[EN] RENIN INHIBITORS<br/>[FR] INHIBITEURS DE LA RÉNINE
申请人:MERCK FROSST CANADA LTD
公开号:WO2009070869A1
公开(公告)日:2009-06-11
The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
Synthesis of 1,1-Diarylethylenes via Efficient Iron/Copper Co-Catalyzed Coupling of 1-Arylvinyl Halides with Grignard Reagents
作者:Abdallah Hamze、Jean-Daniel Brion、Mouad Alami
DOI:10.1021/ol3010112
日期:2012.6.1
An efficient access to 1,1-diarylethylenes of biological interest by coupling functionalized aryl Grignard reagents and 1-arylvinyl halides in the presence of FeCl3/CuTC is described. This bimetallic system proved to be superior to the use of Fe or Cu catalyst alone. The synthetic utility of this protocol is illustrated in the field of steroid chemistry.
A general palladium-catalyzed cross-coupling of aryl fluorides and organotitanium (IV) reagents
作者:Xiao-Yun He
DOI:10.1007/s00706-021-02796-6
日期:2021.7
Pd(OAc)2/1-[2-(di-tert-butylphosphanyl)phenyl]-4-methoxy-piperidine was demonstrated to effectively catalyze cross-coupling of aryl fluoride and aryl(alkyl) titanium reagent. Both electron-deficient and electron-rich aryl fluoride can react effectively with nucleophile and provide extensive functional groups tolerance. 2-Arylated product was realized by selective activation of the C–F bond. Graphic
Preparation of arenesulphonyl chlorides from Grignard reagents
作者:S. N. Bhattacharya、C. Eaborn、D. R. M. Walton
DOI:10.1039/j39680001265
日期:——
Reaction of phenylmagnesium bromide with excess of sulphuryl chloride in ether–hexane at 0° gives benzenesulphonyl chloride and bromide in a combined yield of at least 58%. Substituted sulphonyl halides, YC6H4·SO2X (Y =o-Me, m-Me, m-Cl, and m-CF3), are produced similarly in comparable yields. Diphenylmagnesium, diphenylcadmium, or phenyl-lithium under similar conditions give somewhat smaller yields
苯基溴化镁与过量的磺酰氯在乙醚中的溶剂在0°下反应,得到的苯磺酰氯和溴化物的总收率至少为58%。类似地以可比较的产率生产取代的磺酰卤YC 6 H 4 ·SO 2 X(Y = o -Me,m -Me,m -Cl和m -CF 3)。在相似条件下,二苯基镁,二苯基镉或苯基锂的苯磺酰卤的收率要小一些。使用芳基氯化镁ArMgCl(Ar = Ph,o -MeO·C 6 H 4,p -Me 3 Si·C6 H 4和C 6 Cl 5),在四氢呋喃-己烷中,于0°产生纯的芳烃磺酰氯,产率为53-64%。
Transition metal complexes of N-heterocyclic carbenes, method of preparation and use in transition metal catalyzed organic transformations
申请人:Organ G. Michael
公开号:US20070073055A1
公开(公告)日:2007-03-29
The present invention relates to catalysts of transition metal complexes of N-heterocyclic carbenes, their methods of preparation and their use in chemical synthesis. The synthesis, ease-of-use, and activity of the compounds of the present invention are substantial improvements over in situ catalyst generation. Further, the transition metal complexes of N-heterocyclic carbenes of the present invention may be used as precatalysts in metal-catalyzed cross-coupling reactions.