1229000-68-3Relevant academic research and scientific papers
Reagent-Controlled Divergent Synthesis of 2-Amino-1,3-Benzoxazines and 2-Amino-1,3-Benzothiazines
Putta, V. P. Rama Kishore,Vodnala, Nagaraju,Gujjarappa, Raghuram,Tyagi, Ujjawal,Garg, Aakriti,Gupta, Sreya,Pujar, Prasad Pralhad,Malakar, Chandi C.
, p. 380 - 396 (2020)
A reagent-controlled chemoselective process has been devised for the synthesis of 4H-1,3-benzoxazines and related biologically important heterocycles in high yields under mild conditions. These scaffolds could be efficiently constructed using two different chemoselective reactions that rely on the choice of reagents and reaction conditions. The treatment of various 2-amino-arylalkyl alcohols with isothiocyanates afforded thiourea intermediates, which were reacted in situ with molecular iodine in the presence of triethylamine to give 2-amino-4H-1,3-benzoxazines, whereas the corresponding 2-amino-4H-1,3-benzothiazines were obtained by the reaction of thiourea intermediates in the presence of T3P (a mild cyclodehydrating agent) and triethylamine as the base. The described protocol represents the first example for the synthesis of 4H-1,3-benzoxazines via the dehydrosulfurization method using molecular iodine as the reagent.
P(III)-Mediated Cascade C-N/C-S Bond Formation: A Protocol towards the Synthesis of N,S-Heterocycles and Spiro Compounds
Polina, Saibabu,Putta, V. P. Rama Kishore,Gujjarappa, Raghuram,Singh, Virender,Pujar, Prasad Pralhad,Malakar, Chandi C.
, p. 431 - 445 (2020/12/07)
A P(III)-mediated entry towards construction of C?N/C?S bond has been devised. The developed heterocyclization method was exercised for the synthesis of a diverse range of N,S-heterocycles and related spiro molecules. P(NMe2)3 revealed the maximum efficacies under the aerobic reaction conditions and a spectrum of bis-nucleophiles, and isothiocyanates were tolerated well to serve the access of manifold immense molecules. (Figure presented.).
OPIOID RECEPTOR MODULATORS AND USE THEREOF
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Paragraph 0050; 0222; 0223; 0235; 0236; 0237, (2017/03/21)
Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method
Structural requirement(s) of N-phenylthioureas and benzaldehyde thiosemicarbazones as inhibitors of melanogenesis in melanoma B 16 cells
Thanigaimalai,Le Hoang, Tuan Anh,Lee, Ki-Cheul,Bang, Seong-Cheol,Sharma, Vinay K.,Yun, Cheong-Yong,Roh, Eunmiri,Hwang, Bang-Yeon,Kim, Youngsoo,Jung, Sang-Hun
supporting information; experimental part, p. 2991 - 2993 (2010/08/06)
In order to define the structural requirements of phenylthiourea (PTU), a series of thiourea and thiosemicarbazone analogs were prepared and evaluated as inhibitors of melanogenesis in melanoma B16 cells. The most potent analog was 2-(4-tert-butylbenzylidene)hydrazinecarbothioamide (1u) with an IC50 value of 2.7 μM in inhibition of melanogenesis. The structure for potent inhibitory activity of these derivatives are required with the direct connection of π-planar structure to thiourea without steric hinderance in PTU derivatives and the hydrophobic substituent at para position in case of semicarbazones.
