374590-17-7Relevant articles and documents
Heteroatom-directed alkylcyanation of alkynes
Nakao, Yoshiaki,Yada, Akira,Hiyama, Tamejiro
supporting information; experimental part, p. 10024 - 10026 (2010/10/04)
Alkanenitriles having a heteroatom such as nitrogen, oxygen, and sulfur at the γ-position are found to add across alkynes stereo-and regioselectively by nickel/Lewis acid catalysis to give highly substituted acrylonitriles. The heteroatom functionalities likely coordinate to the nickel center to make oxidative addition of the C-CN bonds of the alkyl cyanides kinetically favorable, forming a five-membered nickelacycle intermediate and, thus, preventing β-hydride elimination to allow the alkylcyanation reaction.
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane
Shah, Shrenik K.,Chen, Natalie,Guthikonda, Ravindra N.,Mills, Sander G.,Malkowitz, Lorraine,Springer, Martin S.,Gould, Sandra L.,DeMartino, Julie A.,Carella, Anthony,Carver, Gwen,Holmes, Karen,Schleif, William A.,Danzeisen, Renee,Hazuda, Daria,Kessler, Joseph,Lineberger, Janet,Miller, Michael,Emini, Emilio A.,MacCoss, Malcolm
, p. 977 - 982 (2007/10/03)
Synthesis of analogs containing more rigid bicyclic piperidine replacements for the 4-benzyloxycarbonyl-(ethyl)amino-piperidine moiety of the CCR5 antagonist structure, 1, is described. Although similar binding affinity to the lead was achieved with some analogs they were overall less potent anti-HIV agents suggesting that other features besides CCR5 binding are required for good anti-viral activity.
Carboxy substituted acylic carboxamide derivatives
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, (2008/06/13)
The present invention relates to novel carboxy substituted acyclic carboxamide derivatives of formula (1)): STR1and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.
Synthetic studies towards the octahydro-1H-benzo[f]pyrrolo[3,2,1-ij]quinolines: Enantioselective synthesis of (2R,3S)-2-[(1S)-3-(benzyloxy)-1-(tert-butyldimethyl-silyloxymethyl) propyl]-3-phenylhexahydropyridine
Zaponakis, George S,Katerinopoulos, Haralambos E
, p. 6393 - 6396 (2007/10/03)
(2R,3S)-2-[(1S)-3-(Benzyloxy)-1-(tert-butyldimethylsilyloxymethyl)propyl]-3- phenylhexahydropyridine - a key synthetic intermediate for the preparation of (6aS,11bS,11cS)-1H-benzo[f]pyrrolo[3,2,1-ij]quinoline - was synthesized in nine steps. The synthetic approach uses both enantiomers of the chiral auxiliary trans-2,5-bis(methoxymethoxymethyl)pyrrolidine, employed in different stages of the synthesis for the construction of two out of the three stereogenic centers in the above mentioned intermediate.
SUBSTITUTED N-METHYL-N-(4-(4-(1H-BENZIMIDAZOL-2-YL) {1,4}DIAZEPAN-1-YL)-2-(ARYL)BUTYL) BENZAMIDES USEFUL FOR THE TREATMENT OF ALLERGIC DISEASES
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, (2008/06/13)
The present invention relates to novel N-methyl-N-(4-(4-(1H-benzimidazol-2-yl)[1,4]diazepan-1-yl)-2-(aryl)butyl)benzamide derivatives of the formula: STR1 stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.