WLI/100 11 Novembre 2011 ACCORD DE MARRAKECH INSTITUANT L
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(12) Patent Application Publication (10) Pub. No.: US 2005/0065361A1 Deshmukh Et Al
US 2005OO65361A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2005/0065361A1 Deshmukh et al. (43) Pub. Date: Mar. 24, 2005 (54) PROCESS FOR PREPARING ALKYLARYL (22) Filed: Sep. 22, 2003 CHLOROFORMATES Publication Classification (76) Inventors: Abdul Rakeeb Abdul Subhan Deshmukh, Maharashtra (IN); Vikas (51) Int. Cl." ........................... C07C 69/74; C07C 69/96 Kalyanrao Gumaste, Maharashtra (IN) (52) U.S. Cl. .............................................................. 558/280 Correspondence Address: (57) ABSTRACT NIXON & VANDERHYE, PC The present invention discloses an improved method for the 1100 N GLEBE ROAD preparation of alky/aryl chloroformates directly from alco 8TH FLOOR hols and triphosgene. This method is simple, mild and ARLINGTON, VA 22201-4714 (US) efficient avoids use of hazardous phosgene. It can be used for the preparation of various aryl as well as alkyl chlorofor (21) Appl. No.: 10/665,410 mates in excellent yields. US 2005/0065361 A1 Mar. 24, 2005 PROCESS FOR PREPARING ALKYLARYL Maligres, K. C. Nicolau, W. Wrasidio Bioorg. Med. Chem. CHLOROFORMATES Lett. 1993, 3, 1051. (c) D. C. Horwell, J. Hughes, J. Hunter, M. C. Pritchard, R. S. Richardson, E. Roberts, G. N. FIELD OF THE INVENTION Woodruff J. Med. Chem., 1991, 34, 404 and tertiary amines as base H. Eckert, B. Forster, Angew. Chem. Int. Ed. Engl., 0001. The present invention relates to a process for 1987,26,894). Hydroquinone is also used in the preparation preparing alkyl/aryl chloroformates. More particularly, the of chloroformates from triphosgene G. Van den Mooter, C. present invention relates to a process for preparing com Samyn, R. Kinget Int. J. Pharm., 1993, 97, 133). -
Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix
United States International Trade Commission Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix USITC Publication 4208 December 2010 U.S. International Trade Commission COMMISSIONERS Deanna Tanner Okun, Chairman Irving A. Williamson, Vice Chairman Charlotte R. Lane Daniel R. Pearson Shara L. Aranoff Dean A. Pinkert Address all communications to Secretary to the Commission United States International Trade Commission Washington, DC 20436 U.S. International Trade Commission Washington, DC 20436 www.usitc.gov Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix Publication 4208 December 2010 (This page is intentionally blank) Pursuant to the letter of request from the United States Trade Representative of December 15, 2010, set forth at the end of this publication, and pursuant to section 1207(a) of the Omnibus Trade and Competitiveness Act, the United States International Trade Commission is publishing the following modifications to the Harmonized Tariff Schedule of the United States (HTS) to implement changes to the Pharmaceutical Appendix, effective on January 1, 2011. Table 1 International Nonproprietary Name (INN) products proposed for addition to the Pharmaceutical Appendix to the Harmonized Tariff Schedule INN CAS Number Abagovomab 792921-10-9 Aclidinium Bromide 320345-99-1 Aderbasib 791828-58-5 Adipiplon 840486-93-3 Adoprazine 222551-17-9 Afimoxifene 68392-35-8 Aflibercept 862111-32-8 Agatolimod -
PHARMACEUTICAL APPENDIX to the TARIFF SCHEDULE 2 Table 1
Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names INN which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service CAS registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. -
Potential Cannabis Antagonists for Marijuana Intoxication
Central Journal of Pharmacology & Clinical Toxicology Bringing Excellence in Open Access Review Article *Corresponding author Matthew Kagan, M.D., Cedars-Sinai Medical Center, 8730 Alden Drive, Los Angeles, CA 90048, USA, Tel: 310- Potential Cannabis Antagonists 423-3465; Fax: 310.423.8397; Email: Matthew.Kagan@ cshs.org Submitted: 11 October 2018 for Marijuana Intoxication Accepted: 23 October 2018 William W. Ishak, Jonathan Dang, Steven Clevenger, Shaina Published: 25 October 2018 Ganjian, Samantha Cohen, and Matthew Kagan* ISSN: 2333-7079 Cedars-Sinai Medical Center, USA Copyright © 2018 Kagan et al. Abstract OPEN ACCESS Keywords Cannabis use is on the rise leading to the need to address the medical, psychosocial, • Cannabis and economic effects of cannabis intoxication. While effective