53937-19-2Relevant articles and documents
Preparation of the iodine-124 derivative of the Bolton-Hunter reagent ([124I]I-SHPP) and its use for labelling a VEGF antibody as a PET tracer
Glaser, Matthias,Carroll, Veronica A.,Collingridge, David R.,Aboagye, Eric O.,Price, Pat,Bicknell, Roy,Harris, Adrian L.,Luthra, Sajinder K.,Brady, Frank
, p. 1077 - 1090 (2002)
This study describes the radioiodination of an antibody specific to the vascular endothelial growth factor (VEGF), VG76e, with [124I]iodine to obtain a novel PET tracer for measurement of angiogenesis. In vitro binding assays showed a significantly higher immunoreactive fraction with the protein labelling reagent N-succinimidyl 3-(4-hydroxy-5-[125I]iodophenyl) propionate ([125I]Bolton-Hunter reagent, [125I]I-SHPP) (34.0 ± 4.0%) as compared with N-succinimidyl 3-[125I]iodobenzoate (10.9 ± 6.4%) or direct radioiodination using [125I]iodide and IodoGen (3.1 ± 3.0%). Consequently, the cyclotron-produced positron-emitting [124I]iodine (T1/2 = 4.2 days) was employed to prepare [124I]I-SHPP. Using an improved radioiodination methodology, [124I]I-SHPP was prepared from sodium [124I] iodide with IodoGen at pH 6.5. The [124I]Bolton-Hunter reagent was isolated with 25-58% (n = 3) radiochemical yield and 88-95% (n = 3) radiochemical purity by the conventional extraction procedure. The conjugate of VG76e with [124I]I-SHPP was prepared with 17-18% (n=3) labelling efficiency and 98% radiochemical purity. The immunoreactive fraction was determined to be 33.5% (n = 2). Copyright
Preparation method 1, 2, 6, 7 - tetrahydro - 8H - indeno [5, 4 - b] furan -8 - ketone
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Paragraph 0053-0057, (2021/09/21)
The invention provides a preparation method of 1, 2, 6, 7 - tetrahydro - 8H - indeno [5, 4 - b] furan -8 - ketone, which comprises the following steps of (1) taking compound II as a raw material, adding a halogenating agent and hydrogen peroxide to halogenate to obtain compound III: 3 - X - 4 - hydroxybenzoic acid. (2) The compound III was mixed with 1 - bromo -2 - chloroethane and an alkali metal hydroxide to give compound IV: 3 - X - 4 - (2 - chloroethoxy) phenylpropionic acid. (3) Compound IV was added to nitrobenzene, and an acylation reagent was added to react to give compound V: 3 - X - 4 - (2 - chloroethoxy) phenylpropionyl chloride. (4) To the reaction system, aluminum trichloride was added to react to give compound VI: 4 - X - 1, 2, 6, 7 - tetrahydro - 8H - indeno [5, 4 - b] furan -8 - ketone. (5) Compound VI was added to toluene, and a palladium carbon and sodium acetate aqueous solution were added to catalyze hydrogenation to give compound I: 1, 2, 6, 7 - tetrahydro - 8H - indeno [5, 4 - b] furan -8 - ketone.