347196-56-9Relevant academic research and scientific papers
Palladium-catalyzed amination of aryl chlorides and bromides with ammonium salts
Green, Rebecca A.,Hartwig, John F.
supporting information, p. 4388 - 4391 (2015/01/08)
We report the palladium-catalyzed coupling of aryl halides with ammonia and gaseous amines as their ammonium salts. The coupling of aryl chlorides and ortho-substituted aryl bromides with ammonium sulfate forms anilines with higher selectivity for the primary arylamine over the diarylamine than couplings with ammonia in dioxane. The resting state for the reactions of aryl chlorides is different from the resting state for the reactions of aryl bromides, and this change in resting states is proposed to account for a difference in selectivities for reactions of the two haloarenes.
Complementary asymmetric routes to (R)-2-(7-hydroxy-2,3-dihydro-1 H-pyrrolo[1,2-a]indol-1-yl)acetate
Schrader, Thomas O.,Johnson, Benjamin R.,Lopez, Luis,Kasem, Michelle,Gharbaoui, Tawfik,Sengupta, Dipanjan,Buzard, Daniel,Basmadjian, Christine,Jones, Robert M.
supporting information, p. 6306 - 6309 (2013/02/25)
Two distinct and scalable enantioselective approaches to the tricyclic indole (R)-2-(7-hydroxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetate, an important synthon for a preclinical S1P1 receptor agonist, are reported. Route 1 employs a modified version of Smith's modular 2-substituted indole synthesis as the key transformation. Route 2 involves a highly enantioselective CuH-catalyzed 1,4-hydrosilylation as the stereodefining step. Both routes can be performed without chromatography to provide multigram quantities of the tricycle in ≥98% ee.
Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV
Karle, Michael,Knecht, Wolfgang,Xue, Yafeng
supporting information; experimental part, p. 4839 - 4843 (2012/08/13)
In a project to find novel neutral P1 fragments for the synthesis of thrombin inhibitors with improved pharmacokinetic properties, fragments containing a benzothiazole guanidine scaffold were identified as weak thrombin inhibitors. WaterLOGSY (Water-Ligan
Positive allosteric modulators of the nicotinic acetylcholine receptor
-
Page 42, (2010/02/05)
The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which α7 nAChR is known to be involved.
