Synthesis of the β2 Agonist (R)-Salmeterol Using a Sequence of Supported Reagents and Scavenging Agents
摘要:
graphicThe enantioselective synthesis of (R)-salmeterol has been achieved by using a sequence of supported reagents and sequestering agents. The saligenin core was installed by a regiospecific alkylation and a chiral auxiliary approach was employed to introduce the desired stereochemistry via a diastereoselective reduction.
The present invention is directed to a compound of formula (I),
methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
An expedient synthetic approach has been developed for the unified total synthesis of (+)-chinensiolide B and (+)-8-epigrosheimin. The point of divergence was provided by the lactone aldehyde 6, in which four contiguous stereocenters were achieved by stereocontrolled Evans syn-aldol reaction of R-carvone derived enantiopure aldehyde and chiral N-succinyl-oxazolidinone. The lactone aldehyde 6 was synthesized
已经开发了一种方便的合成方法,用于统一合成(+)-chinensiolide B和(+)-8-epigrosheimin。分歧点是由内酯醛6提供的,其中通过R-香芹酮衍生的对映纯醛和手性N-琥珀酰-恶唑烷酮的立体控制Evans syn-aldol反应获得了四个连续的立体中心。分三步以数克的量合成内酯醛6。高度优化的化学和立体选择反应以及官能团的相互转化使我们能够从6位组装(+)-chinensiolide B amd(+)-8-epigrosheimin。
Catalyst system
申请人:Eastham Graham
公开号:US20060252935A1
公开(公告)日:2006-11-09
A catalyst suitable for carbonylating ethylenically unsaturated compounds comprising a Group VIIIB metal or compound thereof and a metallocene.
一种适用于酰化乙烯基不饱和化合物的催化剂,包括VIIIB族金属或其化合物和金属茂配合物。
Catalyst System
申请人:Eastham Graham
公开号:US20070282124A1
公开(公告)日:2007-12-06
The present invention provides a catalyst system capable of catalysing the carbonylation of an ethylenically unsaturated compound, which system is obtainable by combining: a) a metal of Group VIB or Group VIIIB or a compound thereof, b) a bidentate phosphine, arsine or stibine ligand, and c) an acid, wherein said ligand is present in at least a 2:1 molar excess compared to said metal or said metal in said metal compound, and that said acid is present in at least a 2:1 molar excess compared to said ligand, a process for the carbonylation of an ethylenically unsaturated compound, a reaction medium, and use of the system.
The present invention provides a catalyst system capable of catalysing the carbonylation of an ethylenically unsaturated compound, which system is obtainable by combining:
a) a metal of Group VIB or Group VIIIB or a compound thereof,
b) a bidentate phosphine, arsine or stibine ligand, and
c) an acid,
wherein said ligand is present in at least a 2:1 molar excess compared to said metal or said metal in said metal compound, and that said acid is present in at least a 2:1 molar excess compared to said ligand, a process for the carbonylation of an ethylenically unsaturated compound, a reaction medium, and use of the system.