CAS: 2267-40-5; 3-(Chlorosulfonyl)-4-Fluorobenzoic Acid

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CAS号456-22-4 对氟苯甲酸 | CAS号160819-39-6 3-甲砜基-4-氟苯甲酸甲酯 | CAS号158608-00-5 3-甲砜基-4-氟苯甲酸

对氟苯甲酸置于氯磺酸体系中,化学反应 6.0H,反应生成3-氯磺酰基-4-氟苯甲酸
参考文献:(2-甲基-5-(甲基磺酰基)苯甲酰基)胍na + / H +反向转运抑制剂.
标题:(2-甲基-5-(甲基磺酰基)苯甲酰基)胍na + / H +反向转运抑制剂.
摘要:已显示在心脏缺血和再灌注期间抑制na + / H +交换剂有利于保存细胞完整性和功能性能.本研究的目的是提出有效和选择性的苯甲酰胍作为nhe抑制剂,以用作辅助治疗急性心肌梗塞.在我们的研究过程中,很明显,邻位酰基胍的取代对于化合物的效力至关重要.使用定向原位金属化技术,以羧酸为导向基团,制备了4-氯-和4-氟-2-甲基苯甲酸6和7.使用lda /甲基碘系统,可以将2-甲基延伸至乙基.通过钯催化的交叉偶联反应将4-烷基插入4-溴-2-甲基苯甲酸甲酯(20).从苯甲酸6-19开始,通过一系列标准反应(磺基氯化,还原和甲基化)引入甲基磺酰基.通过钯催化的suzuki反应合成了4-芳基衍生物68-75.用s-,O-和n-亲核试剂以及氰基和三氟甲基进行了4-位的大量亲核取代反应.使用酯法,酰氯或mukaiyama方法,最终将5-(甲基磺酰基)苯甲酸衍生物与过量的胍转化为(5-(甲基磺酰基)苯甲酰基)
Doi:10.1021/jm960768N

专利信息

专利号:US-2025091989-A1
优先权日:2023-09-19
标 题 :Small molecule protein synthesis modulators
发明人：GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.

专利号:US-9527818-B2
优先权日:2012-09-07
标 题:Method for producing sulfonyl amidine compound
发明人：KIKUCHI TAKASHI; YOSHIDA SHINYA; NAKAMURA ATSUSHI; AKIBA TAKAHIRO; YOSHINO TOSHITAKA; NAKAGAWA SHUICHI; SATO KIICHI
权利人:ASTELLAS PHARMA INC
摘要:Provided are a method for producing a sulfonyl amidine compound, which has an excellent gonadotropin releasing hormone receptor antagonism and is useful as a therapeutic agent for gonadotropin-dependent diseases (for example, prostate cancer, breast cancer, endometriosis, uterine fibroid, prostatic hyperplasia, or the like) or a salt thereof, and a synthesis intermediate useful in the production method. The production method of the present invention controls formation of a by-product which is hardly removed unless column purification is conducted and racemization of a target compound, thereby obtaining the target compound with a high purity, and therefore, the production method is suitable for industrial production.