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Index -acylation 365 , -unsaturated esters -alkoxymethylenation 364–5 enantioselective synthesis 544 -alkylation formation and reactions of 591–6 of [14C]malonates 359–62 from alkoxycarbonyl[14C]methylenezinc of alkyl [14C]cyanoacetates 422 bromide 335–6 -amino acids, exchange labeling 58, 94–5 from alkyl 2-trimethylsilyl[14C]- -amino acids acetates 329 by enantioselective catalytic from [14C]malonates 265–7, 354, 357 tritiation 530–4 from trialkyl phosphono[14C]acetates 218, by enantioselective tritioreduction of 322–8, 544 oximes 540 , -unsaturated ketones, exchange from 2-acetamido-2-cyano[2-14C]- labeling 87 acetate 427 , -unsaturated oximes, exchange from [14C]glycines 316–7 labeling 87 from [2-14C]malonates 371–2 , -unsaturated ketones 542–4 -arylation absorption see ADME studies of [14C]malonates 362–4 [14C]acarbose, by biotransformation 623 of alkyl [14C]cyanoacetates 422 accelerator mass spectrometry (AMS) 1 [3H]- -conotoxin G1 95 [14C]acetaldehyde 290, 445–6 , -dehydrogenation/tritioreduction of [14C]acetamidines 377–8 carbonyls 483–5 2-acetamido[2-14C]acetate, from [14C]- , -unsaturated acids, exchange labeling 76 cyanoacetic acid 427 , -unsaturated acids see also , -unsaturated acetanilide derivatives, exchange labeling 80 esters [2H,3H]acetic acid (chiral) 617 from [14C]cyanohydrins 406–7 [14C]acetic acids from [14C]malonates by Knoevenagel [14C]acetic anhydride and mixed anhydrides reaction 365–7 from 298–301 , -unsaturated [14C]aldehydesCOPYRIGHTED 312 [14C]acetoacetates MATERIAL from 346–8 , -unsaturated amino acids [14C]acetyl halides from 289–90 N-acetyl, enantioselective reduction 532–4 chiral acetate 617 N-acetyl, preparation 530–2 esteriﬁcation 301–2 reconstitution strategies 530–4 formation of 269, 287–9, 446–7 , -unsaturated carbonyls 503–5 -halogenation of 308 , -unsaturated [14C]carboxamides 323, 327 in C-[14C]acetylations 291–6 Preparation of Compounds Labeled with Tritium and Carbon-14 Rolf Voges, J.

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Safety Data Sheet
SAFETY DATA SHEET Preparation Date: 07/06/2015 Revision Date: 12/28/2017 Revision Number: G2 1. IDENTIFICATION Product identifier Product code: C2322 Product Name: CYANOACETIC ACID Other means of identification Synonyms: Acide cyanacetique [French] Cyanessigsaeure [German] Kyselina kyanoctova [Czech] Malonic acid mononitrile Malonic mononitrile Monocyanoacetic acid Acetic acid, 2-cyano- Acetic acid, cyano- CAS #: 372-09-8 RTECS # AG3675000 CI#: Not available Recommended use of the chemical and restrictions on use Recommended use: Chemical intermediate for malonic acid; diethyl malonate for pharmaceuticals; For the production of the fungicide cymoxanil and the cough remedy dextromethorphan. 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) Acute toxicity - Oral Category 4 Skin corrosion/irritation Category 1 Serious eye damage/eye irritation Category 1 Specific target organ toxicity (single exposure) Category 3 Label elements Product code: C2322 Product name: CYANOACETIC ACID 1 / 12 Danger Hazard statements Causes severe
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Dissociation Constants of Organic Acids and Bases
DISSOCIATION CONSTANTS OF ORGANIC ACIDS AND BASES This table lists the dissociation (ionization) constants of over pKa + pKb = pKwater = 14.00 (at 25°C) 1070 organic acids, bases, and amphoteric compounds. All data apply to dilute aqueous solutions and are presented as values of Compounds are listed by molecular formula in Hill order. pKa, which is defined as the negative of the logarithm of the equi- librium constant K for the reaction a References HA H+ + A- 1. Perrin, D. D., Dissociation Constants of Organic Bases in Aqueous i.e., Solution, Butterworths, London, 1965; Supplement, 1972. 2. Serjeant, E. P., and Dempsey, B., Ionization Constants of Organic Acids + - Ka = [H ][A ]/[HA] in Aqueous Solution, Pergamon, Oxford, 1979. 3. Albert, A., “Ionization Constants of Heterocyclic Substances”, in where [H+], etc. represent the concentrations of the respective Katritzky, A. R., Ed., Physical Methods in Heterocyclic Chemistry, - species in mol/L. It follows that pKa = pH + log[HA] – log[A ], so Academic Press, New York, 1963. 4. Sober, H.A., Ed., CRC Handbook of Biochemistry, CRC Press, Boca that a solution with 50% dissociation has pH equal to the pKa of the acid. Raton, FL, 1968. 5. Perrin, D. D., Dempsey, B., and Serjeant, E. P., pK Prediction for Data for bases are presented as pK values for the conjugate acid, a a Organic Acids and Bases, Chapman and Hall, London, 1981. i.e., for the reaction 6. Albert, A., and Serjeant, E. P., The Determination of Ionization + + Constants, Third Edition, Chapman and Hall, London, 1984. BH H + B 7. Budavari, S., Ed., The Merck Index, Twelth Edition, Merck & Co., Whitehouse Station, NJ, 1996.