agents have not yet been • Cannabinoids implemented for the treatment of acute marijuana intoxication, a number of compounds • Antagonist continue to hold promise for treatment of cannabinoid intoxication. Potential therapeutic • Marijuana agents are reviewed with advantages and side effects. Three agents appear to merit • Intoxication further inquiry; most notably Cannabidiol with some evidence of antipsychotic activity • THC and in addition Virodhamine and Tetrahydrocannabivarin with a similar mixed receptor profile. Given the results of this research, continued development of agents acting on cannabinoid receptors with and without peripheral selectivity may lead to an effective treatment for acute cannabinoid intoxication. Much work still remains to develop strategies that will interrupt and reverse the effects of acute marijuana intoxication. ABBREVIATIONS Therapeutic uses of cannabis include chronic pain, loss of appetite, spasticity, and chemotherapy-associated nausea and CBD: Cannabidiol; CBG: Cannabigerol; THCV: vomiting [8]. Recreational cannabis use is on the rise with more Tetrahydrocannabivarin; THC: Tetrahydrocannabinol states approving its use and it is viewed as no different from INTRODUCTION recreational use of alcohol or tobacco [9]. -
Chapter 6 Industrial Applications of Multicomponent Reactions (Mcrs)
University of Groningen Innovative multicomponent reactions and their use in medicinal chemistry Zarganes Tzitzikas, Tryfon IMPORTANT NOTE: You are advised to consult the publisher's version (publisher's PDF) if you wish to cite from it. Please check the document version below. Document Version Publisher's PDF, also known as Version of record Publication date: 2017 Link to publication in University of Groningen/UMCG research database Citation for published version (APA): Zarganes Tzitzikas, T. (2017). Innovative multicomponent reactions and their use in medicinal chemistry. University of Groningen. Copyright Other than for strictly personal use, it is not permitted to download or to forward/distribute the text or part of it without the consent of the author(s) and/or copyright holder(s), unless the work is under an open content license (like Creative Commons). Take-down policy If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. Downloaded from the University of Groningen/UMCG research database (Pure): http://www.rug.nl/research/portal. For technical reasons the number of authors shown on this cover page is limited to 10 maximum. Download date: 24-09-2021 CHAPTER 6 INDUSTRIAL APPLICATIONS OF MULTICOMPONENT REACTIONS (MCRS) Chapter contained in the Rodriguez-Bonne book Stereoselectve Multple Bond-Forming Transformatons in Organic Synthesis 2015 by John Wiley & Sons, Inc. Tryfon Zarganes – Tzitzikas, Ahmad Yazbak, Alexander Dömling Chapter 6 INTRODUCTION Multcomponent reactons (MCRs) can be defned as processes in which three or more reactants introduced simultaneously are combined through covalent bonds to form a single product, regardless of the mechanisms and protocols involved.[1] Many basic MCRs are name reactons, for example, Ugi,[2] Passerini,[3] van Leusen,[4] Strecker,[5] Hantzsch,[6] Biginelli,[7] or one of their many variatons. -
Novel Approaches in Clinical Development of Cannabinoid Drugs
Novel approaches in clinical development of cannabinoid drugs Linda Klumpers novel approaches in clinical development of cannabinoid drugs Novel approaches in clinical development of cannabinoid drugs proefschrift ter verkrijging van de graad van Doctor aan de Universiteit Leiden, op gezag van de Rector Magnificus prof. mr. C.J.J.M. Stolker, volgens besluit van het College voor Promoties, te verdedigen op dinsdag 21 januari 2014, klokke 16:15 uur door Linda Elvira Klumpers, geboren te Rotterdam in 1980 Promotiecommissie chapter i 7 Introduction to the endocannabinoid system as a target for drug development promotores Prof. dr. J.M.A. van Gerven chapter ii 49 Professor of Clinical Neuropsychopharmacology, Leiden University Medical Center Novel ∆9-tetrahydrocannabinol formulation Namisol® has bene- and Centre for Human Drug Research ficial pharmacokinetics and promising pharmacodynamic effects Prof. dr. A.F. Cohen Professor of Clinical Pharmacology, Leiden University Medical Center and Centre chapter iii 79 for Human Drug Research Manipulating brain connectivity with ∆9-tetrahydrocannabinol: a pharmacological resting state fmri study overige leden chapter iv 115 Prof. dr. P.H. van der Graaf Surinabant, a selective cb¡ antagonist, inhibits thc-induced Professor of Bio-pharmaceutical Sciences, Leiden University central nervous system and heart rate effects in humans Dr. J.T. Tamsma Internist and Medical Director of the Leiden University Medical Center chapter v 145 Prof. dr. R.F. Witkamp Peripheral selectivity of the novel cannabinoid receptor -
