丙二醇甲醚置于乙酸乙烯酯,Candida Antarctica B Lipase On Carrier B体系中,用 Phosphate Buffer 作为反应溶剂,化学反应 3.42H,反应生成 (R)-(-)-1-甲氧基-2-丙醇 参考文献:Rapid Screening Of Hydrolases For The Enantioselective Conversion Of 'difficult-To-Resolve' Substrates 标题:Rapid Screening Of Hydrolases For The Enantioselective Conversion Of 'difficult-To-Resolve' Substrates 摘要:Hydrolases Showing High Enantio Selectivity Towards Three Racemic Alcohols (1-Methoxy-2-Propanol,3-Hydroxy-Tetrahydrofuran,3-Butyn-2-Ol) And Pantolactone Were Identified By A Step-Wise Screening Procedure. Initially,Those Biocatalysts,Which Exhibited Hydrolytic Activity Towards The Corresponding Acetates Or Butyrates,Were Selected Out Of >100 Enzymes. Here,Rapid Screening Was Performed In A Ph-Indicator-Based Format In Microtiter Plates. Subsequently,Enantioselectivity Of Active Hydrolases Was Determined In Small Scale Reactions (Similar To1 Mg Substrate Per Reaction) By Means Of Gas Chromatography Using Chiral Columns. Enzymes Exhibiting Highest Enantioselectivities Were Then Chosen For Preparative Scale Resolution. Using This Strategy,At Least One Suitable Hydrolase Was Found For 3 Out Of The 4 Model Compounds Examined,Allowing Efficient Kinetic Resolution. Moreover,In All Cases Enantiocomplementary Enzymes Were Identified Thus Enabling Access To Both Enantiomers Of All Substrates. (C) 2001 Elsevier Science Ltd. All Rights Reserved. DOI:10.1016/s0957-4166(00)00465-1
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:CN-108299221-A 优先权日:2017-01-13 标题:A new method for the synthesis of (S)-metolachlor (Kindur) and its analogues
参考文献:10.1002/bit.21034 摘要:Berendsen WR, Gendrot G, Freund A, Reuss M. A kinetic study of lipase-catalyzed reversible kinetic resolution involving verification at miniplant-scale. Biotechnol Bioeng. 2006 Dec 05;95(5):883–92. doi: 10.1002/bit.21034.