24464-41-3Relevant academic research and scientific papers
Ruthenium-catalyzed chemo-and enantioselective hydrogenation of isoquinoline carbocycles
Jin, Yushu,Makida, Yusuke,Uchida, Tatsuya,Kuwano, Ryoichi
, p. 3829 - 3839 (2018/04/14)
A chemoselective hydrogenation of isoquinoline carbocycles was achieved by using the catalyst prepared from Ru(methallyl)2(cod) and trans-chelate chiral ligand PhTRAP. The unique chemoselectivity achieved in this hydrogenation could be ascribed to the trans-chelation of the chiral ligand. The procedure for preparing the catalyst strongly affects the reproducibility of the carbocycle hydrogenation. Various 5-, 6-, 7-, and 8-substituted isoquinolines were selectively hydrogenated at their carbocycles to afford 5,6,7,8-tetrahydroisoquinolines as major products in high yields with moderate or good enantioselectivities. Some mechanistic studies suggested that the stereogenic center was created during the initial addition of H2 to the aromatic ring in the hydrogenation of 5-substituted isoquinolines. In other words, the stereochemical control was accompanied by the dearomatization.
Chemoselective One-Pot Synthesis of Functionalized Amino-azaheterocycles Enabled by COware
Clohessy, Thomas A.,Roberts, Alastair,Manas, Eric S.,Patel, Vipulkumar K.,Anderson, Niall A.,Watson, Allan J. B.
, p. 6368 - 6371 (2017/12/08)
Functionalized bicyclic amino-azaheterocycles are rapidly accessed in a one-pot cross-coupling/reduction sequence enabled by the use of COware. Incompatible reagents are physically separated in a single reaction vessel to effect two chemoselective transformations - Suzuki-Miyaura cross-coupling and heteroarene reduction. The developed method allows access to novel heterocyclic templates, including semisaturated Hedgehog and dual PI3K/mTOR inhibitors, which show enhanced physicochemical properties compared to their unsaturated counterparts.
Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
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, (2008/06/13)
The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.
INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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, (2008/06/13)
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras
PYRROLO-PYRIDINE DERIVATIVES
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, (2008/06/13)
Compounds of formula I are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia. STR1 wherein Q is STR2
Versatile and Efficient Synthesis of Aryl-1,2,3,4-tetrahydroisoquinolines: Nickel(II) Phosphine Ligand Catalyzed Coupling of Arylmagnesium Halides to Haloisoquinolines
Pridgen, Lendon N.
, p. 1289 - 1291 (2007/10/02)
Dichloronickel(II) (dppp) was used as catalyst to prepare some previously unreported arylisoquinolines 3, which were in turn hydrogenated to aryl-1,2,3,4-tetrahydroisoquinolines 2.This procedure is the most direct and ef
INTRAMOLECULAR FRIEDEL-CRAFTS ALKYLATIONS. II. AN EFFICIENT SYNTHESIS OF BIOLOGICALLY ACTIVE 1,2,3,4-TETRAHYDROISOQUINOLINES
Mendelson, W. L.,Spainhour, C. B.,Jones, S. S.,Lam, B. L.,Wert, K. L.
, p. 1393 - 1396 (2007/10/02)
A new synthesis of tetrahydroisoquinolines bearing electron withdrawing groups is presented.The scope and mechanism of the reaction are discussed.Many of these tetrahydroisoquinolines are potent inhibitors of the enzyme PNMT.
