The present invention provides novel benzene compounds presented by the following formulas, and analogs thereof, that exert an ACC activity-inhibiting effect that is effective in the treatment of obesity, hyperlipemia, fatty liver, hyperglycemia, impaired glucose tolerance, diabetes, diabetic complications (diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, and diabetic macroangiopathy, hypertension, arteriosclerosis), hypertension, and arteriosclerosis.
Benzodiazepine derivatives, compositions containing them and their use in therapy
申请人:MERCK SHARP & DOHME LTD.
公开号:EP0514133A1
公开(公告)日:1992-11-19
Compounds of formula (I), and salts and prodrugs thereof
wherein:
R¹ represents optionally substituted C₁₋₆alkyl or C₃₋₇cycloalkyl;
R² represents an optionally substituted phenyl or pyridyl group;
R³ represents C₁₋₆ alkyl or halo;
R⁴ represents C₃₋₇ cycloalkyl;
X is 0, 1, 2 or 3;
are CCK and/or gastrin antagonists. They and compositions thereof are therefore useful in therapy.
Catalytic activity of magnetic Fe3O4@Diatomite earth and acetic acid for the N-acylation of sulfonamides
作者:Mohammad Hadi Ghasemi、Elaheh Kowsari、Seyed Kiumars Hosseini
DOI:10.1016/j.tetlet.2015.12.044
日期:2016.1
The Brønsted and Lewis acidic promoted N-acylation of sulfonamides with acetic anhydride or benzoyl chloride has been achieved using glacialacetic acid and magnetic Fe3O4@Diatomite earth. Use of acetic acid as solvent omits the need for organic bases and permits the isolation of products by filtration and precipitation. Additionally, the magnetic composite Fe3O4@Diatomite acts as a conjugate proton
使用冰醋酸和磁性Fe 3 O 4 @硅藻土可以实现磺酰胺与乙酸酐或苯甲酰氯的Brønsted和Lewis酸性促进的N-酰化反应。使用乙酸作为溶剂不需要有机碱,并允许通过过滤和沉淀分离产物。此外,磁性复合材料Fe 3 O 4硅藻土还可以作为共轭质子超强酸,实现磺酰胺化合物的酰化。
An expeditious and convenient synthesis of acylsulfonamides utilizing polymer-supported reagents
作者:Ying Wang、Kathy Sarris、Daryl R. Sauer、Stevan W. Djuric
DOI:10.1016/j.tetlet.2007.05.158
日期:2007.7
Acylsulfonamides can be rapidly and conveniently synthesized from a variety of carboxylic acids and sulfonamides utilizing the commercially available reagents, PS-DCC and DMAP under mild reaction conditions. DMAP can be efficiently scavenged by utilization of a silica-supported tosic acid cartridge (Si-SCX). In most of the cases studied, products with high purities and yields were obtained without