C07H5/02

LIQUID-LIQUID EXTRACTION OF DMF

The present invention relates to a method for the chlorination of a sucrose-6-acylate to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate wherein said method includes steps of: (i) combining the sucrose-6-acylate with a chlorinating agent in a reaction vehicle comprising a tertiary amide to afford a mixture; (ii) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1 and 6 positions thereof; and (iii) quenching the product stream of (ii) to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate;
wherein before said quenching, a portion of said tertiary amide is removed by extraction into a solvent in which said tertiary amide is at least partially soluble.

DEVICE AND CASSETTE FOR PERFORMING A PLURALITY OF SYNTHESIS PROCESSES OF PREPARING A RADIOPHARMACEUTICAL IN SERIES

A cassette for performing a plurality of synthesis processes of preparing a radiopharmaceutical in series in a synthesizer, includes: at least one manifold provided with a plurality of valves connectable to and operable by the synthesizer; an anion-exchanger comprising an anionic exchange material; an eluent container comprising an eluent; and a recondition container comprising a reconditioning agent.

DEVICE AND CASSETTE FOR PERFORMING A PLURALITY OF SYNTHESIS PROCESSES OF PREPARING A RADIOPHARMACEUTICAL IN SERIES

A cassette for performing a plurality of synthesis processes of preparing a radiopharmaceutical in series in a synthesizer, includes: at least one manifold provided with a plurality of valves connectable to and operable by the synthesizer; an anion-exchanger comprising an anionic exchange material; an eluent container comprising an eluent; and a recondition container comprising a reconditioning agent.

Liquid-liquid extraction of DMF

The present invention relates to a method for the chlorination of a sucrose-6-acylate to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate wherein said method includes steps of: (i) combining the sucrose-6-acylate with a chlorinating agent in a reaction vehicle comprising a tertiary amide to afford a mixture; (ii) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1 and 6 positions thereof; and (iii) quenching the product stream of (ii) to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate;
wherein before said quenching, a portion of said tertiary amide is removed by extraction into a solvent in which said tertiary amide is at least partially soluble.

Liquid-liquid extraction of DMF

The present invention relates to a method for the chlorination of a sucrose-6-acylate to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate wherein said method includes steps of: (i) combining the sucrose-6-acylate with a chlorinating agent in a reaction vehicle comprising a tertiary amide to afford a mixture; (ii) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1 and 6 positions thereof; and (iii) quenching the product stream of (ii) to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate;
wherein before said quenching, a portion of said tertiary amide is removed by extraction into a solvent in which said tertiary amide is at least partially soluble.

Method of performing a plurality of synthesis processes of preparing a radiopharmaceutical in series, a device and cassette for performing this method

A method of performing a plurality of synthesis processes of preparing a radiopharmaceutical in series includes carrying out a first synthesis run including the steps of: a) providing water containing fluorine-18; b) trapping the fluorine-18 from the water provided in step a) on an anion exchange material; c) eluting the trapped fluorine-18 from the anion exchange material to a reaction vessel of first radiopharmaceutical synthesis cassette; d) preparing a radiopharmaceutical incorporating the eluted fluorine-18 using the first radiopharmaceutical synthesis cassette; where steps a)-d) are repeated in at least one subsequent run using another radiopharmaceutical synthesis cassette; and where the method includes a reconditioning step of the anion exchange material between two consecutive runs. A device for performing this method and a cassette for use in the device are also disclosed.

Method of performing a plurality of synthesis processes of preparing a radiopharmaceutical in series, a device and cassette for performing this method

A method of performing a plurality of synthesis processes of preparing a radiopharmaceutical in series includes carrying out a first synthesis run including the steps of: a) providing water containing fluorine-18; b) trapping the fluorine-18 from the water provided in step a) on an anion exchange material; c) eluting the trapped fluorine-18 from the anion exchange material to a reaction vessel of first radiopharmaceutical synthesis cassette; d) preparing a radiopharmaceutical incorporating the eluted fluorine-18 using the first radiopharmaceutical synthesis cassette; where steps a)-d) are repeated in at least one subsequent run using another radiopharmaceutical synthesis cassette; and where the method includes a reconditioning step of the anion exchange material between two consecutive runs. A device for performing this method and a cassette for use in the device are also disclosed.

Glycan conjugates and methods of use thereof
10342858 · 2019-07-09 · ·

The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions.

Glycan conjugates and methods of use thereof
10342858 · 2019-07-09 · ·

The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions.

PROCESS FOR PRODUCING FLUORINATED COMPOUNDS USING ALCOHOL SOLVENT HAVING CARBONYL GROUP
20190202820 · 2019-07-04 ·

The present invention relates to a process for producing an organic fluoro compound containing [.sup.18F]fluorine. The method of the present invention for producing the organic fluoro compound is not only advantageous for producing the organic fluoro compound with high yield by using the solvent represented by formula 1 for nucleophilic fluorination reaction but also suitable for automatic synthesis of .sup.18F-labeled radiopharmaceuticals due to the excellent solubility of the precursor compound in the solvent.