四氟乙烷-Beta-磺内酯置于水体系中,用100%的收率获得2-氟磺酰基二氟乙酸 参考文献:Zn(Odf)2: Preparation And Application In Asymmetric Alkynylation Of Aldehydes 标题:Zn(Odf)2: Preparation And Application In Asymmetric Alkynylation Of Aldehydes 摘要:一种新型路易斯酸zn(Odf)2首次通过商购的3,3,4,4-四氟[1,2]氧硫杂环己烷2,2-二氧化物经四步反应以56%的收率制备得到,并被应用于催化醛的高度对映选择性炔基化反应,在配体(1S,2S)-3-(叔丁基二甲基硅氧基)-2-N,N-二甲基氨基-1-(对硝基苯基)丙烷-1-醇或配体(-)-N-甲基麻黄碱的存在下,以高产率得到相应的炔丙醇,对映体过量率高达99% Ee. Doi:10.1039/b206868K
专利号:US-2018016227-A1 优先权日:2015-02-03 标题:Process for the synthesis of difluoromethyl ether-based compounds 发明人:SLASSI ABDELMALIK; DOVE PETER 权利人:TRILLIUM THERAPEUTICS INC 摘要:The present application relates to a novel process for the preparation of difluoromethyl ether-based derivatives from, for example, aliphatic and aromatic hydroxyl precursors, compositions comprising these compounds and their use, in particular as precursors for medicines for the treatment of diseases, disorders or conditions. In particular, the present application includes the process of preparing compounds of Formula (I), and compositions and uses thereof:
专利号:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:US-9815842-B2 优先权日:2014-05-28 标题 :Pyrazolo pyrimidine derivatives and their use as MALT1 inhibitors 发明人:SOLDERMANN CAROLE PISSOT; QUANCARD JEAN; SCHLAPBACH ACHIM; SIMIC OLIVER; TINTELNOT-BLOMLEY MARINA; ZOLLER THOMAS 权利人:SOLDERMANN CAROLE PISSOT; QUANCARD JEAN; SCHLAPBACH ACHIM; SIMIC OLIVER; TINTELNOT-BLOMLEY MARINA; ZOLLER THOMAS; NOVARTIS AG 摘要:The present invention describes new pyrazolo-pyrimidine derivatives which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
专利号:CN-107382742-A 优先权日:2017-07-30 标题:A new method for the synthesis of aromatic trifluoromethyl-containing intermediate 5-chloro-2-fluoro-4-(trifluoromethyl)aniline hydrochloride
专利号:WO-2016123707-A1 优先权日:2015-02-03 标题:Process for the synthesis of difluoromethyl ether-based compounds
专利号:EP-1339683-B1 优先权日:2000-11-27 标题 :Estrogen receptor modulators 发明人:WILKENING ROBERT R; PARKER DANN LEROY JR; WILDONGER KENNETH J; MENG DONGFANG; RATCLIFFE RONALD W 权利人:MERCK & CO INC 摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.