Disclosed are a 3-N-cyclopropylmethyl-2-fluorobenzamide compound, a preparation method therefor and the use thereof. The compound has a structure as represented by the following formula I. This compound can be used for the preparation of an m-diamide compound substituted with a 3-N-cyclopropylmethyl derivative. The m-diamide compound substituted with the 3-N-cyclopropylmethyl derivative, when serving as an insecticide, has the characteristics of a good fast-acting property, needing to use a low amount thereof, and being more beneficial for environmental protection. The 3-N-cyclopropylmethyl-2-fluorobenzamide compound is easy to synthesize and has mild conditions, and when used for preparing a m-diamide compound insecticide substituted with a 3-N-cyclopropylmethyl derivative, same is easy to synthesize and has a low synthesis cost and a high yield.

A PSMA-specific agent comprising a compound according to Formula I or Formula II: wherein S.sub.1 is absent or is an organic spacer group comprising 3-10 carbons; A is an amino acid chain comprising 1 to 5 amino acids wherein at least one of the amino acids is selected from glutamic acid and aspartic acid; S2 is absent or is an organic spacer group comprising 1 to 15 carbons and/or 0 to 2 amino acids; I.sub.1 is an imaging group; and I.sub.2 is absent or is an imaging group. The PSMA-specific agents can be used to image PSMA within a tissue region and/or for the treatment of a cancer, such as prostate cancer.

##STR00001##

6-[.sup.18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [.sup.18F]DCFPyL, [.sup.68Ga]HBED-CC-PSMA, [.sup.18F]PSMA-1007 and [Al.sup.18F]HBED-CC-PSMA. Unexpectedly, the 6-[.sup.18F]fluoro-2-alkoxy and 6-[.sup.18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [.sup.18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the .sup.18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[.sup.18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [.sup.68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.

6-[.sup.18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [.sup.18F]DCFPyL, [.sup.68Ga]HBED-CC-PSMA, [.sup.18F]PSMA-1007 and [Al.sup.18F]HBED-CC-PSMA. Unexpectedly, the 6-[.sup.18F]fluoro-2-alkoxy and 6-[.sup.18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [.sup.18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the .sup.18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[.sup.18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [.sup.68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.

The present disclosure provides a method for preparing a nicotinamide mononucleotide cocrystal, and aims to solve the technical problems of larger content/weight difference and inconsistent quality of nicotinamide mononucleotide (NMN) medicines or health care products due to poor fluidity of existing nicotinamide mononucleotide crystals. The method includes the steps of mixing nicotinamide mononucleotide as an active pharmaceutical ingredient with isonicotine as a cocrystal former by adopting solution synthesis and then performing crystal precipitation. The method has the advantages of simple operation and wide application range.

The present disclosure provides a method for preparing a nicotinamide mononucleotide cocrystal, and aims to solve the technical problems of larger content/weight difference and inconsistent quality of nicotinamide mononucleotide (NMN) medicines or health care products due to poor fluidity of existing nicotinamide mononucleotide crystals. The method includes the steps of mixing nicotinamide mononucleotide as an active pharmaceutical ingredient with isonicotine as a cocrystal former by adopting solution synthesis and then performing crystal precipitation. The method has the advantages of simple operation and wide application range.

Provided herein are compounds of formula (I) having activity on a receptor protein tyrosine kinase, wherein R.sup.1, R.sup.2, R.sup.3, A, Q, Z, X and W are set forth in the description, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof.

##STR00001##

The invention relates to a method for the preparation of 2-aminobiphenyls, key intermediates in the preparation of compounds of interest in the agrochemical industry. The process comprises reacting an ortho-substituted aniline and a phenylboro derivative in the presence of a base and a palladium catalyst, said palladium catalyst comprising a palladium source and a biphenyl phosphine ligand of formula (III) or a salt thereof.

##STR00001##

The invention relates to a method for the preparation of 2-aminobiphenyls, key intermediates in the preparation of compounds of interest in the agrochemical industry. The process comprises reacting an ortho-substituted aniline and a phenylboro derivative in the presence of a base and a palladium catalyst, said palladium catalyst comprising a palladium source and a biphenyl phosphine ligand of formula (III) or a salt thereof.

##STR00001##

A new set of bench-stable fluoroalkylphosphines that directly convert C—H bonds in pyridine building blocks, drug-like fragments, and pharmaceuticals, into fluoroalkyl derivatives. No pre-installed functional groups or directing motifs are required. The reaction tolerates a variety of sterically and electronically distinct pyridines and is exclusively selective for the 4-position in most cases. The reaction proceeds via initial phosphonium salt formation followed by sp.sup.2-sp.sup.3 phosphorus ligand-coupling, an underdeveloped manifold for C—C bond formation.