- TETRAZOLONE SUBSTITUTED STEROIDS AND USE THEREOF
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The present disclosure relates to compounds of formula (AI), (I), (AII), and (II), or a pharmaceutically acceptable salt, solvate, stereoisomer, or tautomer thereof, a pharmaceutical composition comprising a compound of formula (AI), (I), (AII), and (II), and use thereof, wherein R2, R3, R4, R5, R6, R7, R10, R11a, R11b, R12, R16, R19a, R19b, and R20 are described herein. Such compounds are envisioned useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, movement disorders, convulsive disorders, schizophrenin spectrum disorders, disorders of memory and/or cognition, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, or tinnitus etc.
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Paragraph 500-502; 520-522
(2020/07/31)
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- A facile route for the synthesis 1,4-disubstituted tetrazolone derivatives and evaluation of their antimicrobial activity
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A facile route for the synthesis of 20 new 1,4-disubstituted tetrazolone derivatives from allyl bromides of Baylis-Hillman adducts and various 1-substituted tetrazolones is described. All the synthesized compounds were screened for in vitro antibacterial
- Santhoshi, Amlipur,Sadhu, Partha Sarathi,Sriram, Rekulapally,Sai Pavan Kumar, Chebolu Naga Sesha,Mahendar, Budde,Sarangapani, Manda,Rao, Vaidya Jayathirtha
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p. 3329 - 3340
(2013/07/19)
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- Electronic properties of 1-methyl-4-phenyl-1H-tetrazole-5(4H)-thiones: An experimental and theoretical study
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The syntheses of 1-(4-methoxyphenyl)-4-methyl-1H-tetrazol-5(4H)-thione 1a, 1-methyl-4-phenyl-1H-tetrazole-5(4H)-thione 1b, 1-(4-chlorophenyl)-4-methyl-1H-tetrazol-5(4H)-thione 1c, 1-methyl-4-(4-nitrophenyl)-1H-tetrazol-5(4H)-thione 1d were carried out and their electronic absorption spectra were obtained in cyclohexane, THF, and acetonitrile. The UV spectra of 1a-d showed a modest dependence on the polarity of the solvent. The change of substituent on the tetrazolethione ring from a strongly electron donating group (p-C6H4OMe, 1a), to a moderately electron donating (C6H5, 1b) to a weakly electron withdrawing group (p-C6H4Cl, 1c) also produced minimal effect on the electronic properties of 1a-c. However, the presence of a strongly electron withdrawing group (p-C6H4NO2, 1d) on the heterocyclic ring produced a marked change in the UV spectrum. Time-dependent density functional calculations revealed that all the bands result from π → π* excitations with some degree of intramolecular charge transfer (ICT) within the molecules. Our studies further showed that as the acceptor strength is increased in the order: 1a (p-C6H4OMe) 6H5) 6H4Cl) 6H4NO2), the ICT also increases. In accordance with the experimental observations, the calculated transitions also showed modest dependence on the polarity of the solvent.
- Rayat, Sundeep,Chhabra, Radhika,Alawode, Olajide,Gundugola, Aditya S.
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experimental part
p. 38 - 45
(2010/02/16)
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- Process for the preparation of 1-4-disubstituted-5 (4H)-tetrazolinones
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1,4-Disubstituted-5(4H)-tetrazolinones of the formula (I) STR1 wherein R1, R2 and R3 have the meanings given in the specification), which are known to be useful as herbicides, can be obtained in very good yields by reacting the corresponding 1-substituted-5(4H)-tetrazolinones with the corresponding carbamoyl chlorides in the presence of 4-dimethylaminopyridine.
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- Process for the preparation of 1-substituted-5(4H)-tetrazolinones
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A process for the preparation of a 1-substituted-5(4H)-tetrazolinone of the formula STR1 wherein R1 is defined in the specification n is 0, 1, 2, 3 or 4, which comprises reacting a 1-substituted-5(4H)-tetrazolinethione of the formula STR2 with an ethylene oxide of the formula STR3 wherein R2 represents hydrogen, methyl or ethyl, in the presence of a base and in the presence of water, an alcohol or a mixture thereof.
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- Reactions of Trimethylsilyl Azide with Heterocumulenes
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Trimethylsilyl azide (TMSA) reacted with aryl isocyanates to give arylcarbamoyl azides, 1-aryl-5(4H)-tetrazolinones, and / or 1-aryl-4-(arylcarbamoyl)-5(4H)-tetrazolinones, whose yields were dependent on the reaction conditions.The reaction between TMSA and benzoyl or thiobenzoyl isocyanates provides a facile method for the preparation of 5-aryl-3-hydroxy-1,2,4-oxadiazoles or -1,2,4-thiadiazoles, respectively.However, with phenyl or benzoyl isothiocyanate, 1-anilino-1,2,3,4-thiatriazole or benzoylcyanamide was obtained in low yield, respectively.TMSA reacted with carbodiimides to afford the corresponding 5-aminotetrazoles.Tetraphenylsuccinimide, N-(diphenylacetyl)tetraphenylsuccinimide, 1,3-bis(diphenylmethyl)urea, and / or benziloylamide were obtained from the reaction of TMSA with diphenyl ketene.The pathways for the formation of the above products are also described.
- Tsuge, Otohiko,Urano, Satoshi,Oe, Koji
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p. 5130 - 5136
(2007/10/02)
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