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Sulfonyl-Containing Nucleoside Phosphotriesters And
Sulfonyl-Containing Nucleoside Phosphotriesters and Phosphoramidates as Novel Anticancer Prodrugs of 5-Fluoro-2´-Deoxyuridine-5´- Monophosphate (FdUMP) Yuan-Wan Sun, Kun-Ming Chen, and Chul-Hoon Kwon†,* †Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John’s University, Jamaica, New York 11439 * To whom correspondence should be addressed. Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John’s University, 8000 Utopia parkway, Jamaica, NY 11439. Tel: (718)-990-5214, fax: (718)-990-6551, e-mail: [email protected]. Abstract A series of sulfonyl-containing 5-fluoro-2´-deoxyuridine (FdU) phosphotriester and phosphoramidate analogues were designed and synthesized as anticancer prodrugs of FdUMP. Stability studies have demonstrated that these compounds underwent pH dependent β-elimination to liberate the corresponding nucleotide species with half-lives in the range of 0.33 to 12.23 h under model physiological conditions in 0.1M phosphate buffer at pH 7.4 and 37 °C. Acceleration of the elimination was observed in the presence of human plasma. Compounds with FdUMP moiety (4-9) were considerably more potent than those without (1-3) as well as 5-fluorouracil (5-FU) against Chinese hamster lung fibroblasts (V-79 cells) in vitro. Addition of thymidine (10 µM) reversed the growth inhibition activities of only 5-FU and the compounds with FdUMP moiety, but had no effect on those without. These results suggested a mechanism of action of the prodrugs involving the intracellular release of FdUMP. Introduction 5-Fluoro-2´-deoxyuridine-5´-monophosphate (FdUMP) is the major metabolite responsible for the anticancer activity of 5-FU (Chart 1). -
Ereztech LLC P3553 Safety Data Sheet
EREZTECH LLC 11555 Medlock Bridge Road, Suite 100, Johns Creek, GA 30097, USA T: +1.888.658.1221 F: 1.678.619.2020 E: [email protected] W: https://ereztech.com Section 1. Identification Product Name: Phosphorus trifluoride Product Type: Gas CAS Number: 7783-55-3 Product Number: P3553 Product Manufacturer: Ereztech LLC 11555 Medlock Bridge Road, Suite 100 Johns Creek, GA 30097 Product Information: (888) 658-1221 In Case of an Emergency: CHEMTREC: 1-800-424-9300 (USA); +1 703-527-3887 (International); CCN836180 *** Contact manufacturer for all non-emergency calls. Section 2. Hazards Identification Appearance/Odor: Colorless, odorless gas. Classification: ACUTE TOXICITY, ORAL - Category 4, H302 ACUTE TOXICITY, DERMAL - Category 4, H312 SKIN CORROSION/IRRITATION - Category 1B, H314 SERIOUS EYE DAMAGE/EYE IRRITATION - Category 2, H318 ACUTE TOXICITY, INHALATION - Category 1, H330 SPECIFIC TARGET ORGAN TOXICITY, SINGLE EXPOSURE; RESPIRATORY TRACT IRRITATION – Category 3, H335 GHS Label Elements Hazard Pictograms: Signal Word: DANGER Hazard Statements: H302: Harmful if swallowed. H312: Harmful in contact with skin. H314: Causes severe skin burns and eye damage. H318: Causes serious eye damage. H330: Fatal if inhaled. H335: May cause respiratory irritation. Ereztech P3553 Page 1 of 13 Revision: 1.00 Date of Issue: 11/27/2020 Phosphorus trifluoride Safety Data Sheet Section 2. Hazards Identification Precautionary Statements Prevention: P260: Do not breathe fumes/gases/mists/vapors/sprays. P264: Wash skin thoroughly after handling. P270: Do not eat, drink or smoke when using this product. P271: Use only outdoors or in a well-ventilated area. P280: Wear protective gloves/ protective clothing/ eye protection/ face protection. -
Hans Renata – Strategic Redox Relay Enables a Scalable Synthesis Of