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Cyanoacetic Acid
Cyanoacetic Acid www.entrepreneurindia.co Introduction Cyanoacetic acid is an organic compound. It is a white, hygroscopic solid. The compound contains two functional groups, a nitrile and a carboxylic acid. It is a precursor to cyanoacrylates, components of adhesives. www.entrepreneurindia.co The largest scale reaction is its esterification to give ethyl cyanoacrylate. Cyanoacetic acid is a versatile intermediate in the preparation of chemicals. It is a precursor to synthetic caffeine via the intermediacy of theophylline. It is a building block for many drugs, including dextromethorphan, amiloride, sulfadimethoxine, and allopurinol. www.entrepreneurindia.co Synthesis of cyanoacetic acid by carbon dioxide and electrogenerated acetonitrile anion in undivided cells equipped with sacrificial anodes: The electrochemical synthesis of cyanoacetic acid was performed by cathodic reduction of tetra alkyl ammonium salts (R4NX) in acetonitrile in undivided cells equipped with sacrificial anodes with concomitant or subsequent addition of carbon dioxide. www.entrepreneurindia.co These syntheses avoid the use of dangerous reagents, yield cyanoacetic acid in moderate faradic yields and confirm that the cathodic reduction of tetra alkyl ammonium salts in the presence of acetonitrile leads to the formation of the anion CNCH2-. As a whole it is a good project for entrepreneurs to invest. www.entrepreneurindia.co Market Outlook Chemical industry is one of the oldest industries in India, which contributes significantly towards industrial and economic growth of the nation. Since this industry has numerous forward and backward linkages, it is called the backbone of the industrial and agricultural development of the country and provides building blocks for many downstream industries. www.entrepreneurindia.co The Chemical Industry of India ranks 6th in world and 3rd in Asia after Japan and China.
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United States Patent Office E
United States Patent Office E. ... 1 -2 Since in the method according to the invention no hy . METHOD. ' ' ' ' OF PREPARING3,773,808 CYANOACETIC. drogen cyanide is required, this method is appreciably '. ACID ESTERS safer and less expensive. Petrus Gerardus Johannes Wesselman, van Houtenlaan, Further it is of importance that after the removal Weesp, Netherlands, assignor to U.S. Philips Corpora of the solvent by evaporation, without further processing, tion, New York, N.Y. No Drawing. Filed Oct. 22, 1969, Ser. No. 868,606 - the product of the method can be marketed as technical Claims priority, application Netherlands, Oct. 26, 1968, grade cyanoacetic acid ester. .' - 6815349 Accordingly, the invention relates to a method of pre - - Int, C. C07c 121/06 paring cyanoacetic acid esters of the general formula U.S. C. 260-465.4 - - 8 Claims O NC-CHCOOR from halogen acetic acid esters of the general formula Hall-CHCOOR, where Hal is a chlo rine or bromine atom and R is an alkyl, alkenyl, cyclo ABSTRACT OF THE DISCLOSURE alkyl, aralkyl or aryl group, and sodium or potassium A method of preparing cyanoacetic acid esters by re cyanide, which method is characterized in that the reac acting halogenacetic acid esters with alkali cyanide in 15 tion is carried out in acetonitrile with an excess of the a reaction medium consisting of acetonitrile. cyanide. The use of sodium cyanide is to be preferred to the The invention relates to a method of preparing cyano use of potassium cyanide. acetic acid esters from halogenacetic acid esters and The cyanide may be used in an excess of up to 100%.
