Cyanide is rapidly alsorbed through oral, inhalation, and dermal routes and distributed throughout the body. Cyanide is mainly metabolized into thiocyanate by either rhodanese or 3-mercaptopyruvate sulfur transferase. Cyanide metabolites are excreted in the urine. (L96)
IDENTIFICATION AND USE: Phenyl isocyanate is a liquid with an acrid odor. It decomposes in water, alcohol; very soluble in ether. It is used as a chemical intermediate and as a reagent. HUMAN EXPOSURE AND TOXICITY: Workers exposed to phenyl isocyanate showed increases in asthmatic symptoms. Exposure to isocyanates is irritating to the skin, mucous membranes, eyes and respiratory tract. Contact dermatitis can result in symptoms such as rash, itching, hives and swelling of the extremities. Phenyl isocyanate is a potent chemical sensitizer. A worker suspected of having isocyanate induced asthma/sensitization will exhibit traditional symptoms of acute airway obstruction coughing, wheezing, shortness of breath, tightness of chest and nocturnal awakening. Isocyanate induced hypersensitivity pneumonitis symptoms are flu like which includes shortness of breath, nonproductive cough, fever, chills sweats and malaise and nausea. An irreversible decline in pulmonary function and interstitial fibrosis have also been observed. At high doses isocyanates affect the mucous membranes of the respiratory tract and may lead to fatal pulmonary edema or chromic catarrh. ANIMAL STUDIES: The toxic effects of repeated inhalation exposures to phenyl isocyanate vapors in male rats was conducted. Animals experienced decreased weight gain, hypoactivity, hypothermia, and signs of respiratory tract irritation. There was delayed onset of mortality, and changes in organ weights. Pulmonary function tests demonstrated decreased forced expiratory flow volume. Arterial hypoxia was also observed. Pregnant mice were given phenyl isocyanate on select days of gestation. Phenyl isocyanate did demonstrate embryotoxicity. In a micronucleus assay, male and female mice received a single administration of phenyl isocyanate ip; there was an altered ratio between polychromatic and normochromatic erythrocytes in the bone marrow, and no clastogenic effect was observed. Phenyl isocyanate did not cause significant induction of chromosomal aberrations in the bone marrow of male mice.
Cyanide is an inhibitor of cytochrome c oxidase in the fourth complex of the electron transport chain (found in the membrane of the mitochondria of eukaryotic cells). It complexes with the ferric iron atom in this enzyme. The binding of cyanide to this cytochrome prevents transport of electrons from cytochrome c oxidase to oxygen. As a result, the electron transport chain is disrupted and the cell can no longer aerobically produce ATP for energy. Tissues that mainly depend on aerobic respiration, such as the central nervous system and the heart, are particularly affected. Cyanide is also known produce some of its toxic effects by binding to catalase, glutathione peroxidase, methemoglobin, hydroxocobalamin, phosphatase, tyrosinase, ascorbic acid oxidase, xanthine oxidase, succinic dehydrogenase, and Cu/Zn superoxide dismutase. Cyanide binds to the ferric ion of methemoglobin to form inactive cyanmethemoglobin. (L97)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
致癌物分类
对人类无致癌性（未列入国际癌症研究机构IARC清单）。
No indication of carcinogenicity to humans (not listed by IARC).
