CAS: 2401-24-3; 2-Chloro-5-Methoxyaniline

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2-氯-5-甲氧基苯胺盐酸盐置于sodium Carbonate体系中,用 水 用作溶剂,化学反应生成2-氯-5-甲氧基苯胺
参考文献:(r,S)-[18 F] Ge387的放射合成:一种潜在的pet放射性示踪剂,可对18Kda转运蛋白(tspo)成像,对人基因多态性rs6971的结合敏感性低.
标题:(r,S)-[18 F] Ge387的放射合成:一种潜在的pet放射性示踪剂,可对18Kda转运蛋白(tspo)成像,对人基因多态性rs6971的结合敏感性低.
摘要:转运蛋白(tspo)是神经炎症的生物标志物,是许多神经退行性疾病的标志,已被用作正电子发射断层扫描(pet)靶标.尽管碳同位素标记的同位素寿命短且脑通透性较低,但碳11标记的pk11195仍然是tspo成像最常用的试剂.第二代放射性示踪剂显示了受tspo基因的遗传多态性(rs6971)引起的受试者(低亲和力,高亲和力和低亲和力)之间的亲和力差异.为了克服这些限制,基于tspo药效团探索了一种新的结构支架,其低亲和力/高亲和力(lab / Hab)比与(R)相似(1.2 Vs. 1.3)的类似物研究了-[11 C] Pk11195.参比化合物的合成分六个步骤完成,总收率为9%,并通过八个步骤制备了前体,总产率为8%.参考和前体化合物的手性分离是使用超临界流体色谱法(> 95%ee)进行的.绝对构型由圆二色性确定.手动放射性标记反应条件的优化表明乙腈是100oc的首选溶剂.该放射性标记方法的自动化提供了分别为21
Doi:10.1002/cmdc.201900023

专利信息

专利号:WO-2025119975-A1
优先权日:2023-12-04
标 题:A method for synthesis of harmine
发明人：HETT ROBERT; GRAB HANUSCH; LAGOUTTE ROMAN
权利人:RECONNECT LABS AG
摘要:The invention relates to a method of synthesis of a compound of formula (I), harmine, according to the method comprising a step of transforming the compound of formula (II), into the compound of formula (I). The invention further relates to a compound of formula (II), which is an intermediate in synthesis of harmine according to the present invention.

专利号:US-5231198-A
优先权日:1992-07-06
标题:Asymmetric synthesis of hexahydrodibenzofurans by stereospecific inversion of ortho substituted 2-phenylcyclohexanols
发明人：POWERS MATTEW R; GOLEC FREDERICK A
权利人:RHONE POULENC RORER PHARMA
摘要:This invention relates to the stereospecific process for the preparation, separation and purification of hexahydrodibenzofurans which are used in the preparation of the 5HT 3 compounds. More specifically, the present invention relates to a process for the preparation of substantially optically pure cishexahydrodibenzofuran compounds including at least two chiral fused ring centers which comprises the acidic catalyzed stereospecific ring closure by the intra-molecular inversion of a gamma, i.e. 2', carbon atom of a 2-[(2'-leaving group)cycloalkyl]phenol.

专利号:US-9951011-B2
优先权日:2013-09-20
标题 :Carbazole compounds for in vivo imaging
发明人：TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER
权利人:GE HEALTHCARE LTD
摘要:The present invention concerns in vivo imaging and in particular in vivo imaging of translocator protein (TSPO, formerly known as the peripheral benzodiazepine receptor). An indole-based in vivo imaging agent is provided that overcomes problems relating to known TSPO-binding radiotracers. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said precursor compound. Other aspects of the invention include a method for the synthesis of the in vivo imaging agent of the invention comprising use of the precursor compound of the invention, a kit for carrying out said method, and a cassette for carrying out an automated version of said method. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.

专利号:US-9220795-B2
优先权日:2011-09-22
标题 :Indole derivatives
发明人：WADSWORTH HARRY JOHN; O'SHEA DENNIS; PASSMORE JOANNA; TRIGG WILLIAM; EEWAN AMANDA; SHAN BO
权利人:GE HEALTHCARE LTD
摘要:An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.

专利号:US-8790619-B2
优先权日:2009-03-27
标题 :Indole derivatives
发明人：WADSWORTH HARRY JOHN; SHAN BO; O'SHEA DENNIS; PASSMORE JOANNA MARIE; TRIGG WILLIAM JOHN; EWAN AMANDA
权利人:WADSWORTH HARRY JOHN; SHAN BO; O'SHEA DENNIS; PASSMORE JOANNA MARIE; TRIGG WILLIAM JOHN; EWAN AMANDA; GE HEALTHCARE LTD
摘要:An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.

专利号:US-12378242-B2
优先权日:2018-06-29
标题 :Inhibiting CREB binding protein (CBP)
发明人：SCHILLER SHAWN E R; HERBERTZ TORSTEN; LI HONGBIN; GRAVES BRADFORD; MISCHKE STEVEN; WEST Angela; DOWNING JENNIFER R; ERICSSON ANNA
权利人:FORMA THERAPEUTICS INC
摘要:The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.