合成目标产物 1-Methyl-1H-Pyrazole-4-Boronic Acid 主要起始原料 4-Bromo-1-Methylpyrazole And Bis(Pinacolato)Diboron
15803-02-8 = 847818-55-7 反应条件:1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran,Hexane; -90 °C; < -80 °C; 1 H,-90 °C1.2 Reagents: Trimethyl Borate; 0.5 H,-70 °C; -70 °C -> -15 °C1.3 Reagents: Ammonium Chloride Solvents: Water; Neutralized,-15 °C; -15 °C -> Rt; 1 H,Rt 标题:Synthesis Of Pinacol Esters Of 1-Alkyl-1H-Pyrazol-5-Yl- And 1-Alkyl-1H-Pyrazol-4-Ylboronic Acids 作者:Ivachtchenko,Alexandre V.; Kravchenko,Dmitry V.; Zheludeva,Valentina I.; Pershin,Dmitry G. 参考文献:Journal Of Heterocyclic Chemistry 日期:2004 卷标:41(6) 页码:931-939]
1173889-20-7 = 847818-55-7 反应条件:1.1 Reagents: Ammonium Hydroxide Solvents: Methanol,Water; > 15 Min,Rt 标题:Synthesis Of The Hydrazinyl Pyridine Intermediate: Phase-Appropriate Delivery 作者:Wilsily,Ashraf; Mennen,Steven M.; Cosbie,Andrew; Milne,Jacqueline E. 参考文献:Organic Process Research & Development 日期:2017 卷标:21(9) 页码:1286-1293]
15803-02-8 = 847818-55-7 反应条件:1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran; -90 °C1.2 Reagents: Trimethyl Borate; -90 °C 标题:Process Development And Large-Scale Synthesis Of A C-Met Kinase Inhibitor 作者:Stewart,Gavin W.; Brands,Karel M. J.; Brewer,Sarah E.; Cowden,Cameron J.; Davies,Antony J.; Et Al 参考文献:Organic Process Research & Development 日期:2010 卷标:14(4) 页码:849-858]
15803-02-8 = 847818-55-7 反应条件:1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran; -90 °C1.2 Reagents: Trimethyloxonium Tetrafluoroborate; -90 °C1.3 Reagents: Ammonium Chloride; -90 °C 标题:An Improved Synthesis Of 1-Methyl-1H-Pyrazole-4-Boronic Acid Pinacol Ester And Its Corresponding Lithium Hydroxy Ate Complex: Application In Suzuki Couplings 作者:Mullens,Peter R. 参考文献:Tetrahedron Letters 日期:2009 卷标:50(49) 页码:6783-6786
专利号:EP-3567040-B1 优先权日:2013-06-24 标 题 :Method for the preparation of intermediates useful for the synthesis of [1,2,4]-triazolo[4,3-a]pyridines
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-2022204495-A1 优先权日:2019-05-03 标题:Inhibiting trabid 发明人:CAMPBELL ANNE-MARIE; MARCIN Lawrence; KAYSER-BRICKER KATHERINE 权利人:VALO HEALTH INC; INTEGRAL HEALTH HOLDINGS LLC 摘要:The present disclosure is directed to compounds of formulas (I)-(VII), which are useful as modulators of TRABID. The compounds are further useful in the inhibition of TRABID and the treatment of diseases or disorders associated with the inhibition of TRABID. For instance, the disclosure is concerned with compounds and compositions for inhibition of TRABID, methods of treating diseases associated with the inhibition of TRABID (e.g., autoimmune inflammatory diseases including, but not limited to, psoriasis), and methods of synthesis of these compounds.
专利号:EP-3567040-A1 优先权日:2013-06-24 标题 :Method for the preparation of intermediates useful for the synthesis of [1,2,4]-triazolo[4,3-a]pyridines
专利号:WO-2022162606-A1 优先权日:2021-01-30 标 题:Heterocyclic compounds as kinase inhibitor and uses thereof 发明人:YAN ZHIYU; WANG XIAOHUI; LIU HANLAN; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; PENDHARKAR DHANANJAY; JADHAVAR PRADEEP S; SAEED UZMA; KUMAR VIVEK 权利人:SPEROGENIX THERAPEUTICS LTD; INTEGRAL BIOSCIENCES PRIVATE LTD 摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (J), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes such as cancer, idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed. Formula (J)
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 175. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 199. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 102. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).