Abstract: The present invention provides an efficient, safe and cost effective way to prepare 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)-benzenamine which is a key intermediate for the preparation of substituted pyrimidinylaminobenzamides of formula (II):
Type:
Grant
Filed:
June 7, 2006
Date of Patent:
August 24, 2010
Assignee:
Novartis AG
Inventors:
Stephan Abel, Murat Acemoglu, Bernhard Erb, Christoph Krell, Joseph Sclafani, Mark Meisenbach, Mahavir Prashad, Wen-Chung Shieh, Song Xue
Abstract: Method of asymmetrically hydrosilylating substrates using catalysts having a ligand of the compound of the formula (I) wherein R is optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; R? is hydrogen, optionally substituted lower alkyl; and R? is hydrogen, halogen, optionally substituted alkyl, hydroxy, amino (e.g., primary, secondary or tertiary), alkenyl; or an enantiomer thereof; or an enantiomeric mixture thereof with a transition metal. Particularly suitable reactions include the asymmetric hydrosilylation of ketones.
Abstract: The present invention provides bipyrimidinyl diphosphine compounds of the formula wherein R is optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; R? and R? are independently optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; or an enantiomer thereof; or an enantiomeric mixture thereof. The compounds of the formula (I) are chiral atropisomeric bipyrimidinyl diphosphine compounds and, thus, may be employed as ligands to generate chiral transition metal catalysts which may be applied in a variety of asymmetric reactions, e.g., in palladium catalyzed asymmetric allylic substitution reactions. The compounds of the present invention are easily accessible in high enantiomeric purity according to the methods disclosed herein.
Type:
Grant
Filed:
June 5, 2008
Date of Patent:
May 11, 2010
Assignee:
The Hong Kong Polytechnic University
Inventors:
Albert S Chan, Gang Chen, Rongwei Guo, Jing Wu
Abstract: Ionic liquids comprising a mixture of one or more triflate or bis(trifluoromethylsulfonyl)imide salt(s) with one or more Lewis acids(s), wherein the total of the molar contents of the Lewis acid(s) in the mixture is from about 0.01-98%, are provided, that are useful as catalysts in Lewis acid catalyzed reactions.
Type:
Grant
Filed:
July 16, 2004
Date of Patent:
April 6, 2010
Assignee:
Novartis AG
Inventors:
Peter Wasserscheid, Andreas Metlen, Nicole Brausch
Abstract: The present invention provides bipyrimidinyl diphosphine compounds of the formula wherein R is optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; R? and R? are independently optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; or an enantiomer thereof; or an enantiomeric mixture thereof. The compounds of the formula (I) are chiral atropisomeric bipyrimidinyl diphosphine compounds and, thus, may be employed as ligands to generate chiral transition metal catalysts which may be applied in a variety of asymmetric reactions, e.g., in palladium catalyzed asymmetric allylic substitution reactions. The compounds of the present invention are easily accessible in high enantiomeric purity according to the methods disclosed herein.
Type:
Grant
Filed:
May 11, 2005
Date of Patent:
March 9, 2010
Assignee:
The Hong Kong Polytechnic University
Inventors:
Albert Sun-Chi Chan, Gang Chen, Rongwei Guo, Jing Wu
Abstract: An improved drug delivery composition and method of use is disclosed. The composition comprises one or more biodegradable block copolymer drug carriers; and a reconstitution enhancing and enabling agent comprising polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative. The composition can be administered as is or after being be dissolved or rapidly reconstituted in an aqueous vehicle to afford a homogeneous solution or uniform colloidal systems.
Abstract: Method for the preparation of asymmetric alkynylated ?-amino esters of the formula wherein R1 and R2 are independently optionally substituted alkyl cycloalkyl, aryl or heteroaryl, and Y is hydrogen or a nitrogen protecting group.