130634-09-2Relevant articles and documents
New Bifunctional Chelator p-SCN-PhPr-NE3TA for Copper-64: Synthesis, Peptidomimetic Conjugation, Radiolabeling, and Evaluation for PET Imaging
Gai, Yongkang,Sun, Lingyi,Hui, Wenqi,Ouyang, Qin,Anderson, Carolyn J.,Xiang, Guangya,Ma, Xiang,Zeng, Dexing
, p. 6892 - 6901 (2016)
Bifunctional chelators play an important role in developing metallic radionuclide-based radiopharmaceuticals. In this study, a new bifunctional ligand, p-SCN-PhPr-NE3TA, was synthesized and conjugated to a very late antigen-4 targeting peptidomimetic, LLP2A, for evaluating its application in 64Cu-based positron emission tomography (PET) imaging. The new ligand exhibited strong selective coordination of Cu(II), leading to a robust Cu complex, even in the presence of 10-fold Fe(III). The LLP2A conjugate of p-SCN-PhPr-NE3TA was prepared and successfully labeled with 64Cu under mild conditions. The conjugate 64Cu-NE3TA-PEG4-LLP2A showed significantly higher specific activity, compared with 64Cu-NOTA-PEG4-LLP2A, while maintaining comparable serum stability. Subsequent biodistribution studies and PET imaging in mice bearing B16F10 xenografts confirmed its favorable in vivo performance and high tumor uptake with low background, rendering p-SCN-PhPr-NE3TA a promising bifunctional chelator for 64Cu-based radiopharmaceuticals.
Synthesis method of nifekalant hydrochloride medical intermediate 2-[3-(4-nitrophenyl) propyl amino] ethyl alcohol
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Paragraph 0019-0023, (2017/04/04)
The invention discloses a synthesis method of nifekalant hydrochloride medical intermediate 2-[3-(4-nitrophenyl) propyl amino] ethyl alcohol. The synthesis method comprises the following steps: adding 2-[3-(4-nitrophenyl) propionylamino] ethyl alcohol and aluminum borohydride into a trifluorothioacetate solution, adding an ethyl acetate solution drop by drop for heating reaction, then cooling, adding a butanone solution and the ethyl acetate solution to continue to carry out heating reaction, adjusting the pH value of the solution, separating out crystals, performing suction filtration, dehydrating with a dehydrating agent, washing, heating and filtration, cooling for crystallization, and performing suction filtration again and decompressed drying, so as to obtain 2-[3-(4-nitrophenyl) propyl amino] ethyl alcohol. Compared with the conventional synthesis method, the synthesis method disclosed by the invention has the advantages that the number of medium procedures of reaction is reduced, the reaction time is shortened, and the reaction yield is increased; meanwhile, a new reaction line is developed, so that the reaction yield can be further increased favorably in the later stage.
Synthesis and pharmacological studies of N-substituted 6-[(2- aminoethyl)amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinediones, novel class III antiarrhythmic agents
Katakami,Yokoyama,Miyamoto,Mori,Kawauchi,Nobori,San-nohe,Kaiho,Kamiya
, p. 3325 - 3330 (2007/10/02)
A series of 6-[(2-aminoethyl)amino]-1,3-dimethyl-2,4(1H,3H)- pyrimidinedione derivatives were synthesized and studied for their class III electrophysiological activity and class II (β-blocking) effects in in vitro and in vivo models. Structure-activity re
