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- InChIKey: KDLLNMRYZGUVMA-ZYMZXAKXSA-N
- 1S/C18H23FO2/c1-18-7-6-13-12-5-3-11(20)8-10(12)2-4-14(13)15(18)9-16(19)17(18)21/h3,5,8,13-17,20-21H,2,4,6-7,9H2,1H3/t13-,14-,15+,16-,17+,18+/m1/s1/i19-1
- 计算化学: 氢键受体数3.0氢键供体数2.0可旋转键数*
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专利信息
专利号:US-10065985-B2
优先权日:2015-02-03
标题 :Method for fully automated synthesis of 16β-18F-fluoro-5α-dihydrotestosterone (18F-FDHT)
发明人:MURPHY JENNIFER MARIE; LAZARI MARK SAUL
权利人:UNIV CALIFORNIA
摘要:The automated synthesis of clinically relevant amounts of 16β- 18 F-fluoro-5α-dihydrotestosterone ( 18 F-FDHT) using a commercially available radiosynthesizer. Synthesis was performed in 90 minutes with a decay-corrected radiochemical yield of 29±5%. The specific activity was 4.6 Ci/μmol (170 GBq/μmol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated 18 F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.
专利号:US-10695450-B2
优先权日:2016-07-26
标 题 :Synthesis of a radioactive agent composition
发明人:VIOT GILLES
权利人:LABORATOIRES CYCLOPHARMA
摘要:The present invention relates to a method for the synthesis of a radioactive agent composition comprising at least a purification step carried out in the presence of an antioxidant, to the composition obtained by this method comprising radioactive agent and excipient, and to the method for preventing radiolysis of radioactive agent composition comprising the synthesis of said radioactive agent according to the method of the invention.
专利号:US-2022251025-A1
优先权日:2019-05-22
标 题 :Automated ultra-compact microdroplet radiosynthesizer
发明人:VAN DAM R MICHAEL; WANG JIA
权利人:UNIV CALIFORNIA
摘要:A chemical synthesis platform based on a particularly simple chip is described herein, where reactions take place atop a hydrophobic substrate patterned with a circular hydrophilic liquid trap. The overall supporting hardware (heater, rotating carousel of reagent dispensers, etc.) can be packaged into a very compact format (about the size of a coffee cup). We demonstrate the consistent synthesis of [ 18 F]fallypride with high yield, and show that protocols optimized using a high-throughput optimization platform we have developed can be readily translated to this device with no changes or reoptimization.
专利号:US-11094424-B2
优先权日:2013-10-18
标 题 :Closed evaporation system
发明人:FRANCI XAVIER; LIGNON STEVE; LANGE AUDREY
权利人:GE HEALTHCARE LTD
摘要:The present invention provides a system for evaporating a radioactive fluid, a method for the synthesis of a radiolabelled compound including this system, and a cassette for the synthesis of a radiolabelled compound comprising this system. The present invention provides advantages over known methods for evaporation of a radioactive fluid as it reduces drastically the amount of radioactive gaseous chemicals that are released in the hot cell. It is gentler and more secure compared to the known process and provides access to radiosyntheic processes that may not been acceptable for safety reasons related to release of volatile radioactive gases during evaporation. In addition, the process yields are higher because the radioactive volatiles are labelled intermediate species.
专利号:US-2024116978-A1
优先权日:2022-10-10
标 题:Method of preparing estradiol derivatives by solid-phase synthesis
发明人:OKARVI SUBHANI M; AL-JAMMAZ IBRAHIM
权利人:KING FAISAL SPECIALIST HOSPITAL & RES CENTRE
摘要:The present invention relates to a method of preparing estradiol derivatives and/or estrone derivatives, which are suitable for radiolabeling. The present invention further relates to the estradiol derivatives and/or estrone derivatives, preferably obtained by the method of the present invention, as well as to the use of the estradiol derivatives and/or estrone derivatives for radiolabeling with diagnostic and/or therapeutic radionuclides. The present invention further relates to a method of imaging and/or diagnosis of breast cancer as well as to a method of treatment of breast cancer.
专利号:US-6096874-A
优先权日:1990-10-01
标 题:High affinity tamoxifen derivatives
发明人:WALLACE SIDNEY; YANG DAVID; DELPASSAND EBRAHIM; CHERIF ABDALLAH; QUADRI SYED M
权利人:UNIV TEXAS
摘要:The synthesis of tamoxifen derivatives, most particularly halo, halo alkyl, hydroxy, and amino tamoxifen derivatives is disclosed. The native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule. Particular tamoxifen derivatives of the invention include chloro, bromo, iodo, fluoro, amino and DTPA tamoxifen derivatives, and corresponding lower alkyl halogenated forms. The halogenated tamoxifen derivatives possess superior binding affinities for estrogen receptor rich tissues, such as uterine tissue and breast tissue, relative to unsubstituted native tamoxifen. Radiolabeled forms of the tamoxifen derivatives may be used as highly specific imaging agents for estrogen receptor rich tissues. The fluoro and bromo tamoxifen derivatives are particularly useful for imaging estrogen receptors by PET whereas the iodinated tamoxifens are particularly useful in imaging estrogen receptors by SPECT. Rapid and efficient methods of preparing the tamoxifen derivatives having high specific activity (>6 Ci/μmol) are also disclosed. Aliphatic chain substituted tamoxifen derivatives are shown to possess greater estrogen receptor binding affinity and more potent tumor cell inhibition than tamoxifen or tamoxifen derivatives substituted at other locations on the molecule (i.e., non-aliphatic chain substituted tamoxifen). The tanioxifen derivatives of the present invention may advantageously be used as anti-cancer therapeutic agents to halt estrogen-receptor positive tumors, such as those of breast and uterine tissue. The present invention also provides a hydrophilic DTPA-tamnoxifen analogue, and uses thereof in imaging estrogen receptor positive ER+ lesions.