Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand-valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR as necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Ketones and related compounds/
Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if necessary. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . For contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool. Administer activated charcoal ... . /Ketones and related compounds/
Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias if necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Ketones and related compounds/
/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Groups of 10 male and 10 female Sprague-Dawley rats were administered 1,1-dichloro-2-propanone in corn oil by gavage at 0, 10, 20, 40, or 80 mg/kg/day for 90 consecutive days. Food and water consumption, body and organ weights, organ-to-body weight ratios, hematology, and clinical chemistry parameters were determined. Gross and microscopic pathology examinations also were conducted. No treatment-related mortality was observed during the study; however, liver, forestomach, and kidney toxicity was evident. Liver changes consisted of cytoplasmic alteration, cytomegaly, karyomegaly, and bile duct hyperplasia. These occurred with significance of p < or = 0.05 at or above 10 mg/kg/day in both sexes. The forestomach lesions included hyperkeratosis and epithelial hyperplasia in both sexes at 40 and 80 mg/kg/day, and ulcerations at 80 mg/kg/day. Also, an increased incidence and severity of spontaneously occurring chronic progressive nephropathy was most apparent in high dose males. Increases in organ-to-body weight ratios were noted for the liver and kidneys in females at the highest dose level and in males at the two highest dose levels. Serum enzymes (ALT, AST, and LDH) were increased in females and decreased in males. Based on liver lesions and biochemical changes, it was concluded that there was no experimentally definable NOAEL.
/LABORATORY ANIMALS: Chronic Exposure or Carcinogenicity/ Several chlorinated acetones have been identified in drinking water and these, as well as a number of chlorinated acroleins, are produced by chlorination of humic acid solutions. Many of these chlorinated compounds and the brominated acrolein analog were positive in the Ames Assay in the laboratory. To determine if carcinogenic activity was associated with these chemicals the following acetone derivatives: monochloro (MCA); 1,1-dichloro (1,1-DCA), 1,3-dichloro (1,3-DCA), 1,1,1-trichloro (1,1,1-TCA), 1,1,3-trichloro (1,1,3-TCA), and substituted acroleins: 2-chloro (CAC), 3,3-dichloro (DCAC), 2,3,3-trichloro (TCAC) and 2-bromo (BAC), were applied topically to SENCAR mice (25, 30, or 40/group) at the following dose levels: 50 mg/kg (MCA and 1,1,3-TCA); 50, 75 and 100 mg/kg (1,3-DCA); 100, 200 and 400 mg/kg (CAC, DCAC, and TCAC); 200 and 300 mg/kg (BAC); and 400, 600, and 800 mg/kg (1,1-DCA, and 1,1,1-TCA). Doses were applied six times over a 2-week period in 0.2 mL ethanol per application. 1,3-DCA was also tested with single doses of 37.5, 75, 150 and 300 mg/kg in 0.2 mL ethanol. Control animals received 0.2 mL ethanol per application as a single dose or multiple doses to match corresponding studies. Two weeks after the final dose, 1.0 ug TPA in 0.2 mL acetone was applied three times weekly for 20 weeks. After 24 weeks the percentage of animals with tumors for dose groups above were: MCA (8); 1,1,3-TCA (10); 1,3-DCA, multiple doses (48, 45, 32); CAC (30, 28, 38); DCAC (3, 0, 0); TCAC (10, 5, 0); BAC (54, 43); 1,1-DCA (0, 5, 0); 1,1,1-TCA (10, 5, 0); 1,3-DCA, single doses (47, 47, 63, 20); controls (12 ... , 9 ... average). These data show that 1,3-DCA, CAC and BAC, when applied topically, initiate tumors in the mouse skin. These chemicals administered orally in a 2% emulphor solution ... did not initiate tumors in the mouse skin. /Chlorinated acetones and acroleins/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
...在沐浴过程中，通过收集和分析六名受试者在30分钟沐浴期间和之后呼出的气体样本的时间变化，研究了两种卤代酮（1,1-二氯丙酮和1,1,1-三氯丙酮）和氯仿的皮肤吸收情况。在沐浴过程中，呼出气体中的消毒副产物浓度逐渐增加至最大浓度。在皮肤接触期间，卤代酮的最大呼气浓度范围为0.1至0.9微克/立方米，大约比氯仿在接触期间的最大呼气浓度低两个数量级。基于单室模型，氯仿、1,1-二氯丙酮和1,1,1-三氯丙酮的体内渗透率分别近似为0.015、7.5 x 10^-4和4.5 x 10^-4厘米/小时。因此，在正常沐浴条件下，卤代酮的皮肤渗透性远低于氯仿...