Strategic Redox Relay Enables A Scalable Synthesis of Ouabagenin, A Bioactive Cardenolide A thesis presented by Hans Renata to The Scripps Research Institute Graduate Program in partial fulfillment of the requirements for the degree of Doctor of Philosophy in the subject of Chemistry for The Scripps Research Institute La Jolla, California February 2013 UMI Number: 3569793 All rights reserved INFORMATION TO ALL USERS The quality of this reproduction is dependent upon the quality of the copy submitted. In the unlikely event that the author did not send a complete manuscript and there are missing pages, these will be noted. Also, if material had to be removed, a note will indicate the deletion. UMI 3569793 Published by ProQuest LLC (2013). Copyright in the Dissertation held by the Author. Microform Edition © ProQuest LLC. All rights reserved. This work is protected against unauthorized copying under Title 17, United States Code ProQuest LLC. 789 East Eisenhower Parkway P.O. Box 1346 Ann Arbor, MI 48106 - 1346 © 2013 by Hans Renata All rights reserved ! ii! ACKNOWLEDGEMENTS To Phil, thank you for taking me under your wing, the past five years have been a wonderful learning experience. You truly are a fantastic teacher, both in and out of the fumehood and your unbridled enthusiasm, fearlessness and passion for chemistry are second to none. In the words of Kurt Cobain, I am “forever indebted to your priceless advice.” To the members of the Baran lab, in the words of Kurt Cobain, “Our little (?) group has always been and always will until the end.” See what I did there? Oh well, whatever, nevermind. -
1 Abietic Acid R Abrasive Silica for Polishing DR Acenaphthene M (LC
1 abietic acid R abrasive silica for polishing DR acenaphthene M (LC) acenaphthene quinone R acenaphthylene R acetal (see 1,1-diethoxyethane) acetaldehyde M (FC) acetaldehyde-d (CH3CDO) R acetaldehyde dimethyl acetal CH acetaldoxime R acetamide M (LC) acetamidinium chloride R acetamidoacrylic acid 2- NB acetamidobenzaldehyde p- R acetamidobenzenesulfonyl chloride 4- R acetamidodeoxythioglucopyranose triacetate 2- -2- -1- -β-D- 3,4,6- AB acetamidomethylthiazole 2- -4- PB acetanilide M (LC) acetazolamide R acetdimethylamide see dimethylacetamide, N,N- acethydrazide R acetic acid M (solv) acetic anhydride M (FC) acetmethylamide see methylacetamide, N- acetoacetamide R acetoacetanilide R acetoacetic acid, lithium salt R acetobromoglucose -α-D- NB acetohydroxamic acid R acetoin R acetol (hydroxyacetone) R acetonaphthalide (α)R acetone M (solv) acetone ,A.R. M (solv) acetone-d6 RM acetone cyanohydrin R acetonedicarboxylic acid ,dimethyl ester R acetonedicarboxylic acid -1,3- R acetone dimethyl acetal see dimethoxypropane 2,2- acetonitrile M (solv) acetonitrile-d3 RM acetonylacetone see hexanedione 2,5- acetonylbenzylhydroxycoumarin (3-(α- -4- R acetophenone M (LC) acetophenone oxime R acetophenone trimethylsilyl enol ether see phenyltrimethylsilyl... acetoxyacetone (oxopropyl acetate 2-) R acetoxybenzoic acid 4- DS acetoxynaphthoic acid 6- -2- R 2 acetylacetaldehyde dimethylacetal R acetylacetone (pentanedione -2,4-) M (C) acetylbenzonitrile p- R acetylbiphenyl 4- see phenylacetophenone, p- acetyl bromide M (FC) acetylbromothiophene 2- -5- -
US5169929.Pdf
|||||||||||| USOO5169929A United States Patent (19) 11) Patent Number: 5,169,929 Tour et al. 45 Date of Patent: Dec. 8, 1992 (54) LITHIUM/HMPA-PROMOTED SYNTHESIS Noren, et al. Macromolecular Reviews (1971) 5. pp. OF POLY(PHENYLENES) 386-431. Yamamoto, et al. Bulletin Che. Soc. of Japan (1978) 51. 75 Inventors: James M. Tour; Eric B. Stephens, (7) pp. 2091-2097. both of Columbia, S.C. Shacklette, et al. J. Chem. Soc., Chem. Commun. (1982) 73 Assignee: University of South Carolina, pp. 361-362. Columbia, S.C. Ivory, et al. J. Chem. Phys. (1979) 71. (3) pp. 1506-1507. Shacklette, et al. J. Chem. Phys. (1980) 73. (8) pp. 21 Appl. No.: 543,673 4098-4102. 22 Filed: Jun. 25, 1990 Kovacic, et al. J. Org. Chem. (1963) 28. pp. 968-972, 1864-1867. I51) Int. Cl. .............................................. CO8G 61/00 Kovacic, et al. J. Org. Chem. (1964) 29. pp. 100-104, 52 U.S.C. .................................................... 528/397 2416-2420. 58 Field of Search ......................................... 528/397 Kovacic et al. J. Org. Chem. (1966) 31. pp. 2467-2470. (56) References Cited Primary Examiner-John Kight, II U.S. PATENT DOCUMENTS Assistant Examiner-Terressa M. Mosley Attorney, Agent, or Firm-Brumbaugh, Graves, 4,576,688 3/1966 David .................................. 528/397 Donohue & Raymond OTHER PUBLICATIONS 57 ABSTRACT Kovacic, et al. Chem. Rev. (1987) 87, pp. 357-379. Poly(phenylene) that is substantially free of insoluble Elsenbaumer, et al. Handbook of Conducting Polymers material is prepared by the polymerization of a lithi (1986), T. A. Skotheime ed. pp. 213-263. oarylhalide compound in the presence of a polar aprotic Perlstein, Angew. -
