40566-85-6Relevant academic research and scientific papers
Continuous flow synthesis of arylhydrazines: via nickel/photoredox coupling of tert -butyl carbazate with aryl halides
Mata, Alejandro,Tran, Duc N.,Weigl, Ulrich,Williams, Jason D.,Kappe, C. Oliver
supporting information, p. 14621 - 14624 (2020/12/02)
Nickel/photoredox catalyzed C-N couplings of hydrazine-derived nucleophiles provide a powerful alternative to Pd-catalyzed methods. This continuous-flow photochemical protocol, optimized using design of experiments, achieves these couplings in short residence times, with high selectivity. A range of (hetero)aryl bromides and chlorides are compatible and understanding of process stability/reactor fouling has been discerned. This journal is
Diaza [1,4] Wittig-type rearrangement of N-allylic-N-Boc-hydrazines into γ-amino- N -Boc-enamines
Tayama, Eiji,Kobayashi, Yoshiaki,Toma, Yuka
supporting information, p. 10570 - 10573 (2016/09/02)
Diaza [1,4] Wittig-type rearrangement of N-allylic-N-Boc-hydrazines into γ-amino-N-Boc-enamines was demonstrated. The scope and limitation, experimental mechanistic studies, and a proposed reaction mechanism were also described.
BICYCLIC HETEROARYL INDOLE ANALOGUES USEFUL AS ROR GAMMA MODULATORS
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Page/Page column 39, (2015/06/25)
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X, X1, M, R2, R3, R4, R5, m, n, and p are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, neurodegenerative diseases and cancer.
PYRAZOLIDINEDIONE DERIVATIVES AND THEIR USE AS PLATELET AGGREGATION INHIBITORS
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Page 56, (2010/02/10)
Pyrazolidinedione derivatives of the general formula (I), wherein R1 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl; and R2 is aryl or heteroaryl; tautomers thereof; geometric is
Syntheses of 4-(5-oxo-1,2,4-triazol-3-yl)-sydnones and 4(4-arylamino-5-oxo-1,2,4-triazol-3-yl)-sydnones from sydnone derivatives and their fragments
Kuo,Lee,Yeh
, p. 227 - 240 (2007/10/03)
4-(5-oxo-1,2,4-triazol-3-yl)-sydnones 11 and 4-(4-arylamino-5-oxo-1,2,4-triazol-3-yl)-sydnones 13 have been obtained from a-chloroformylarylhydrazine hydrochloride 2. Moreover, the intermediates, including 3, 4, 9 and 10, in this study are synthetically informative and valuable. It is also noteworthy that three reactants, 1, 2 and sydnonecarbaldehydes, were prepared from sydnone derivatives and their fragments. The oxidative cyclizations of sydnonecarbaldehyde semicarbazones 9 and carbazpnes 10 with two different oxidizing agents (Cu(ClO4)2 and Fe(ClO4)3) have been extensively examined. The reaction time and the yields of cyclizations were affected by the substituents of semicarbazones 9 and carbazones 10.
A mild and efficient procedure for ring-opening reactions of piperidine and pyrrolidine derivatives by single electron transfer photooxidation
Cocquet, Guillaume,Ferroud, Clotilde,Guy, Alain
, p. 2975 - 2984 (2007/10/03)
Various N-arylamino-1-pyrrolidines and N-arylamino-1-piperidines are selectively converted into the corresponding acyclic aminoaldehydes or amino- dialkylacetals under mild photooxidation conditions. (C) 2000 Elsevier Science Ltd.
Indole-substituted five-membered heteroaromatic compounds as 5-HT1 agonists
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, (2008/06/13)
A class of indole-substituted five-membered heteroaromatic compounds are specific agonists of 5-HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a s
Synthesis and Serotonergic Activity of 5-(Oxadiazolyl)tryptamines: Potent Agonists for 5-HT1D Receptors
Street, Leslie J.,Baker, Raymond,Castro, Jose L.,Chambers, Mark S.,Guiblin, Alexander R.,et al.
, p. 1529 - 1538 (2007/10/02)
The synthesis and 5-HT1D receptor activity of a novel series of 5-(oxadiazolyl)tryptamines is described.Modifications of the oxadiazole 3-substituent, length of the linking chain (n), and the amine substituents are explored and reveal a large binding pocket in the 5-HT1D receptor domain.Oxadiazole substituents such as benzyl are accommodated without loss of agonist potency or efficacy.The incorporation of polar functionality on a phenyl or benzyl spacer group results in a 10-fold increase in affinity and functional potency.Optimal 5-HT1D activity is observed when the heterocycle is conjugated with the indole and the benzyl sulfonamides 20t and 20u represent some of the most potent 5-HT1D agonist known.Replacement of O for S in the heterocycle leads to a further increase in potency.Deletion of oxadiazole N-2 does not reduce activity, suggesting the requirements for only one H-bond acceptor in this location.The selectivity of these compounds for 5-HT1D receptors over other serotonergic receptors is discussed.Sulfonamide 20t shows 1000-fold selectivity for 5-HT1D over 5-HT2, 5-HT1C, and 5-HT3 receptors and 10-fold selectivity with respect to 5-HT1A receptors.The functional activity of this series of compounds is studied and demonstrates high 5-HT1D receptor potency and efficacy comparable to that of 5-HT.
Indole-substituted five-membered heteroaromatic compounds
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, (2008/06/13)
A class of indole-substituted five-membered heteroaromatic compounds are specific agonists of 5-HT1-like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a se