... Dermal absorption of two haloketones (1,1-dichloropropanone and 1,1,1-trichloropropanone) and chloroform while bathing, /were examined/ by collecting and analyzing time profiles of expired breath samples of six human subjects during and following a 30-min bath. The disinfection byproduct concentrations in breath increased towards a maximum concentration during bathing. The maximum haloketone breath concentration during dermal exposure ranged from 0.1 to 0.9 ug /cu m, which was approximately two orders of magnitude lower than the maximum chloroform breath concentration during exposure. Based on a one-compartment model, the in vivo permeability of chloroform, 1,1-dichloropropanone, and 1,1,1-trichloropropanone were approximated to be 0.015, 7.5 x 10- 4, and 4.5 x 10- 4 cm /hr, respectively. Thus, haloketones are much less permeable across human skin under normal bathing conditions than is chloroform...
One pot three-component regioselective and diastereoselective synthesis of halogenated pyrido[2,1-b][1,3]oxazines
作者：Sakineh Asghari、Ahmad Khabbazi Habibi
DOI：10.1016/j.tet.2012.08.038
日期：2012.10
of 3-substituted pyridines, dimethyl acetylenedicarboxylate (DMAD), and α-halo ketones led to regioselective and stereoselective synthesis of pyrido[2,1-b][1,3]oxazines in high to excellent yields under mild conditions. All the reactions gave the pyrido[2,1-b][1,3]oxazine derivatives without formation of any indolizine products.
3-取代的吡啶，乙炔二甲酸二甲酯（DMAD）和α-卤代酮的三组分反应导致在温和条件下以高产率至优异产率进行吡啶并[2,1- b ] [1,3]恶嗪的区域选择性和立体选择性合成。所有反应得到吡啶并[2，1- b ] [1，3]恶嗪衍生物，而没有形成任何吲哚嗪产物。
Reactivity of Various α-Halo Ketones in One-Pot Synthesis of γ-Iminolactones
作者：Sakineh Asghari、Ahmad Khabbazi Habibi
DOI：10.1080/00397911.2011.571806
日期：2012.10
Abstract The highly reactive 1:1 intermediate generated in the reaction of tert-butyl isocyanide and dialkyl acetylenedicarboxylate is trapped by α-haloketones to produce halogenated iminolactones as the sole product in good yields. GRAPHICAL ABSTRACT
A kinetic and mechanistic study of the gas-phase reactions of OH radicals and Cl atoms with some halogenated acetones and their atmospheric implications
作者：Sin�ad Carr、Dudley E. Shallcross、Carlos E. Canosa-Mas、John C. Wenger、Howard W. Sidebottom、Jack J. Treacy、Richard P. Wayne
DOI：10.1039/b304298g
日期：——
Rate coefficients for the reactions of hydroxyl radicals and chlorine atoms with a series of halogenated acetones of the type CX3COCH3 (X = H, Cl, F) have been determined using a photolytic relative-rate technique at T = 298 K and at 760 Torr total pressure. The reactions studied and the rate coefficients obtained are shown in the table. ReactionReaction number Rate coefficient/cm3 molecule−1 s−1
The present invention relates to difluoromethyl-phenyl triazoles of general formula (I) which are modulators of GABA
A
receptors containing the α5 subunit, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
本发明涉及一般式（I）的二氟甲基苯基三唑化合物，这些化合物是包含α5亚基的GABA A 受体的调节剂，用于治疗中枢神经系统疾病和其他疾病。此外，本发明涉及制备药物组合物的方法，以及根据本发明制造化合物的方法。
Kinetics and mechanistic investigation into the degradation of naproxen by a UV/chlorine process
combined with chlorine (UV/chlorine) was used to degrade naproxen (NPX), a typical non-steroidal anti-inflammatory drug (NSAID) widely used for the treatment of symptoms associated with inflammation, in water. Compared with UV irradiation alone and direct chlorination, the UV/chlorine process shows a synergistic effect on NPX degradation. The effects of different factors, including the chlorine dose, solution