Chemical Chemical Hazard and Compatibility Information
Chemical Chemical Hazard and Compatibility Information Acetic Acid HAZARDS & STORAGE: Corrosive and combustible liquid. Serious health hazard. Reacts with oxidizing and alkali materials. Keep above freezing point (62 degrees F) to avoid rupture of carboys and glass containers.. INCOMPATIBILITIES: 2-amino-ethanol, Acetaldehyde, Acetic anhydride, Acids, Alcohol, Amines, 2-Amino-ethanol, Ammonia, Ammonium nitrate, 5-Azidotetrazole, Bases, Bromine pentafluoride, Caustics (strong), Chlorosulfonic acid, Chromic Acid, Chromium trioxide, Chlorine trifluoride, Ethylene imine, Ethylene glycol, Ethylene diamine, Hydrogen cyanide, Hydrogen peroxide, Hydrogen sulfide, Hydroxyl compounds, Ketones, Nitric Acid, Oleum, Oxidizers (strong), P(OCN)3, Perchloric acid, Permanganates, Peroxides, Phenols, Phosphorus isocyanate, Phosphorus trichloride, Potassium hydroxide, Potassium permanganate, Potassium-tert-butoxide, Sodium hydroxide, Sodium peroxide, Sulfuric acid, n-Xylene. Acetone HAZARDS & STORAGE: Store in a cool, dry, well ventilated place. INCOMPATIBILITIES: Acids, Bromine trifluoride, Bromine, Bromoform, Carbon, Chloroform, Chromium oxide, Chromium trioxide, Chromyl chloride, Dioxygen difluoride, Fluorine oxide, Hydrogen peroxide, 2-Methyl-1,2-butadiene, NaOBr, Nitric acid, Nitrosyl chloride, Nitrosyl perchlorate, Nitryl perchlorate, NOCl, Oxidizing materials, Permonosulfuric acid, Peroxomonosulfuric acid, Potassium-tert-butoxide, Sulfur dichloride, Sulfuric acid, thio-Diglycol, Thiotrithiazyl perchlorate, Trichloromelamine, 2,4,6-Trichloro-1,3,5-triazine -
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— Studies on Lithium Acetylide Kenneth N. Campbell and Barbara K. Campbell, The University of Notre Dame In contrast to the large amount of work done on the acetylene derivatives of sodium, potassium and calcium, little attention has been paid to the analogous compounds of lithium. In 1898 Moissani prepared lithium acetylide on a small scale, by the action of acetylene on a liquid ammonia solution of lithium. He reported that lithium acetylide was less soluble in liquid ammonia than sodium acetylide, and that when isolated from the solvent, it was less stable, undergoing decomposition with evolu- tion of acetylene. On the basis of the weight of lithium acetylide obtained from a given weight of lithium, and from the amount of acetylene liberated on hydrolysis, he assigned to lithium acetylide the formula C2Li2.C2H2.2NH3. Since that time no references to lithium acetylide or lithium alkylacetylides have appeared in the literature. It was the pur- pose of the present work, therefore, to prepare and analyze lithium acetylide and a lithium alkylacetylide, and to compare their reactions with those of the better known sodium derivatives. Experimental Procedure Preparation of Lithium and Sodium Acetylides.—Acetylene gas, washed by bubbling through concentrated sulfuric acid, was passed into two liters of liquid ammonia, while 7 g. (1 mole) of metallic lithium, cut in small pieces, was added gradually, with stirring, at a rate such that the solution did not develop a permanent deep blue color. When the solution became colorless after the addition of the last piece of lithium, the flow of acetylene was stopped. -
Safety Data Sheet
