1,2-dihydro-2,2,4-trimethylquinoline appears as dark cloudy copper-colored or yellow liquid. Odorless. (NTP, 1992)
颜色/状态：
LIGHT TAN POWDER
闪点：
214 °F (NTP, 1992)
分解：
DISASTER HAZARD: SEE QUINOLINE. DANGEROUS; WHEN HEATED TO DECOMPOSITION IT EMITS TOXIC FUMES OF /NITROGEN OXIDES/. /QUINOLINE/
计算性质
辛醇/水分配系数(LogP)：
2.8
重原子数：
13
可旋转键数：
0
环数：
2.0
sp3杂化的碳原子比例：
0.333
拓扑面积：
12
氢给体数：
1
氢受体数：
1
ADMET
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案例。
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
LONG-TERM INTRAGASTRIC ADMINISTRATION OF 1,2-DIHYDRO-2,2,4-TRIMETHYLQUINOLINE TO RATS DECREASED BODY WEIGHT, DEPRESSED THE NERVOUS SYSTEM, AND DISRUPTED LIVER FUNCTION. IT ALSO DECREASED THE AMOUNT OF HEMOGLOBIN & THE NUMBER OF ERYTHROCYTES IN THE BLOOD.
1,2-Dihydro-2,2,4-trimethylquinoline (DTQ) was evaluated for mutagenicity in the Salmonella/microsome preincubation assay using a standard protocol approved by the National Toxicology Program. DTQ was tested at doses of 0, 1, 3.3, 10, 33, 100, and 220 ug/plate in four Salmonella typhimurium strains (TA98, TA100, TA1535, and TA1537) in the presence and absence of Aroclor-induced rat or hamster liver S9. DTQ was negative in these tests and the highest ineffective dose level tested in all four Salmonella tester strains without slight or total clearing of the background lawn was 33 ug/plate.
... CONCLUSIONS: Under the conditions of these 2 yr dermal studies, there was some evidence of carcinogenic activity of 1,2-dihydro-2,2,4-trimethylquinoline in male F344/N rats, based on increased incidences of renal tubule adenoma and adenoma or carcinoma (combined). There was no evidence of carcinogenic activity of 1,2-dihydro-2,2,4-trimethylquinoline in female F344/N rats receiving 36, 60, or 100 mg/kg, or in male or female B6C3Fl mice receiving 3.6, 6, or 10 mg/kg.
Novel Heteroarotinoids as Potential Antagonists of Mycobacteriumbovis BCG
摘要：
A series of 15 heteroarotinoids has been prepared and evaluated for activity against Mycobacterium bovis BCG with the thiourea-containing isoxyl (7) (0.5 mug/mL) as the standard. 2,2,4-Trimethyl-2H-chromen-7-yl 4-(methoxycarbonyl)benzoate (8) displayed the most significant activity (2.0-4.0 mug/mL) in terms of the lowest concentration (mug/mL) (MIC, minimum inhibitory concentration) required to produce a 99% reduction in the number of colonies on a plate as compared to that system free of the agent at the same dilution of the culture suspension. Ethyl 4-{[N-(2,2,4,4-tetramethylchroman-6-yl)thiocarbamoyl] amino}benzoate (9) and {[(1E,3Z,5E)-1-aza-4-methyl-6-(1,2,2,4-tetramethyl(1,2-dihydroquinolyl))hexa-1,3,5-trienyl]-amino}aminomethane-1-thione (10) exhibited activity at 5.0-10.0 and 10.0-20.0 mug/mL, respectively, while the other examples had MIC values of 20 mug/mL or greater. The inhibitory ability of 8 may occur via the inhibition of mycolic acid synthesis in a like manner as found with 7, but this requires further study. The heteroarotinoids are the first examples to exhibit inhibitory ability against the growth of Mycobacterium bovis BCB.
Compounds of the formula (II) ##STR1## or a salt, N-oxide or acyl derivative thereof, wherein Y is a group ##STR2## which is optionaly substituted and which optionally contain a nitrogen atom at one of positions A, B, C, D or E, in which the dotted line represents aromatic rings unless one of the rings contains a nitrogen atom in which case this ring is either aromatic or partially saturated, have antimicrobial properties. Processes for making these compounds, pharmaceutical compositions containing them and the medical use of the compounds are also disclosed.
1,3-dipolar compound bearing an imidazole functional group
申请人：COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN
公开号：US10202471B2
公开（公告）日：2019-02-12
In a 1,3-dipolar compound of formula Q-A-B, Q comprises a dipole containing at least and preferably one nitrogen atom, A, which is preferably divalent, is an atom or a group of atoms connecting Q to B, and B comprises an imidazole ring. An unsaturated polymer modified by grafting the 1,3-dipolar compound is also disclosed.
[EN] INTRACELLULAR RECEPTOR MODULATOR COMPOUNDS AND METHODS<br/>[FR] COMPOSÉS MODULATEURS DE RÉCEPTEURS INTRACELLULAIRES ET PROCÉDÉS DE PRODUCTION ET D'UTILISATION DE CEUX-CI
申请人：LIGAND PHARM INC
公开号：WO2006019716A1
公开（公告）日：2006-02-23
This invention relates to compounds of Formula I, II or III with the definitions of R1-R10 according to claim 1 that bind to intracellular receptors and/or modulate activity of intracellular receptors, and to methods for making and using such compounds.
[EN] PROCESS FOR PREPARING (R)-4-AMINOINDANE AND CORRESPONDING AMIDES<br/>[FR] PROCÉDÉ DE PRÉPARATION DE (R)-4-AMINOINDANE ET D'AMIDES CORRESPONDANTS
申请人：ISAGRO SPA
公开号：WO2021059146A1
公开（公告）日：2021-04-01
The present invention relates to a process for preparing 1,1,3 -trimethylindan-4-amine of formula (I), or a salt thereof, enriched in one of its two enantiomers, in particular the enantiomer (R), (I) which comprises the chiral separation of an optionally substituted 2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline of formula (III). The present invention also relates to a process for preparing optically active amides of formula (II), (II) starting from said compounds of formula (I).
[EN] PROCESS FOR THE PREPARATION OF 4-AMINOINDANE DERIVATIVES AND RELATED AMINOINDANE AMIDES<br/>[FR] PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS DE 4-AMINOINDANE ET D'AMIDES D'AMINOINDANE ASSOCIÉS
申请人：STICHTING I-F PRODUCT COLLABORATION
公开号：WO2017178868A1
公开（公告）日：2017-10-19
The present invention relates to a process for the preparation of 4-aminoindane derivatives of Formula (I) (I). The present invention also relates to a process for the preparation of aminoindane amides of Formula (II), having fungicidal activity, starting from a 4- aminoindane derivative intermediate of Formula (I) obtained through the above-mentioned process. (II).
