65739-64-2Relevant academic research and scientific papers
Investigations of possible prodrug structures for 2-(2-mercaptophenyl)tetrahydropyrimidines: Reductive conversion from anti-HIV agents with pyrimidobenzothiazine and isothiazolopyrimidine scaffolds
Okazaki, Shiho,Oishi, Shinya,Mizuhara, Tsukasa,Shimura, Kazuya,Murayama, Hiroto,Ohno, Hiroaki,Matsuoka, Masao,Fujii, Nobutaka
, p. 4706 - 4713 (2015/04/27)
3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182) and 3,4-dihydro-2H-benzo[4,5]isothiazolo[2,3-a]pyrimidine are the heterocyclic antiretroviral agents against human immunodeficiency virus type 1 (HIV-1) infection. On the basis of simi
Four-electron oxidative dehydrogenation induced by proton-coupled electron transfer in ruthenium(III) complex with 2-(1,4,5,6-tetrahydropyrimidin-2-yl) phenolate
Mitsuhashi, Ryoji,Suzuki, Takayoshi,Sunatsuki, Yukinari
, p. 10183 - 10190 (2013/09/23)
New ruthenium(II or III) complexes with general formula [Ru(O-N)(bpy) 2]n+ (O-N = unsymmetrical bidentate phenolate ligand; bpy = 2,2'-bipyridine) were synthesized, and their crystal structures and electrochemical properties were cha
Concise synthesis and anti-HIV activity of pyrimido[1,2-c][1,3] benzothiazin-6-imines and related tricyclic heterocycles
Mizuhara, Tsukasa,Oishi, Shinya,Ohno, Hiroaki,Shimura, Kazuya,Matsuoka, Masao,Fujii, Nobutaka
supporting information; experimental part, p. 6792 - 6802 (2012/09/22)
3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182) is a virucidal heterocyclic compound active against various viruses, including HCV, HIV, and simian immunodeficiency virus. Using facile synthetic approaches that we developed for the synthesis of pyrimido[1,2-c][1,3]benzothiazin-6-imines and related tricyclic derivatives, the parallel structural optimizations of the central 1,3-thiazin-2-imine core, the benzene part, and the cyclic amidine part of PD 404182 were investigated. Replacement of the 6-6-6 pyrimido[1,2-c][1,3] benzothiazin-6-imine framework with 5-6-6 or 6-6-5 derivatives led to a significant loss of anti-HIV activity, and introduction of a hydrophobic group at the 9- or 10-positions improved the potency. In addition, we demonstrated that the PD 404182 derivative exerts anti-HIV effects at an early stage of viral infection.
Geometric selectivity, hydrogen-bonding interaction, and solvatochromism of Bis{N-(aminoalkyl)salicylamidato(2-)}cobaltate(III)
Mitsuhashi, Ryoji,Suzuki, Takayoshi,Sunatsuki, Yukinari,Kojima, Masaaki
body text, p. 696 - 698 (2011/08/08)
Cobalt(III) complexes with N-(aminoalkyl)salicylamide dianions, Ln 2- (n = 14), have been prepared and their molecular and crystal structures have been determined. The geometric (mer- or fac-) selectivity of [Co(Ln)2]- com
Cu(ii)-mediated oxidative intermolecular ortho C-H functionalisation using tetrahydropyrimidine as the directing group
Mizuhara, Tsukasa,Inuki, Shinsuke,Oishi, Shinya,Fujii, Nobutaka,Ohno, Hiroaki
supporting information; experimental part, p. 3413 - 3415 (2009/12/26)
Tetrahydropyrimidine works efficiently as a directing group in Cu(ii)-mediated oxidative aromatic C-H functionalisation for the selective introduction of oxygen or nitrogen to the ortho-position.
Reactions of 2-Hydroxybenzonitrile with Isocyanates
Petridou-Fischer, J.,Papadopoulos, E. P.
, p. 1159 - 1167 (2007/10/02)
Triethylamine catalyzes the reaction of 2-hydroxybenzonitrile (1) with arylisocyanates to form the corresponding carbamates 2a-c, as well as the cyclization of the latter compounds to either 4--3-aryl-2H-1,3-benzoxazin-2-ones 4a-c, or 4-arylamino-2H-1,3-benzoxazin-2-ones 7a-c, depending on the reaction temperature.Under analogous conditions, the carbamates obtained from 1 and 2-chloroethyl isocyanate, 3-chloropropyl isocyanate and ethyl isocyanatoacetate undergo a double cyclization yielding imidazo- and pyrimidobenzoxazinones 13a, b, 17.Upon heating in phenyl ether, compounds 7a-c, rearrange to 2-(2-hydroxyphenyl)-4(3H)-quinazolinones 10a-c.