SAFETY DATA SHEET Preparation Date: 7/21/2017 Revision Date: 7/21/2017 Revision Number: G1 1. IDENTIFICATION Product identifier Product code: S1725 Product Name: SULFUR, LUMP Other means of identification Synonyms: No information available CAS #: 7704-34-9 RTECS # WS4250000 CI#: Not available Recommended use of the chemical and restrictions on use Recommended use: In manufacturing sulfuric acid, carbon disulfide, sulfites, insecticides, plastics, enamels, metal-glass, cements; in vulcanizing rubber; in syntheses of dyes; in making gunpowder, matches; for bleaching wood pulp, straw, wool, silk, felt, linen; in making phosphatic fertilizers; bleaching of dried fruits; fungicide and acaricide; rodent repellent; soil conditioner; nucleating reagent for photographic film; used in cosmetics, such as acne ointments and lotions, and in antidandruff shampoos. Uses advised against No information available Supplier: Spectrum Chemical Mfg. Corp 14422 South San Pedro St. Gardena, CA 90248 (310) 516-8000. Order Online At: https://www.spectrumchemical.com Emergency telephone number Chemtrec 1-800-424-9300 Contact Person: Martin LaBenz (West Coast) Contact Person: Ibad Tirmiz (East Coast) 2. HAZARDS IDENTIFICATION Classification This chemical is considered hazardous according to the 2012 OSHA Hazard Communication Standard (29 CFR 1910.1200) Considered a dangerous substance or mixture according to the Globally Harmonized System (GHS) Flammable solids Category 2 Label elements Warning Flammable solids Product code: S1725 Product name: SULFUR, LUMP 1 / 14 Hazards not otherwise classified (HNOC) Not Applicable Other hazards Not available Precautionary Statements - Prevention Keep away from heat/sparks/open flames/hot surfaces. — No smoking Ground/bond container and receiving equipment Use explosion-proof electrical/ventilating/lighting/.../equipment Wear protective gloves Wear eye/face protection Prevent dust accumulations to minimize explosion hazard In case of fire: Use CO2, dry chemical, or foam to extinguish. -
SOM KINETIC STUDIES OH KETONE FORMATION THESIS Submitted for the Degree of Doctor of Philosophy at Glasgow University Hy Margare
S O M KINETIC STUDIES OH KETONE FORMATION THESIS submitted for the Degree of Doctor of Philosophy at Glasgow University hy Margaret Bennett Thornley May, 1956 Supervisor Dr. R. I. Reed. ProQuest Number: 13848948 All rights reserved INFORMATION TO ALL USERS The quality of this reproduction is dependent upon the quality of the copy submitted. In the unlikely event that the author did not send a complete manuscript and there are missing pages, these will be noted. Also, if material had to be removed, a note will indicate the deletion. uest ProQuest 13848948 Published by ProQuest LLC(2019). Copyright of the Dissertation is held by the Author. All rights reserved. This work is protected against unauthorized copying under Title 17, United States Code Microform Edition © ProQuest LLC. ProQuest LLC. 789 East Eisenhower Parkway P.O. Box 1346 Ann Arbor, Ml 4 8 1 0 6 - 1346 TABLE OF CONTENTS. Page. SUMMARY. 2 Part I. HISTORICAL INTRODUCTION. 5 EXPERIMENTAL RESULTS. 13 Comparison of Reaction Rates in Different Media. 8® THEORETICAL INTERPRETATION OP RESULTS. S3 KINETIC OBSERVATIONS. 38 Dilatometry. 35 Colorimetric Estimation. 39 Chemical Analysis. 40 Experimental Determination. 43 Specimen Results. 44 Dieckmann Ring Closure of Diethyl Pimelate. 46 FORMAL PROOF OF UNIQUE RING FORMATION. 50 Experimental Procedure. 53 PREPARATIVE WORK. 55 Part II. HISTORICAL SURVEY. 59 PRELIMINARY EXPERIMENTAL WORK. 69 Preparation and Analysis of Sodium Salts. 71 KINETIC OBSERVATIONS. 74 Experimental Method. 75 Specimen Results. 76 EXPERIMENTAL RESULTS. 81 Page. EXPERIMENTAL RESULTS. 81 Mathematical Analysis. 82 Effect of Nature of Reaction Vessel. 86 To Investigate the Effect of Reaction Products. 89 Pyrolysis of Disodium (3-methyladipate. -
Chemical Matrix
