C07C309/73

Aromatic amino acid derivative and positron emission topography (PET) probe using the same

A compound having a structure represented by the general formula (I): ##STR00001##
(wherein n is 0 or 1;
R.sup.1 represents a hydrogen atom (only if n=0), a halogen atom, a C1-C6 alkyl group, a C1-C6 haloalkyl group, an optionally substituted amino group, an optionally substituted phenyl group, a C1-C6 alkylthio group, a C1-C6 alkoxy group, a C1-C6 haloalkoxy group or a C7-C12 aralkyloxy group;
R.sup.2 represents —(CH.sub.2).sub.p—[O(CH.sub.2).sub.q].sub.r—X (wherein X is a halogen atom, p is an integer of 1 to 6, q is an integer of 1 to 4, and r is an integer of 0 to 4);
R.sup.3 represents a hydrogen atom, a C1-C6 alkyl group, a C7-C16 aralkyl group or a C6-C14 aryl group; and
R.sup.4 represents a hydrogen atom or a C1-C6 alkyl group), or a pharmaceutically acceptable salt thereof excels FAMT in terms of the tendency to accumulate intensively in cancer, the affinity for LAT1 and the selectivity for cancer, and can be labeled using an automated synthesizer in clinical settings, and therefore is useful as a highly versatile PET imaging agent.

Aromatic amino acid derivative and positron emission topography (PET) probe using the same

A compound having a structure represented by the general formula (I): ##STR00001##
(wherein n is 0 or 1;
R.sup.1 represents a hydrogen atom (only if n=0), a halogen atom, a C1-C6 alkyl group, a C1-C6 haloalkyl group, an optionally substituted amino group, an optionally substituted phenyl group, a C1-C6 alkylthio group, a C1-C6 alkoxy group, a C1-C6 haloalkoxy group or a C7-C12 aralkyloxy group;
R.sup.2 represents —(CH.sub.2).sub.p—[O(CH.sub.2).sub.q].sub.r—X (wherein X is a halogen atom, p is an integer of 1 to 6, q is an integer of 1 to 4, and r is an integer of 0 to 4);
R.sup.3 represents a hydrogen atom, a C1-C6 alkyl group, a C7-C16 aralkyl group or a C6-C14 aryl group; and
R.sup.4 represents a hydrogen atom or a C1-C6 alkyl group), or a pharmaceutically acceptable salt thereof excels FAMT in terms of the tendency to accumulate intensively in cancer, the affinity for LAT1 and the selectivity for cancer, and can be labeled using an automated synthesizer in clinical settings, and therefore is useful as a highly versatile PET imaging agent.

Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.

Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.

Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.

Preparation method of supercritical carbon dioxide thickener for tight oil and gas reservoir

The present invention disclosed a method for preparing a thickener for tight oil and gas reservoir, which relieves damages. The technical solution includes the following steps: putting a three-flask in ice; adding perfluoroalkyl alcohol, P-toluenesulfonyl chloride and pyridine; reacting for 3 h at 0-20° C.; adding filter paper; ultrasonic dispersing for 1 h; removing the filter paper; washing the solution for 3-5 times by adding dilute hydrochloric acid to collect the intermediate product (I); adding 1,3-dihydroxy-propane-2-tert-butyl carbamate and the intermediate product (I) in another three-flask; adding potassium carbonate and N,N-dimethylformamide; reacting for 4 h at 40° C. to collect the intermediate product (II); adding trifluoroacetic acid and methylene chloride into the intermediate product (II); reacting at 45° C. for 2 h; extracting and vacuum drying; and adding 1,6-hexamethylene diisocyanate; reacting for 2 h to collect the final product (III).

Preparation method of supercritical carbon dioxide thickener for tight oil and gas reservoir

The present invention disclosed a method for preparing a thickener for tight oil and gas reservoir, which relieves damages. The technical solution includes the following steps: putting a three-flask in ice; adding perfluoroalkyl alcohol, P-toluenesulfonyl chloride and pyridine; reacting for 3 h at 0-20° C.; adding filter paper; ultrasonic dispersing for 1 h; removing the filter paper; washing the solution for 3-5 times by adding dilute hydrochloric acid to collect the intermediate product (I); adding 1,3-dihydroxy-propane-2-tert-butyl carbamate and the intermediate product (I) in another three-flask; adding potassium carbonate and N,N-dimethylformamide; reacting for 4 h at 40° C. to collect the intermediate product (II); adding trifluoroacetic acid and methylene chloride into the intermediate product (II); reacting at 45° C. for 2 h; extracting and vacuum drying; and adding 1,6-hexamethylene diisocyanate; reacting for 2 h to collect the final product (III).

Methods for making functionalized fluorinated monomers, fluorinated monomers, and compositions for making the same
11492318 · 2022-11-08 · ·

A method of making a functionalized fluorinated monomer for use in making oligomers and polymers that can be used to improve surface properties of polymer-derived systems, such as coatings. The method of making a functionalized fluorinated monomer includes reacting at least one fluorinated nucleophilic reactant, such as a fluorinated alcohol, with at least one compound containing at least one epoxide group. Other methods include reaction of a fluorinated alcohol with a cyclic carboxylic anhydride. In another embodiment, a method includes reacting a fluorinated mesylate, tosylate or triflate with an amine, alkoxide or phenoxide. In other embodiments, the method includes reacting a fluorinated alcohol with an alkyl halide, or reacting a fluorinated alkyl halide with an amine. The functionalized fluorinated monomers may be used as intermediates and reacted to modify the functional groups thereon. Further, the functionalized fluorinated monomers may be reacted to form polymers or oligomers, or with polymers or oligomers having functional groups to modify the polymer or oligomer through the functional group thereon.

Methods for making functionalized fluorinated monomers, fluorinated monomers, and compositions for making the same
11492318 · 2022-11-08 · ·

A method of making a functionalized fluorinated monomer for use in making oligomers and polymers that can be used to improve surface properties of polymer-derived systems, such as coatings. The method of making a functionalized fluorinated monomer includes reacting at least one fluorinated nucleophilic reactant, such as a fluorinated alcohol, with at least one compound containing at least one epoxide group. Other methods include reaction of a fluorinated alcohol with a cyclic carboxylic anhydride. In another embodiment, a method includes reacting a fluorinated mesylate, tosylate or triflate with an amine, alkoxide or phenoxide. In other embodiments, the method includes reacting a fluorinated alcohol with an alkyl halide, or reacting a fluorinated alkyl halide with an amine. The functionalized fluorinated monomers may be used as intermediates and reacted to modify the functional groups thereon. Further, the functionalized fluorinated monomers may be reacted to form polymers or oligomers, or with polymers or oligomers having functional groups to modify the polymer or oligomer through the functional group thereon.

Inhibitors of ERCC1-XPF and methods of using the same

Compositions and methods for inhibiting the DNA repair protein complex, ERCC1-XPF, and methods to enhance clinical responses to anticancer drugs that interact with DNA such as cisplatin, and to overcome drug resistance due to DNA repair mechanisms, are described.