The Preparation of Certain Organic Chloroformates and Carbonates
Brigham Young University BYU ScholarsArchive Theses and Dissertations 1947-04-01 The preparation of certain organic chloroformates and carbonates Robert E. Brailsford Brigham Young University - Provo Follow this and additional works at: https://scholarsarchive.byu.edu/etd BYU ScholarsArchive Citation Brailsford, Robert E., "The preparation of certain organic chloroformates and carbonates" (1947). Theses and Dissertations. 8175. https://scholarsarchive.byu.edu/etd/8175 This Thesis is brought to you for free and open access by BYU ScholarsArchive. It has been accepted for inclusion in Theses and Dissertations by an authorized administrator of BYU ScholarsArchive. For more information, please contact [email protected], [email protected]. THE PREPARATI OH OF CERTAI N 0RG.1NIC CHLOROFORJ.'\Ll.TES AND CARBON T Thesis ubmitted to the Department of Chemistry Brigham Young University ~ .. ... "') .~ . ~ . "'). ... .. .. .. .. , ... .. ... : : ....: . ..-. ~ ..·.: : ..: ...• : ·.. ~ . : ,.. .~ : :. : ·: : ··.... ; ~ : ·. : : .: . : . : : : ••• .... •." •,.r_·: -••• ~ .... In Parti a l Fulfillment of the Re~uirements for the Degree Master of cienoe 147143 by Robert E. Brailsford .tipril 1947 This Thesis by Robert E. Brailsford is accepted in its present farm by the Department of Chemistry of Brigham Young University as satisfying the ·rhesis requirement for the degree of Master of Science. PREFACE flhile working for the Hooker Electrochemical Company of Niagara Falls , New York , from April 3 , 1943 , to January 30 , 1946 , the writer became interested in organic chloroformates and. carbonates , an interest instigated by requests from B. F . Goodrich Company for a number of samples . fter returning to Brigham Young University that preliminary interest was revived and the experi - mental work of this thesis was performed. under the direction of Dr . Charles ' . :Maw and Professor Joseph K. -
Carbonate and Benzyl Benzotriazol-L-Yl Carbonate. Now
70 Bull. Korean Chem. Soc., Vol. 7, No. 1, 1986 Sunggak Kim and Heung Chang t-Butyl Benzotriazol-l-yl Carbonate and Benzyl Benzotriazol-l-yl Carbonate. Now Reactive Amino Protective Reagents for t-Butoxy carbonylation and Benzyloxycarbonylation of Amines and Amino Acids Sunggak Kim* and Heung Chang Department of Chemistry, Korea Advanced Institute of Science and Technology, Seoul 131, Received September24,1985 New amino protective reagents, /-butyl benzotriazol-l-yl carbonate and benzyl benzotriazol-l-yl carbonate, for t~ butoxycarbonylation and benzyloxycarbonylation of amines and amino acids have been developed. f-Butyl benzotriazol-1 -yl carbonate reacts rapidly and cleanly with various amines and amino acids to afford N-Boc amines and N-Boc amino acids in high yields and benzyl benzotriazol-l-yl carbonate is also found to be very effective in the benzyloxycarbonylation of amino acids. Introduction a solution of an equimolar amount of 1-hydroxybenzotriazole and pyridine in methylene chloride to the solution of an ex The Z-butoxycarbonyl (Boc) group is one of the most im cess amount of phosgene in toluene under cooling portant amino protective groups along with benzyloxycarbonyl (-20~ 一 10°C). The resulting product was relatively unstable (Cbz) group in peptide synthesis.1 Since /-butyl chloroformate and was mainly decomposed to 1-hydroxybenzotriazole dur is only fairly stable above 10°C,2 it is difficult to is이 ate t- ing workup with cold water. Thus； benzotriazol-l-yl chlorofor butyl chloroformate as a pure form in high yields. Thus, con mate was used in a crude form. BBC could be prepared readily siderable efforts have been devoted to the development of a by the reaction of benzotriazol-l-yl chloroformate with variety of useful and reliable reagents for the preparation of equimolar amounts of f나 mtyl alcohol and pyridine in N-Boc amino acids during last 30 years.1 methylene chloride at room temperature for 2 h (eq. -
The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters. -
Cannabinoid Receptor Cannabinoid Receptor
