31250-99-4Relevant academic research and scientific papers
Method for synthesizing 1 - methyl - 1H -1, 2 and 4 - triazol -3 - methyl formate
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Paragraph 0026-0028, (2021/11/26)
The invention discloses a synthetic 1 - methyl - 1H -1. The invention discloses a method for 2,4 - triazole -3 - methyl formate and belongs to the technical field of organic synthesis. The reaction of 1,2 and 4 - triazole as a raw material is followed by
TRICYCLIC COMPOUNDS AS INHIBITORS OF IMMUNOSUPPRESSION MEDIATED BY TRYPTOPHAN METABOLIZATION
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Paragraph 0185, (2014/10/15)
Presently provided are inhibitors of IDO and TDO and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase and tryptophan 2,3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
Synthesis, SAR and selectivity of 2-acyl- and 2-cyano-1-hetarylalkyl- guanidines at the four histamine receptor subtypes: A bioisosteric approach
Geyer, Roland,Igel, Patrick,Kaske, Melanie,Elz, Sigurd,Buschauer, Armin
supporting information, p. 72 - 81 (2014/01/06)
In the search for potential bioisosteres of the 4-imidazolyl ring in acylguanidines (e.g. UR-AK24), known to possess affinity to several histamine receptor subtypes (HxR, x = 1-4), and cyanoguanidine-type H 4R agonists (e.g. UR-PI376
Design, synthesis, and antifungal activity of triazole and benzotriazole derivatives
Rezaei, Zahra,Khabnadideh, Soghra,Pakshir, Keyvan,Hossaini, Zahra,Amiri, Fatemeh,Assadpour, Elham
experimental part, p. 3064 - 3067 (2009/10/02)
This study describes the design, synthesis and evaluation of a novel series of 1,2,4-triazole and benzotriazole derivatives as inhibitors of cytochrome P450 14α-demethylase (14DM). The chemical structures of the new compounds were confirmed by elemental a
Aromatic heterocycle compounds having HIV integrase inhibiting activities
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, (2008/06/13)
A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORAwherein RAis hydrogen or ester residue, —CONRBRCwherein RBand RCeach is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.
INTEGRASE INHIBITORS CONTAINING AROMATIC HETEROCYCLE DERIVATIVES
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, (2008/06/13)
A compound of the formula (I): whereinX is hydroxy or the like;Y is -C(=R2)-R3-R4 wherein R2 and R3 is oxygen atom or the like, R4 is hydrogen, optionally substituted alkyl, optionally subs
An investigation into the alkylation of 1,2,4-triazole
Bulger, Paul G.,Cottrell, Ian F.,Cowden, Cameron J.,Davies, Antony J.,Dolling, Ulf-H.
, p. 1297 - 1301 (2007/10/03)
The alkylation of 1,2,4-triazole with 4-nitrobenzyl halides and a variety of bases afforded the 1- and 4-alkylated isomers with a consistent regioselectivity of 90:10. Previously reported regiospecific alkylations of 1,2,4-triazole were re-examined and the quoted isomer ratios were shown to depend on the isolation procedure. The use of DBU as base in the alkylation of 1,2,4-triazole allows for a convenient and high yielding synthesis of 1- substituted-1,2,4-triazoles. (C) 2000 Elsevier Science Ltd.
Synthesis of novel cyclobutylphosphonic acids as inhibitors of imidazole glycerol phosphate dehydratase
Norcross, Roger D.,Von Matt, Peter,Kolb, Hartmuth C.,Bellus, Daniel
, p. 10289 - 10312 (2007/10/03)
Diethyl 3-oxocyclobutylphosphonate (5) has been synthesised via a novel one-pot cyclisation reaction of the α-phenylsulphonyl-γ,δ-epoxyphosphonate 8. Addition of 5-lithio-1-trityl-1,2,4-triazole to ketone 5 and deprotection then afforded cis-3-hydroxy-3-(1,2,4-triazol-3-yl])cyclobutylphosphonic acid (cis-4) which showed modest in vitro inhibition of the enzyme imidazole glycerol phosphate dehydratase. In an attempt to obtain the corresponding trans isomer (trans-4), whose inhibitory activity was anticipated to he higher, an efficient three-step synthesis was developed employing base-mediated cyclisation of the γ,δ-epoxy-γ-(1,2,4-triazol-5-yl)phosphonate 35. Although this latter route stereoselectively afforded cis-36, an efficient epimerisation reaction could be subsequently used to obtain the desired trans stereochemistry. However, all attempts at deprotection of trans-36 proceeded with simultaneous re-epimerisation to give the previously prepared cis-4. High level ab initio calculations have been used to rationalise the relative thermodynamic stability of cis-4 and trans-4.
Triazole phosphoric acid derivatives and their use as herbicides
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, (2008/06/13)
A herbicidal compound of formula (I) STR1 or a salt, tautomer or cyclic derivative thereof; where R1 and R2 are hydrogen and A is an optionally substituted saturated or unsaturated chain or ring of three carbon atoms. Methods for pre
An improved method for the N-alkylation of benzotriazole and 1,2,4-triazole
Katritzky, Alan R.,Kuzmierkiewiecz, Wojciech,Greenhill, John V.
, p. 369 - 373 (2007/10/02)
The N-alkylation of benzotriazole and 1,2,4-triazole with alkyl halides proceeds efficiently in the presence of sodium hydroxide in N,N-dimethylformamide.