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Ethyl Cynoacetate.Pdf
Health 1 1 Fire 1 1 1 Reactivity 1 Personal E Protection Material Safety Data Sheet Ethyl cyanoacetate MSDS Section 1: Chemical Product and Company Identification Product Name: Ethyl cyanoacetate Contact Information: Catalog Codes: 10691 Finar Limited CAS#: 105-56-6 184-186/P, Chacharwadi Vasna, RTECS: AG4110000 Sarkhej-Bavla Highway, TSCA: Not available Ta.: Sanand, Dist.: Ahmedabad, Synonym: Cyanoacetic Acid Ethyl Ester Email: [email protected] Cyanoacetic Ester Web: www.finarchemicals.com Ethyl Cyanoethanoate Malonic Acid Ethyl Ester Nitrile Chemical Formula: C5H7NO2 Section 2: Composition and Information on Ingredients Composition: Name CAS #% Ethyl cyanoacetate 105-56-6 99% Section 3: Hazards Identification EMERGENCY OVERVIEW LACHRYMATOR IRRITANT Irritating to skin, eyes, and respiratory system. May have harmful effects if inhaled or swallowed. Avoid prolonged exposure. Do not breathe vapor. Potential Health Effects Skin contact may cause skin irritation with discomfort or rash. Skin absorption may occur in amounts capable of producing toxic effects. Eye contact may cause eye irritation with discomfort, tearing or blurring of vision. Inhalation may cause irritation of the nose and throat with sneezing, sore throat, runny nose, or shortness of breath. Other effects of exposure may include headache, nausea or vomiting. Section 4: First Aid Measures Eye Contact: Check for and remove any contact lenses. IMMEDIATELY flush eyes with running water for at least 15 minutes while keeping eyes open. COLD water may be used. Seek medical attention. Skin Contact: After contact with skin, wash with plenty of water. Gently and thoroughly wash the contaminated skin with running water and non-abrasive soap. COLD water may be used.
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Substituted Pyrazolopyrimidines and Imidazopyridazines As Angiotensin II Antagonists
fill ill lllllW @ EuroPean Patent Office ^-S Office europeen des brevets (fi) Publication number : 0 490 587 A1 @ EUROPEAN PATENT APPLICATION @ Application number : 91311361.9 @ Int. CI.5 : C07D 487/04, A61 K 31/50, A61 K 31/505, // @ Date of filing : 06.12.91 (C07D487/04, 239:00, 231:00), (C07D487/04, 237:00, 235:00) (30) Priority : 07.12.90 US 623880 Inventor : Maccoss, Malcolm 25.11.91 US 794533 48 Rose Court 25.11.91 US 794534 Freehold, NJ 07728 (US) Inventor : Chakravarty, Prasun K. (43) Date of publication of application : 16 Churchill Road 17.06.92 Bulletin 92/25 Edison, NJ 08820 (US) Inventor : Patchett, Arthur A. @) Designated Contracting States : 1090 Minisink Way CH DE FR GB IT LI NL Westfield, NJ 07090 (US) Inventor : Greenlee, William J. (n) Applicant : MERCK & CO. INC. 115 Herrick Avenue 126, East Lincoln Avenue P.O. Box 2000 Teaneck, NJ 07666 (US) Rahway New Jersey 07065-0900 (US) Inventor : Walsh, Thomas F. 127 Marion Avenue (g) Inventor : Allen, Eric E. Westfield, NJ 07090 (US) 10 Cedarbrook Drive Somerset, NJ 08873 (US) (74) Representative : Thompson, John Dr. et al Merck & Co., Inc. European Patent Department Terlings Park Eastwick Road Harlow, Essex CM20 2QR (GB) (54) Substituted pyrazolopyrimidines and imidazopyridazines as angiotensin II antagonists. (57) Novel substituted pyrazolopyrimidines and imidazopyridazines of formula (I), wherein A and B are N or C, butonly one of A or B is N angiotensin II antagonists, are disclosed. < X o o ci) LU Jouve, 18, rue Saint-Denis, 75001 PARIS EP 0 490 587 A1 INTRODUCTION OF THE INVENTION This invention relates to novel substituted pyrazolopyrimidine and imidazopyridazine compounds and deri- vatives thereof which are useful as angiotensin II antagonists in the treatment of elevated blood pressure, in 5 the treatment of congestive heart failure, and in the treatment of elevated intraocular pressure.
