45results about How to "High radiochemical yield" patented technology

Based on the principle of bioelectronic isosteric replacement, the present invention provides [ 18 F] trifluoromethyl sulfur-containing amino acid PET imaging agent, the PET imaging agent is [ 18 F] Trifluoromethyl‑ L ‑cysteine ​​or [ 18 F] Trifluoromethyl‑ D ‑cysteine; PET imaging agent can also be [ 18 F] Trifluoromethyl‑ L ‑Methionine or [ 18 F] Trifluoromethyl‑ D ‑Methionine. The PET imaging agent has high uptake in tumor tissue and low uptake in normal tissues and organs, and has good tumor specificity; and has high stability in vivo and in vitro, showing good pharmacokinetic properties. The present invention also provides this [ 18 F] Preparation method of trifluoromethyl sulfur-containing amino acid PET imaging agent and its application in tumor diagnosis and curative effect detection.

The invention discloses 18F click labelling transferrin receptor targeting polypeptide T7 as well as a preparation method and application thereof. According to the preparation method, synthesis steps of click chemistry are improved, addition amount of a prosthetic group TsOTEGay is reduced, the addition amount of polypeptide T7 is appropriately increased, feeding ratio of the prosthetic group to the polypeptide T7 is adjusted to be 1:(1-2); after 18F-TEGay is synthesized through reaction, a polypeptide precursor is directly added for carrying out click reaction without carrying out HPLC purification, a 'one-pot two-step' process is adopted for synthesizing 18F-TEG-T7, and finally HPLC purification is carried out; and one purification process is reduced, the whole synthesis and purification time is greatly reduced and can be controlled to be within 120 minutes, radiochemical yield is about 28.26 minus and plus 7.43% (n=3). The optimized 'two-step one-pot' click reaction can be applied to research of 18F labelling polypeptide, and a novel tumor targeted probe can be prepared.

The present invention relates to a process for producing an organic compound comprising an 18F atom. The compounds comprising an 18F can be useful as PET ligands for use in diagnostics and / or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridized carbon atom, with (i) 18F— and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridized carbon atom, in a process for producing an organic compound comprising an 18F atom, which process comprises treating the organoboron compound with (i)18F— and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PGA is independently H or an alcohol protecting group; PGB is H or a carboxylic acid protecting group; each PGC is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4.