Cyclocondensation of oxalyl chloride with 1,2-glycols
摘要:
Oxalyl chloride reacts with a wide range of acyclic 1,2-glycols 1 in the presence of triethylamine to produce 1,3-dioxolan-2-ones 3 together with 1,4-dioxane-2,3-diones 2. Ethylene glycol (1d), monosubstituted ethylene glycols 1e, j-1, and erythro-1,2-disubstituted ethylene glycols 1f, m,o provide the cyclic carbonates 3 as the minor products, while the threo-compounds 1g, i, n,p,q and pinacol (1h) afford 3 as the main products. The formation of 3 may be rationalized in terms of stereoelectronically controlled cleavage of the conjugate base 17- of the tetrahedral intermediates. The rate for the conformational change of 17- into 18- and the equilibrium constant between these conformers are proposed to be the major factors affecting the reaction pattern.
Enantioselective Hydroalkenylation of Olefins with Enol Sulfonates Enabled by Dual Copper Hydride and Palladium Catalysis
作者:Alexander W. Schuppe、James Levi Knippel、Gustavo M. Borrajo-Calleja、Stephen L. Buchwald
DOI:10.1021/jacs.1c02117
日期:2021.4.14
The catalytic enantioselective synthesis of α-chiral olefins represents a valuable strategy for rapid generation of structural diversity in divergent syntheses of complex targets. Herein, we report a protocol for the dual CuH- and Pd-catalyzed asymmetric Markovnikov hydroalkenylation of vinyl arenes and the anti-Markovnikov hydroalkenylation of unactivated olefins, in which readily available enol triflates
Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
申请人:Carter H. Percy
公开号:US20050054626A1
公开(公告)日:2005-03-10
The present application describes modulators of MCP-1 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
The chemical shifts and 31P-H spin-spincouplingconstants of protons on saturated CH groups have been examined for a variety of model organophosphorus compounds. Correlations of these data with the charge on the phosphorus atom and proximity of hydrogen atoms to that nucleus are suggested and related to other data previously reported in the literature.
[EN] HYODEOXYCHOLIC ACID DERIVATIVES AND USE THEREOF<br/>[FR] DÉRIVÉS D'ACIDE HYODEOXYCHOLIQUE ET LEURS UTILISATIONS
申请人:BAR PHARMACEUTICALS SOCIETA' A RESPONSABILITA' LIMITATA
公开号:WO2018002897A1
公开(公告)日:2018-01-04
The present invention concerns compounds having formula (I) and compositions thereof with a pharmacologically acceptable excipient and uses thereof as a medicament, in particular for the treatment and/or prevention of a disorder selected from the group consisting of: gastrointestinal disorders, liver diseases, cardiovascular and vascular diseases, pulmonary and metabolic diseases, infectious diseases, cancer, renal disorders, inflammatory disorders comprising immune mediated disorders, and neurological disorders.
Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against bacteria, including gram positive organisms, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.