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(12) United States Patent (10) Patent No.: US 9,206,198 B2 Ding Et Al
USOO9206198B2 (12) United States Patent (10) Patent No.: US 9,206,198 B2 Ding et al. (45) Date of Patent: Dec. 8, 2015 (54) INHIBITORS OF THE RENAL OUTER (56) References Cited MEDULLARY POTASSIUM CHANNEL U.S. PATENT DOCUMENTS Applicant: Merck Sharp & Dohme Corp., (71) 2.988,551 A 6, 1961 Morren Rahway, NJ (US) 3.435,002 A 3, 1969 Holub 3,632,608 A 1, 1972 Holub (72) Inventors: Fa-Xiang Ding, Staten Island, NY (US); 3,749,722 A 7, 1973 Holub Shuzhi Dong, Plainsboro, NJ (US); 4,579,863. A 4, 1986 Horwell et al. Jessica Frie, Harleysville, PA (US); Xin 4,806,536 A 2f1989 Cross et al. 4,992,547 A 2f1991 Berner et al. Gu, Scotch Plains, NJ (US); Jinlong 5,145,885 A 9, 1992 Berner et al. Jiang, Scotch Plains, NJ (US); 5,215,989 A 6/1993 Baldwin et al. Alexander Pasternak, Princeton, NJ 5,614,526 A 3, 1997 Godel et al. (US); Haifeng Tang, Metuchen, NJ 5,736,546 A 4, 1998 Kawashima et al. (US); Zhicai Wu, Montvale, NJ (US); (Continued) Yang Yu, Edison, NJ (US); Takao Suzuki, Pudong Shanghai (CN) FOREIGN PATENT DOCUMENTS (73) Assignee: Merck Sharp & Dohme Corp., EP O099.148 B1 2/1988 Rahway, NJ (US) EP O175376 B1 4f1991 (Continued) (*) Notice: Subject to any disclaimer, the term of this OTHER PUBLICATIONS patent is extended or adjusted under 35 U.S.C. 154(b) by 0 days. Felix; Assay and Drug Development Technologies, 2012, 10, 417 431.* Doggrell; Cardiovascular Research, 1998, 39, 89-105.* (21) Appl.
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To USP 39–NF 34, First Supplement the Following Index Is For
Index to USP 39–NF 34, First Supplement The following Index is for convenience and informational use only and shall not be used for interpretive purposes. In addition to official articles, this Index may also include items recently omitted from the USP–NF in the indicated Book or Supplement. The requirements stated in the General Notices and Requirements section of the USP–NF apply to all articles recognized in the USP–NF and to all general chapters unless specifically stated otherwise. Although this revision (USP 39–NF 34 1S) is generally official beginning August 1, 2016; particular provisions may indicate another earlier or later official date. In addition, the monographs and general chapters listed in this Index may reference other general chapter specifications. The articles listed in this Index are not intended to be autonomous standards and should only be interpreted in the context of the entire USP–NF publication. For the most current version of the USP–NF please see the USP–NF Online Combined Index to USP 39 and NF 34 Abaca-Acety I-1 Combined Index to USP 39 and NF 34, including First Supplement Page citations refer to the pages of Volumes 1, 2, 3, and 4 of USP 39±NF 34 and its First Supplement. This index is repeated in its entirety in each volume. 1±2280 Volume 1 2281±4454 Volume 2 4455±6446 Volume 3 6447±7608 Volume 4 7609±8194 First Supplement Numbers in angle brackets such as 〈421〉 refer to chapter numbers in the General Chapters section. and (salts of) chlorpheniramine, and tramadol hydrochloride oral A dextromethorphan,
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Cyanoacetamide Derivatives As Synthons in Heterocyclic Synthesis
