专利号:US-10337033-B2 优先权日:2016-12-30 标 题 :Carbonyl reductase oligomers and their application in synthesis of chiral alcohols 发明人:ZHANG RONGZHEN; XU YAN; LI KUNPENG 权利人:ZHANG RONGZHEN; XU YAN; LI KUNPENG; UNIV JIANGNAN 摘要:Disclosed are methods for the synthesis of chiral alcohols by Sortase A-mediated oxidoreductase oligomers, which relates to the field of biocatalysis. In the present disclosure, oxidoreductase oligomers were used as biocatalysts for chiral alcohol preparation. Compared to wild-type enzymes, the oxidoreductase oligomers significantly improved catalytic activity and thermal stability. The sortase A-mediated oxidoreductase oligomers had 6-8 folds improvement in specific activity over that of the wild-type enzymes. The oligomers displayed a T m value 6-12° C. higher than that of the wild-type, suggesting the sortase A-mediated oxidoreductase oligomers significantly improved thermostability of the enzymes. The oxidoreductase oligomers catalyzed asymmetric transformation to produce (S)-1-phenyl-1,2-ethanediol or (R)-1-phenethyl alcohol within 3-6 hr, with an optical purity of 98%-100% and a yield of 98%-99%.
专利号:US-6630602-B1 优先权日:1998-04-16 标题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them 发明人:BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS 权利人:YISSUM RES DEV CO 摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I:wherein R1 is a methyl or ethyl group; R2 is H, methyl or an ethyl group; R3 is ethyl or a propyl group; and R4 is a hydroxyl or amide group; and the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to. The present invention further relates to a method for the stereoselective synthesis of the 2S and 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.
专利号:US-6969732-B2 优先权日:1999-04-12 标 题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them 发明人:BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS 权利人:YISSUM RES DEV CO 摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I n n R 1 is a methyl or ethyl group; R 2 is H, methyl or an ethyl group; R 3 is ethyl or a propyl group; and R 4 is a hydroxyl or amide group,n nand the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to.n nn The present invention further relates to a method for the stereoselective synthesis of the 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.
专利号:US-6838581-B2 优先权日:2002-12-04 标题:Process for the preparation of enantiomerically pure 3-phenyl-3-hydroxypropylamine 发明人:KUMAR PRADEEP; PANDEY RAJESH KUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to an improved process for the synthesis of enantiomerically pure 3-phenyl-3-hydroxypropylamine of formula I; more particularly the present invention relates to the said process using styrene; n n nthe synthetic strategy features a Sharpless asymmetric dihydroxylation (SAD) route to the target compound, using styrene, a readily accessible starting material gives the optically pure dihydroxy compound (ee >97%; the selective monotosylation of primary alcohol, nucleophilic displacement by cyano and subsequent reduction to amino group furnishes the desired 3-phenyl-3-hydroxypropylamine in enatiomerically pure form, a key intermediate in the synthesis of variety of oxetine related anti-depressant drugs.
专利号:US-2019276389-A1 优先权日:2015-12-18 标题:Synthesis of aryl cyclohexane ester derivatives useful as sensates in consumer products 发明人:WOS JOHN AUGUST; YELM KENNETH EDWARD; BUNKE GREGORY MARK; FREDERICK HEATH ALAN; REILLY MICHAEL; HAUGHT JOHN CHRISTIAN; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Personal care compositions, such as oral care and skin care compositions containing a flavor/perfume system comprising one or more coolants. The pleasant cool sensation provided by a coolant is enhanced in terms of quicker onset, greater intensity, impact or longer duration, which improves appeal and acceptability of the compositions to consumers.
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).
参考标题:Application Of Tethered Ruthenium Catalysts To Asymmetric Hydrogenation Of Ketones, And The Selective Hydrogenation Of Aldehydes 作者:Katherine E. Jolley,Antonio Zanotti‐gerosa,Fred Hancock,Alan Dyke,Damian M. Grainger,Jonathan A. Medlock,Hans G. Nedden,Jacques J. M. Le Paih,Stephen J. Roseblade,Andreas Seger,Vilvanathan Sivakumar,Ivan Prokes,David J. Morris,Martin Wills |发布日期:2012.9.17 摘要:An Improved Method For The Synthesis Of Tethered Ruthenium(II) Complexes Of Monosulfonylated Diamines Is Described, Together With Their Application To The Hydrogenation Of Ketones And Aldehydes. The Complexes Were Applied Directly, In Their Chloride Form, To Asymmetric Ketone Hydrogenation, To Give Products In Excess Of 99% Ee In The Best Cases, Using 30 Bar Of Hydrogen At 60 °C, And To The Selective
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