96326-44-2Relevant academic research and scientific papers
Development of the route of manufacture of an oral H1-H 3 antagonist
Harling, Sandra J.,Herbal, Karim,Langlade, Nathalie,Sanganee, Mahesh,Strachan, John B.,Turner, Peter G.,Whiting, Matthew P.,Bret, Guillaume,Loft, Mike,Negus, Alan,Shanahan, Steve
experimental part, p. 112 - 122 (2011/10/13)
A new route to an H1-H3 antagonist was developed to address scalability and environmental and cost of goods issues associated with the initial route.
3- (4-{ [4-(4-{ [3-(3, 3-DIMETHYL-1-PIPERIDINYL) PROPYL] 0XY} PHENYL) -1-PIPERIDINYL] CARBONYL }-1-NAPHTHALENYL) PROPANOIC OR PROPENOIC ACID AS H1 AND H3 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY AND/OR ALLERGIC DISORDERS
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Page/Page column 37; 40, (2008/06/13)
The present invention relates to a compound of formula (I), or a salt thereof wherein the naphthalene ring can be substituted in the 2, 3, 4, 5, 6, 7 or 8 position by R1, and R1 represents -CH2CH2COOH or -CH=C(CH3)COOH, and to processes for their preparation, to compositions containing them and to their use in the treatment of various diseases such as allergic rhinitis.
Chemoselective hydrogenation of imides catalyzed by Cp*Ru(PN) complexes and its application to the asymmetric synthesis of paroxetine
Ito, Masato,Sakaguchi, Ayaka,Kobayashi, Chika,Ikariya, Takao
, p. 290 - 291 (2008/04/18)
This work represents the first catalytic hydrogenation of imides into amides and primary alcohols, in which the unique chemoselectivity is originated from the bifunctional nature of ruthenium-NH moiety in the catalyst. Copyright
A multireceptorial binding reinvestigation on an extended class of σ ligands: N-[ω-(indan-1-yl and tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine reveal high affinities towards σ1 and EBP sites
Berardi, Francesco,Ferorelli, Savina,Colabufo, Nicola Antonio,Leopoldo, Marcello,Perrone, Roberto,Tortorella, Vincenzo
, p. 1325 - 1335 (2007/10/03)
New 1-[ω-(2,3-dihydro-1H-inden-1-yl)- and (2,3-dihydro-5-methoxy-1H-inden-1-yl)alkyl]- and 1-[ω-(1,2,3,4-tetrahydronaphthalen-1-yl)- and (6-methoxy- or 6-fluoro-1,2,3,4-tetrahydronaphthalen-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine were synthesized, as homologous compounds of an existing series of σ ligands, in order to carry out σ receptor subtypes structure-affinity relationships. The new compounds and some of their related analogues, already reported, were tested in new multireceptorial radioligand binding assays. As reference compounds, the known σ1 ligands SA 4503, BD 1008 and NE 100 were also prepared and tested. All reported compounds showed high σ1 affinity assayed by (+)-[3H]-pentazocine on guinea-pig brain (apparent Ki=1.75-72.2 nM) and moderate or low σ2 affinity by [3H]-DTG on rat liver, in contrast with previous results. One tertiary amine function spaced by a five-membered chain from a phenyl group is the structural feature shared by the most active compounds 26 and 43 and some reference σ1 ligands. The reported σ1 ligands, including reference compounds, also demonstrated a high affinity towards EBP (Δ8-Δ7 sterol isomerase) site (apparent Ki=0.48-14.8 nM) and some of them (37 and 44) were good ligands at L-type Ca++ channel. 1-[4-(2,3-Dihydro-1H-inden-1-yl)butyl]-3,3-dimethylpiperidine (26) was the best mixed σ1 and EBP ligand (apparent Ki=1.75 and 1.54 nM, respectively) with a good selectivity versus σ2 receptor (138- and 157-fold, respectively).
Asymmetric synthesis catalyzed by chiral ferrocenylphosphine transition metal complexes. 10 gold(I)-catalyzed asymmetric aldol reaction of isocyanoacetate
Hayashi, Tamio,Sawamura, Masaya,Ito, Yoshihiko
, p. 1999 - 2012 (2007/10/02)
Optically active ferrocenylbisphosphine ligands containing 2-(dialkylamino)ethylamino group on the ferrocenylmethyl position have been prepared and used for the gold(I)-catalyzed asymmetric aldol reaction of isocyanoacetate with aldehydes. Six-membered ring amines, such as morpholino or piperidino group, at the terminal of the side chain were most stereoselective to give optically active trans-4- methoxycarbonyl-5-alkyl-2-oxazolines (up to 97% ee) with high enantio- and diastereoselectivity in a quantitative yield.