Turk J Chem 32 (2008) , 259 – 286. c TUB¨ ITAK˙ Review Cyanoacetamide Derivatives as Synthons in Heterocyclic Synthesis Ahmed Ali FADDA, Samir BONDOCK∗,RamyRABIE, Hassan Ali ETMAN Department of Chemistry, Faculty of Science, Mansoura University, ET-35516 Mansoura-EGYPT e-mail: [email protected] Received 09.10.2007 This review presents a systematic and comprehensive survey of the methods of preparation and the chemical reactivity of cyanoacetamide derivatives. These compounds are important intermediates for the synthesis of a variety of otherwise diﬃcult to obtain synthetically useful and novel heterocyclic systems. Key Words: Cyanoacetanilide, thiophene, pyrazole, thiazole, pyridine, pyridazine, pyrimidine, hetero- cycles Introduction Cyanoacetamides are highly reactive compounds. They are extensively utilized as reactants or reaction intermediates since the carbonyl and the cyano functions of these compounds are suitably situated to enable reactions with common bidentate reagents to form a variety of heterocyclic compounds. Moreover, the active hydrogen on C-2 of these compounds can take part in a variety of condensation and substitution reactions. In addition, the diverse biological activities reported for many derivatives of cyanoacetamide have also drawn the attention of biochemists in the last decade. The literature covering the chemistry of cyanoacetamide derivatives has been limited. However, a review of the chemistry and reactions of cyanothioacetamide (in Russian) was published in 1999.1 The main objective of the present survey is to provide a comprehensive account of the synthetic utility of N-aryl and/or heteryl cyanoacetamides in building various organic heterocycles and to highlight their potential in evolving better chemotherapeutic agents. Synthesis The synthesis of cyanoacetamides may be carried out in several ways.
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Tetrahedron Laboratofies Private Limited MANUFACTURERS of API
Tetrahedron Laboratofies Private Limited MANUFACTURERS OF API. INTERMEDIATE ANo.i'LlIEO PRODUCTS .. Telefax: +91-22-25342435 Registered Office: ~ Email: [email protected] 201-A, Harmony. Netaji Subhash Chandra Bos9 Road, ' Thane (W), 400601. Maharashtra. India. Website: www.tetrahedronJabs.com Date: 23.06.2018 To, The Member Secretary (IndU3Uy 11), Ministry of Environment, Forests and Climate Change, Indh'a PL,.,-aVAran BhawaD, Jor Bagh Roat'lt New De1hi~11000s Refwence: MOM Of 37th Expert Appraisal Committee [lndustry-z] Meeting held on so- May 2018. Subject: Submission of MoM Compliance for Environmental Clearance for proposed "'ManuJacturi:ng of Bulk f)rugs, Intermediates &. AlHf!d Products" at Plot No. F-2~, Mfnc Chind-uii1, 'if4h1kR:Mono1, nlt;trlct: SotApUf, Maharashtra. India by MIs.. Tetmhedro!l Lahomtoriea Pvt. Ltd.. Dear Sir, This is with reference to the above subject and reference, We, Mis. Tetrahedron Laboratories Pvt. Ltd., are proposing for flMonufa.cturing of Bulk Drugs, Intermediates &. A11iedProducts" at Plot No. F 25, M11)C Chincho1i, 1'iJ1ulm:Mohol, nistrict: Solupur. Maharashtra, India. and submitted EIAReport online on dated 13.01.2018. In this connection, MoRF &. ce, New DeJhi hRd con kkred our case in 37th :IT.pe.. rt Appraisal Committee (lndustry-z] meeting on 30/05/2018 stating that ~The EACj after ddibe ticn~, ob:~ discre ei potiDJly l"esl'em of the di«~nt uuburtrUd l'~!G uti l.1'1~tlMd.Dut; to th.at, it Wg not possible to UDdGl'Stand the po11UtJoB COBcema aDd/or the impact or the project 011 different &avirontneatal puametera. The- Comm!~ also desired for-presence of the EtA ~tor for taUon of the pl'(J~".
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To USP 39–NF 34, Second Supplement the Following Index Is
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Acid Dissociation Constants
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