MONOMETHYLACETAMIDE IS A METABOLITE OF DIMETHYLACETAMIDE & APPEARS IN MEASURABLE AMOUNTS IN URINE AFTER SINGLE EXPOSURE TO A TLV (THRESHOLD LIMIT VALUE) DOSE OF DIMETHYLACETAMIDE.
In a recent comparative toxicity & metab study of 4 formamides & on N-methylacetamide, the sole metabolite of N-methylacetamide in the urine of mice was identified as N-(hydroxymethyl)acetamide. There was no evidence of induction of hepatic drug metabolizing enzymes in rats following treatment with N-methylacetamide. N-Methylacetamide influenced neither the sleeping time induced by hexobarbital nor the metabolism of hexobarbital or aniline.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
副作用
职业性肝毒素 - 第二性肝毒素：在职业环境中的毒性效应潜力是基于人类摄入或动物实验的中毒病例。
Occupational hepatotoxin - Secondary hepatotoxins: the potential for toxic effect in the occupational setting is based on cases of poisoning by human ingestion or animal experimentation.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
SIMULTANEOUS TREATMENT OF PREGNANT RATS WITH SODIUM NITRITE IN DRINKING WATER & N-METHYLACETAMIDE PRODUCED GREATER TERATOGENIC EFFECTS THAN TREATMENT WITH N-METHYLACETAMIDE ALONE. THUS, ENDOGENOUS NITRATION OF CMPD MAY BE TERATOGENIC FACTOR.
Basic treatment: Establish a patent airway. Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with normal saline 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 ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poison A and B/
Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in respiratory arrest. Positive pressure ventilation techniques with a bag valve mask device may be beneficial. Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start an IV with D5W /SRP: "To keep open", minimal flow rate/. Use lactated Ringer's if signs of hypovolemia are present. Watch for signs of fluid overload. Consider drug therapy for pulmonary edema ... . For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poison A and B/
/Liver toxicity was assessed in/ workers /exposed/ to N,N-dimethylacetamide (DMAC) in an acrylic fiber manufacturing facility. /Measurements were made/ over a 1 yr study period. ... Evidence of liver toxicity was assessed by serum clinical chemistry tests (serum levels of total bilirubin, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, & gamma-glutamyl transpeptidase) at least once during the study period for all 127 male workers in the two study departments & for 217 male in plant controls with no previous or current exposure to DMAC. If a worker's biomonitoring results exceeded one of two trigger values established for the study (60 mg N-methylacetamide/g creatinine or 136 mg DMAC equivalent/g creatinine), addnl serum clinical chemistry tests were conducted at weekly intervals for 3 wk. DMAC exposed workers were classified as either high exposure, if 1 or more biomonitoring result exceeded one of the trigger values, or unspecified exposure if none of them did. Control group employees were classified as no exposure. Mean DMAC in air levels for the high & unspecified exposure groups appeared to differ (geometric mean DMAC in air levels of 1.9 & 1.3 ppm 12 hr time weighted avg, respectively). No significant DMAC exposure related trends in hepatic serum clinical chemistry results were detected. Neither transient incr in serum analyte levels after a high biomonitoring result (one that exceeded a trigger value) nor an elevated mean level over the study period when compared with in plant controls were observed. These results /indicate/ that brief threshold limit value level exposures & chronic low level exposure (maximum likelihood estimate of the arithmetic mean for DMAC in air for the high exposure group over the study period was 3.0 ppm 12 hr time weighted avg) do not cause hepatotoxic clinical chemistry responses. /N,N-dimethylacetamide/
The determination of urinary N-monomethylacetamide (MMAC) in the end of shift urine sample was used to /evaluate/ worker exposure to dimethylacetamide (DMAC). Five workers were observed and followed for 4 consecutive weeks. Airborne DMAC appeared to account for the greatest amount of urinary MMAC detected, and at the exposure concn encountered ().5 to 2 ppm), a relationship of 10 ppm urinary MMAC for each 1 ppm DMAC inhaled was observed. ... It was concluded that changes in DMAC exposures can be quantitatively reflected by urinary MMAC.