Exposure to high levels of cyanide for a short time harms the brain and heart and can even cause coma, seizures, apnea, cardiac arrest and death. Chronic inhalation of cyanide causes breathing difficulties, chest pain, vomiting, blood changes, headaches, and enlargement of the thyroid gland. Skin contact with cyanide salts can irritate and produce sores. (L96, L97)
来源:Toxin and Toxin Target Database (T3DB)
毒理性
暴露途径
该物质可以通过吸入和摄入被身体吸收。
The substance can be absorbed into the body by inhalation and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
1-Propanephosphonic Acid Cyclic Anhydride (T3P) as an Efficient Promoter for the Lossen Rearrangement: Application to the Synthesis of Urea and Carbamate Derivatives
The synthesis of hydroxamic acids starting from carboxylic acids employing 1-propanephosphonic acid cyclic anhydride (T3P) activation is described. Application of ultrasonication accelerates this conversion. Further, the T3P has also been employed to activate the hydroxamates, leading to isocyanates via the Lossenrearrangement. The isocyanates were trapped with suitable nucleophiles to afford the
[EN] COMPOUNDS FOR THE TREATMENT OF AMYLOID-ASSOCIATED DISEASES<br/>[FR] COMPOSÉS POUR LE TRAITEMENT DE MALADIES ASSOCIÉES À LA SUBSTANCE AMYLOÏDE
申请人：REMYND NV
公开号：WO2016083490A1
公开（公告）日：2016-06-02
This invention provides novel compounds of formulae (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein the substituents are as defined in the specification. The present invention also relates to the novel compounds for use as a medicine, more in particular for the prevention or treatment of amyloid-related diseases, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such amyloid-related diseases. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
For the purpose to examine as to their antiviral activities, 2-acylaminoacetamidine (II) and 3-acylaminopropionamidine hydrochlorides (III) were synthesized from the corresponding nitriles via ethyl imidates. The difference of the reactivity between ethyl 2-acylaminoacetimidates and ethyl 3-acylaminopropionimidates on the course of amidination were postulated. Iminoesterification of dinitrile, (p-cyano) benzamidopropionitrile (XVIII), was discussed by referring the infrared spectrum of a corresponding monocyanomonoester, ethyl p-(N-cyanoethylcarbamoyl) benzoate (XXI). Among the compounds obtained hereof, 3-(p-methyl) benzamidopropionamidine hydrochloride was found to have an inhibitory effect on influenza virus in mice and in membrane culture.
Synthesis of Thiocarbamates from Thiols and Isocyanates Under Catalyst- and Solvent-Free Conditions
作者：Barahman Movassagh、Mohammad Soleiman-Beigi
DOI：10.1007/s00706-007-0762-7
日期：2008.2
A simple and efficient procedure was developed for the synthesis of S -alkyl (aryl) thiocarbamates under solvent-free conditions without the use of a catalyst. The significant features of this protocol are (a) operational simplicity, (b) mild reaction conditions, (c) short reaction times, (d) solvent-free conditions, and (e) high product yields.
Nucleophilic Substitution Reactions of Aryl <i>N</i>-Phenyl Thiocarbamates with Benzylamines in Acetonitrile
作者：Hyuck Keun Oh、Jie Eun Park、Dae Dong Sung、Ikchoon Lee
DOI：10.1021/jo049845+
日期：2004.4.1
reactions of esters. This large rate increase and the similar change in the aminolysis rates that are reported to occur from aryl ethyl carbonate (EtOC(O)OC6H4Z; 2a) to aryl ethylthiocarbonate (EtOC(O)SC6H4Z; 2b) lead us to conclude that the aminolysis of 3b proceeds by a concerted mechanism in contrast to a stepwiseprocess for 3a. The negative ρXZ values (−0.63) and violation of the reactivity−selectivity
研究了芳基N-苯硫代氨基甲酸酯（PhNHC（O）SC 6 H 4 Z; 3b）与苄胺（XC 6 H 4 CH 2 NH 2）在乙腈中的氨解反应。速率比芳基N-苯基氨基甲酸酯（PhNHC（O）OC 6 H 4 Z; 3a）的相应反应快得多。速率从3a增加到3b大于在酯的逐步氨解反应中用噻吩氧化物取代苯酚离去基团所期望的值。据报道，从碳酸芳基乙酯（EtOC（O）OC 6 H 4 Z; 2a）到硫代碳酸芳基乙酯（EtOC（O）SC 6 H 4 Z; 2b）发生的速率大幅度提高，氨解率也发生了类似的变化。导致我们得出结论，与3a的逐步过程相反，3b的氨解是通过协同机制进行的。负ρ XZ值（-0.63）和违反反应性选择性原则（RSP）都支持所提出的机制。大β X所获得的值（1.3-1.5）被认为是表示在过渡状态，这是与比较大的动力学同位素效应是一致的（在很大程度上键制作ķ ħ / ķ d观察到> 1