Cannabinoid Receptor Cannabinoid Receptor Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol. www.MedChemExpress.com 1 Cannabinoid Receptor Antagonists, Agonists, Inhibitors, Modulators & Activators (S)-MRI-1867 (±)-Ibipinabant Cat. No.: HY-141411A ((±)-SLV319; (±)-BMS-646256) Cat. No.: HY-14791A (S)-MRI-1867 is a peripherally restricted, orally (±)-Ibipinabant ((±)-SLV319) is the racemate of bioavailable dual cannabinoid CB1 receptor and SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent inducible NOS (iNOS) antagonist. (S)-MRI-1867 and selective cannabinoid-1 (CB-1) receptor ameliorates obesity-induced chronic kidney disease antagonist with an IC50 of 22 nM. (CKD). Purity: >98% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg 2-Arachidonoylglycerol 2-Palmitoylglycerol Cat. No.: HY-W011051 (2-Palm-Gl) Cat. No.: HY-W013788 2-Arachidonoylglycerol is a second endogenous 2-Palmitoylglycerol (2-Palm-Gl), an congener of cannabinoid ligand in the central nervous system. 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119. -
Benzyl Chloroformate (CHLOROFORMIC ACID, BENZYL ESTER)
Rev B Benzyl Chloroformate (CHLOROFORMIC ACID, BENZYL ESTER) C8H7O2Cl Molecular Weight = 170.6 CAS# 501‐53‐1 SPECIFICATIONS Assay: 98.% min. Color (APHA): 50 max. Benzyl Alcohol: 0.1% max. Hydrogen Chloride: 0.1% max. Benzyl Chloride: 1.5% max. Phosgene: 0.1% max. Dibenzyl Carbonate: 0.5% max. Iron: 1.5 PPM max. PHYSICAL PROPERTIES Appearance: Clear liquid free of visible contaminants BP: Decomposes at elevated temperature Odor: Pungent Density: 1.195 ‐1.22 MP/Range: ‐30°C Flash Point: 126°C NOTICE: The technical information and suggestions for use made herein are based on VanDeMark’s research and experience and are believed to be reliable, but such information and suggestions do not constitute a warranty, and no patent liability can be assumed. This publication is not to be taken as a license to operate under or infringe on any patents. Since VanDeMark has no control over the conditions under which the product is transported, stored, handled, used or applied, buyer must determine for himself by preliminary tests or otherwise, the suitability of the product for his purposes. VanDeMark’s liability on any basis is limited to the price of the product used. The information in this bulletin supersedes all previously issued bulletins on the subject matter covered. VanDeMark Benzyl Chloroformate APPLICATIONS SPILLS AND DISPOSAL Benzyl Chloroformate is a reactive chemical intermediate Use personal protective equipment (see MSDS). used in the synthesis of pharmaceutical and agrochemical Evacuate personnel to safe areas. Dike far ahead of products. It is used as a reagent in peptide synthesis to liquid spill for later disposal. -
Synthesis, Utility and Medicinal Importance of 1,2- & 1,4
RSC Advances REVIEW View Article Online View Journal | View Issue Synthesis, utility and medicinal importance of 1,2- & 1,4-dihydropyridines Cite this: RSC Adv.,2017,7, 2682 Vivek K. Sharmaa and Sunil K. Singh*b Dihydropyridine (DHP) is among the most beneficial scaffolds that have revolutionised pharmaceutical research with unprecedented biological properties. Over the years, metamorphosis of easily accessible 1,2- and 1,4-dihydropyridine (1,4-DHP) intermediates by synthetic chemists has generated several drug molecules and natural products such as alkaloids. The 1,4-dihydropyridine (1,4-DHP) moiety itself is the main fulcrum of several approved drugs. The present review aims to collate the literature of 1,2- and the 1,4-DHPs relevant to synthetic and medicinal chemists. We will describe various Received 6th October 2016 methodologies that have been used for the synthesis of this class of compounds, including the Accepted 14th November 2016 strategies which can furnish enantiopure DHPs, either by asymmetric synthesis or by chiral resolution. DOI: 10.1039/c6ra24823c We will also elaborate the significance of DHPs towards the synthesis of natural products of medicinal www.rsc.org/advances merit. Creative Commons Attribution 3.0 Unported Licence. 1. Introduction oxidation–reduction reactions, has made the 1,4-DHP core even more lucrative. Perhaps less studied in the past, the potential of Arthur Hantzsch added one of the most valuable scaffolds to the 1,2-dihydropyridines has recently been explored as a critical toolbox of medicinal chemists, reporting the synthesis of scaffold for the synthesis of alkaloids and other drugs. 1,2-DHPs dihydropyridine (DHP) in 1882.