[EN] GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES [FR] ANTAGONISTE DES RECEPTEURS DU GLUCAGON, PREPARATION ET UTILISATIONS THERAPEUTIQUES
Nickel-Catalyzed Umpolung Arylation of Ambiphilic α-Bromoalkyl Boronic Esters
作者:Shang-Zheng Sun、Ruben Martin
DOI:10.1002/anie.201712428
日期:2018.3.26
A nickel‐catalyzed reductive arylation of ambiphilic α‐bromoalkyl boronic esters with aryl halides is described. This platform provides an unrecognized opportunity to promote the catalytic umpolung reactivity of ambiphilic reagents with aryl halides, thus unlocking a new cross‐coupling strategy that complements existing methods for the preparation of densely functionalized alkyl‐substituted organometallic
We developed a chromium-catalyzed, photochemical, and linear-selective alkylation of aldehydes with alkylzirconium species generated in situ from a wide range of alkenes and Schwartz’s reagent. Photochemical homolysis of the C–Zr bond afforded alkyl radicals, which were then trapped by a chromium complex catalyst to generate the alkylchromium(III) species for polar addition to aldehydes. The reaction
Glucagon receptor antagonists, preparation and therapeutic uses
申请人:Eli Lilly and Company
公开号:US07816557B2
公开(公告)日:2010-10-19
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES
申请人:CONNER Scott Eugene
公开号:US20110124648A1
公开(公告)日:2011-05-26
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
Deaminative Addition of Alkylpyridinium Salt to Aldehyde
作者:Yu Huang、Zhengqiang Liu、Wenbo H. Liu
DOI:10.1021/acs.orglett.3c01724
日期:2023.7.7
Here we show that a primary amine can engage in the nucleophilic addition to an aldehyde to synthesize an alcohol following preactivation of the amine. The enabling reagent for this radical-polar crossover process is CrCl2. This reaction is selective for aldehydes and compatible with numerous functional groups, which are not tolerated under classical Grignard-type conditions. Complementary to the well-established