compound of formula IV CF.sub.3-C(O)-R.sub.2 (IV), wherein R.sub.2 is halogen, hydroxyl, C.sub.I-C.sub.4alkoxy, (di-C.sub.I-C.sub.4alkyl)amino, OC(O)CF.sub.3, phenoxy or OM.sup.1; wherein M.sup.1 is Lithium, Magnesium, Sodium or Potassium; to a compound of formula V, and b) reacting the compound of formula V with alkali metal fluoride in the presence of catalytic amounts of a phase transfer catalyst in the presence of a polar solvent to the compound of formula I.

##STR00001##

A convergent synthetic method for the production of CRAC channel inhibitors is described herein. The synthetic method provides a method for producing highly pure CRAC channel inhibitors for clinical testing.

A convergent synthetic method for the production of CRAC channel inhibitors is described herein. The synthetic method provides a method for producing highly pure CRAC channel inhibitors for clinical testing.

The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.

The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.

The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.