154233-38-2Relevant academic research and scientific papers
Hydrogen bond directed aerobic oxidation of amines via photoredox catalysis
Wang, Hongyu,Man, Yunquan,Wang, Kaiye,Wan, Xiuyan,Tong, Lili,Li, Na,Tang, Bo
, p. 10989 - 10992 (2018/10/08)
An application of H-bonding interactions for directing the α-C-H oxidation of amines to amides and amino-ketones catalyzed by an organic photocatalyst is reported. The high efficiency of this method is demonstrated by the aerobic oxidation of pyrrolidines, diarylamines and benzylamines bearing urea groups with high yields and a wide substrate scope.
N-(Alkylsulfamoyl)aldimines: Easily deprotected precursors for diarylmethylamine synthesis
Crampton, Rosemary H.,Fox, Martin,Woodward, Simon
, p. 599 - 605 (2013/06/27)
The sequential reaction of chlorosulfonyl isocyanate with t-BuOH, t-BuNH2 and TFA allows formation of H2NSO 2NHBut. Condensation of the latter with Ar1CHO in the presence of Ti(OEt)4 provides the activated imines Ar 1CHNSO2NHBut (59-89%). Commercially available boronic acids add to these imines with good stereoselectivity (76-98% ee) using readily available diene ligands. Simple deprotection with 5% w/w water in pyridine affords free Ar1CHNH2Ar2.
THERAPEUTIC METHODS
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Page/Page column 45; 46, (2013/06/27)
The present invention relates to methods of treatment of diseases mediated by ROR?.
Rapid, one-pot synthesis of α,α-disubstituted primary amines by the addition of Grignard reagents to nitriles under microwave heating conditions
Gregg, Brian T.,Golden, Kathryn C.,Quinn, John F.,Wang, Hong-Jun,Zhang, Wei,Wang, Ruifang,Wekesa, Francis,Tymoshenko, Dmytro O.
experimental part, p. 3978 - 3981 (2009/10/04)
A series of α,α-disubstituted amines have been prepared in a simple and efficient one-pot procedure by the addition of Grignard reagents to a series of aliphatic, aromatic, and heteroaromatic nitriles. Key to this reported procedure is the unprecedented addition of the Grignard reagent to the nitrile under heating by microwave irradiation which both significantly improves reaction yields and reduces reaction times. In general, the Grignard addition reaction is complete within 5-10 min at 100 °C followed by rapid reduction with sodium borohydride to give the target amines.
α-Methylation at benzylic fragment of N-aryl-N′-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model
Gomtsyan, Arthur,Bayburt, Erol K.,Keddy, Ryan,Turner, Sean C.,Jinkerson, Tammie K.,Didomenico, Stanley,Perner, Richard J.,Koenig, John R.,Drizin, Irene,McDonald, Heath A.,Surowy, Carol S.,Honore, Prisca,Mikusa, Joe,Marsh, Kennan C.,Wetter, Jill M.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 3894 - 3899 (2008/02/09)
SAR studies for N-aryl-N′-benzyl urea class of TRPV1 antagonists have been extended to cover α-benzyl alkylation. Alkylated compounds showed weaker in vitro potencies in blocking capsaicin activation of TRPV1 receptor, but possessed improved pharmacokinetic properties. Further structural manipulations that included replacement of isoquinoline core with indazole and isolation of single enantiomer led to TRPV1 antagonists like (R)-16a with superior pharmacokinetic properties and greater potency in animal model of inflammatory pain.
Substituted benzhydryl lactamimide derivatives
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, (2008/06/13)
Novel compounds useful as diuretic agents and anticoagulants are represented by the following formula SPC1 Wherein m is a positive whole integer of from 1 to 3; n is a positive whole integer of from 3 to 7; R and R1 may be the same or different
