- Development of safe and scalable continuous-flow methods for palladium-catalyzed aerobic oxidation reactions
-
The synthetic scope and utility of Pd-catalyzed aerobic oxidation reactions has advanced significantly over the past decade, and these reactions have the potential to address important green-chemistry challenges in the pharmaceutical industry. This potential has not been realized, however, because safety concerns and process constraints hinder large-scale applications of this chemistry. These limitations are addressed by the development of a continuous-flow tube reactor, which has been demonstrated on several scales in the aerobic oxidation of alcohols. Use of a dilute oxygen gas source (8% O2 in N 2) ensures that the oxygen/organic mixture never enters the explosive regime, and efficient gas-liquid mixing in the reactor minimizes decomposition of the homogeneous catalyst into inactive Pd metal. These results provide the basis for large-scale implementation of palladium-catalyzed (and other) aerobic oxidation reactions for pharmaceutical synthesis. The Royal Society of Chemistry 2010.
- Ye, Xuan,Johnson, Martin D.,Diao, Tianning,Yates, Matthew H.,Stahl, Shannon S.
-
scheme or table
p. 1180 - 1186
(2010/10/20)
-
- PYRIDINYL AMINE DERIVATIVES AS INHIBITORS OF CHOLESTERYL ESTER TRANSFER PROTEIN (CETP)
-
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the variables are as defined, useful as inhibitors of chlosteryl ester transfer protein.
- -
-
Page/Page column 101
(2008/06/13)
-
- Dibenzyl Amine Compounds and Derivatives
-
Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid le
- -
-
Page/Page column 34
(2010/11/28)
-
- Dibenzylamine compound and medicinal use thereof
-
A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 alkyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7) (R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.
- -
-
Page/Page column 37
(2010/02/11)
-