A Heteroleptic Dirhodium Catalyst for Asymmetric Cyclopropanation with α‐Stannyl α‐Diazoacetate. “Stereoretentive” Stille Coupling with Formation of Chiral Quarternary Carbon Centers
作者：Fabio P. Caló、Alois Fürstner
DOI：10.1002/anie.202004377
日期：2020.8.10
The heteroleptic dirhodium paddlewheel catalyst 7 with a chiral carboxylate/acetamidate ligand sphere is uniquely effective in asymmetric [2+1] cycloadditions with α‐diazo‐α‐trimethylstannyl (silyl, germyl) acetate. Originally discovered as a trace impurity in a sample of the homoleptic parent complex [Rh2((R )‐TPCP)4] (5 ), it is shown that the protic acetamidate ligand is quintessential for rendering
Thiourea-Catalyzed Asymmetric Michael Addition of Activated Methylene Compounds to α,β-Unsaturated Imides: Dual Activation of Imide by Intra- and Intermolecular Hydrogen Bonding
A thiourea-catalyzed asymmetricMichaeladdition of activated methylene compounds to α,β-unsaturated imides derived from 2-pyrrolidinone and 2-methoxybenzamide has been developed. In the case of 2-pyrrolidinone derivatives, the reaction with malononitrile proceeded in toluene with high enantioselectivity, providing the Michael adducts in good yields. However, the nucleophiles that could be used for
已开发出硫脲催化的活化亚甲基化合物与衍生自 2-吡咯烷酮和 2-甲氧基苯甲酰胺的 α,β-不饱和酰亚胺的不对称迈克尔加成反应。在 2-吡咯烷酮衍生物的情况下，与丙二腈的反应在甲苯中以高对映选择性进行，以良好的收率提供迈克尔加合物。然而，由于底物的反应性差，可用于该反应的亲核试剂仅限于丙二腈。进一步的研究表明，在芳环上带有不同取代基的相应苯甲酰胺衍生物中，N-链烯酰基-2-甲氧基苯甲酰胺是最好的底物。事实上，几种活化的亚甲基化合物如丙二腈、α-氰基乙酸甲酯、硝基甲烷可用作亲核试剂，以良好至极好的收率获得高达 93% ee 的迈克尔加合物。光谱实验的结果表明，这种增强的反应性可归因于分子内氢...
Broad spectrum antibiotics
申请人：Pfizer Inc.
公开号：US04025506A1
公开（公告）日：1977-05-24
6-[.alpha.-(Amidino- and imidoylaminoalkanoylamino)aracylamino]-penicillanic acids and synthetic methods for the preparation thereof.
6-α-(酰胺基和亚胺基氨基烷酰氨基)阿拉伯氨基-青霉素酸及其制备的合成方法。
A Simple Protocol for Efficient N-Chlorination of Amides and Carbamates
作者：Giampaolo Giacomelli、Lidia De Luca、Giammario Nieddu
DOI：10.1055/s-2004-836061
日期：——
N-Chlorination of various amides, lactams, and carbamates with very cheap trichloroisocyanuric acid proceeds efficiently under very mild conditions. Excellent results were also observed for the N-chlorination of carbamates of free amino acids.
Selective N-Nitrosation of Amines,<i>N</i>-Alkylamides and<i>N</i>-Alkylureasby N<sub>2</sub>O<sub>4</sub>Supported on Cross-Linked Polyvinylpyrrolidone(PVP-N<sub>2</sub>O<sub>4</sub>)
N2O4 was supported on the cross-linked polyvinylpyrrolidone (PVP) to afford a solid, stable and recyclable nitrosating agent. This reagent shows excellent selectivity for N-nitrosation of dialkyl amines in the presence of diaryl-, arylalkyl-, trialkylamines and also for secondary amides in dichloromethane at room temperature under mild and heterogeneous conditions. Also N-nitroso-N-alkyl amides can be selectively prepared in the presence of primary amides and N-phenylamides under similar reaction conditions. Selective N-nitrosation or dealkylation and N-nitrosation of tertiary amines can also be performed by this reagent.