Chemical Matrix - Ceramics Studio Recommended Personal Protective Key Hazardous Properties Storage Location Disposal Equipment Face Body Hands Protection Respiratory Respiratory Product Form / Phase Key Composition Combustible High Toxicity High Flash Point F Flash Point Plaster Room Plaster Sanitary Drain Sanitary Compressed Gas Compressed Strong Acid/Base Strong Non-Haz Disposal Non-Haz Non-Flam Cabinet Non-Flam Glaze Mixing Room Haz Waste Disposal Waste Haz Flammables Cabinet Flammable/Explosive Potentially SensitizingPotentially MSDS Strong Oxidizer / Reducer Oxidizer Strong Cartirdge Face Shield Nitrile Gloves Nitrile Use with Local Only Exhaust Ventilation with Use Non-Flam Cupboard / Shelving / Counter Cupboard Non-Flam Chemical Splash Apron Chemical Safety Glasses Safety Chemical Flame Resistant Lab Coat Lab Resistant Flame Half Face Respitator with P100 P100 with Respitator Face Half Chemical Protective Gloves per per Gloves Protective Chemical Acetone Liquid Acetone -4 X X X X X X X Albany Slip Powder Silty glacial clay used for pottery, contains up to 30% quartz free silica according to Columbus Clay web X X X X X X MSDS Alumina Hydrate Powder Alumina Hydrate X X X X X X Angelos Copperslip Liquid (thick) Copper oxide, frit 3110, CMC gum, bentonite X X Antimony oxide Powder Antimony oxide X X X X X X X X Baking Soda Powder Sodium bicarbonate X X X X X X X Bell Dark Ball Clay Powder Kaolinite, plus up to 30% quartz free silica X X X X X X Bernard Slip Clay Powder Clay, plus up to 30% silica, some considered respirable according -
Part I. Inversion of Secondary Cyclic Grignard Reagents
This dissertation has been , 69-11,692 microfilmed exactly as received PECHHOLD, Engelbert, 1933- STUDIES OF THE BEHAVIOR AND GENERATION OF GARB ANIONS: PART I. INVERSION OF SECONDARY CYCLIC GRIGNARD REAGENTS. PART II. FRAGMENTATION OF AZOFORMATE SALTS AND ACYLAZO COMPOUNDS WITH BASES. The Ohio State University, Ph.D., 1968 Chemistry, organic University Microfilms, Inc., Ann Arbor, Michigan ©Copyright "by- Engelbert Pechhold 1969 STUDIES OF THE BEHAVIOR MD GENERATION OF CARBANIONS PART I. INVERSION OF SECONDARY CYCLIC GRIGNARD REAGENTS PART II. FRAGMENTATION OF AZOFORMATE SADIS AND ACYLAZO COMPOUNDS WITH BASES DISSERTATION Presented in Partial Fulfillment of the Requirements for the Degree Doctor of Philosophy in the Graduate School of The Ohio State University By Engelbert Pechhold * # # * * # The Ohio State University 1968 Approved by •pV-gpa.-t— Adviser Department of Chemistry DEDICATION To my wife, Ingrid, and my parents, whose love, understanding, and encouragement have made this venture possible. ii ACKNOWLEDaEMElWS I -wish to express my deepest appreciation to Professor Gideon Fraenkel for suggestinf^ this problem, and for his guidance and encouragement throughout the course of this research. His assistance in the preparation of this dissertation is gratefully acknowledged. It is an understatement to say that without his un usual courage of conviction and high standards for academic perfor mance, this work could not have come into being. I owe special debt of gratitude to my colleagues for many suimtü-ating discussions of chemical matters and otherwise. In particular, I wish to express my gratitute to Dr. Don Dix, Dr. Dave Mams, and James Morton, who gave me much insight in ny research. -
WO 2016/074683 Al 19 May 2016 (19.05.2016) W P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2016/074683 Al 19 May 2016 (19.05.2016) W P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C12N 15/10 (2006.01) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (21) International Application Number: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, PCT/DK20 15/050343 DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 11 November 2015 ( 11. 1 1.2015) KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, (25) Filing Language: English PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, (26) Publication Language: English SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: PA 2014 00655 11 November 2014 ( 11. 1 1.2014) DK (84) Designated States (unless otherwise indicated, for every 62/077,933 11 November 2014 ( 11. 11.2014) US kind of regional protection available): ARIPO (BW, GH, 62/202,3 18 7 August 2015 (07.08.2015) US GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (71) Applicant: LUNDORF PEDERSEN MATERIALS APS TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, [DK/DK]; Nordvej 16 B, Himmelev, DK-4000 Roskilde DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, (DK).