CAS: 115010-10-1; Benzo[d][1,3]Dioxole-5-Sulfonyl Chloride

相似化合物

313681-67-3 147809-42-5 246033-22-7

上下游产品

CAS号274-09-9 1,2-亚甲二氧基苯 | CAS号79-37-8 草酰氯 | CAS号107-06-2 1,2-二氯乙烷 | CAS号75-34-3 1,1-二氯乙烷标准溶液 | CAS号94839-07-3 3,4-(亚甲基二氧基)苯硼酸 | CAS号69849-38-3 trimethyl(3,4-m...

📜胡椒环置于氯化亚砜,硫酸,乙酸酐,N,N-二甲基甲酰胺体系中,用 乙酸乙酯 用作溶剂,化学反应 6.5H,反应生成1,3-苯并二氧-5-磺酰氯
参考文献:以 D2/d3 受体配体为特征的新型构象限制性 N-芳基哌嗪衍生物的设计,合成和药理学评价,可用于治疗神经退行性疾病
标题:以 D2/d3 受体配体为特征的新型构象限制性 N-芳基哌嗪衍生物的设计,合成和药理学评价,可用于治疗神经退行性疾病
摘要:大多数神经退行性疾病是多因素的,与其发病机制相关的几种分子机制的发现不断推进.多巴胺和多巴胺能受体亚型涉及几种神经系统疾病的病理生理学,例如精神分裂症,抑郁症和药物成瘾.因此,多巴胺能系统和多巴胺受体配体在此类疾病的治疗中起关键作用.在这种情况下,一系列对 D 2 /d 3具有非常好亲和力的新型构象受限的n-芳基哌嗪衍生物 ( 5A-F )本文报道了多巴胺受体.化合物被设计为药物阿立哌唑 (2) 和卡利拉嗪 (3) 的苯间苯类似物,呈现 1,3-苯并二氧戊环亚基作为这些受体二级结合位点的配体.使用经典方法以非常好的收率合成了六种新的n-芳基哌嗪化合物,并进行了结合和鸟苷三磷酸 (Gtp) 位移研究.发现靶受体的亲和力值低于 1 μm 和不同的内在功效谱.对接研究表明,化合物5A-F与多巴胺 D 2和 D 3呈现不同的结合模式受体,主要是由于对 2 和 3 的柔性间隔基施加的构象限制.
Doi:10.3390/biom12081112

专利信息

专利号:US-5387681-A
优先权日:1992-08-19
标题:Synthesis of bicyclic aromatic sulfonic acids sulfonyl chlorides and sulfonamides
发明人：MILLER WILLIAM D; TAO EDDIE V P
权利人:LILLY CO ELI
摘要:This invention provides a novel process for the synthesis of bicyclic aromatic sulfonic acids employing reacting a bicyclic aromatic compound with sulfur trioxide-N,N-dimethylformamide complex in the presence of a water miscible, non-reactive solvent. The resulting sulfonic acid may be converted into the corresponding sulfonyl halide by the reaction with a thionyl halide. This invention further provides a novel process for the synthesis of bicyclic aromatic sulfonamides employing the reaction conditions described supra followed by an ammonolysis or amination.

专利号:EP-0254577-B1
优先权日:1986-07-23
标 题:Synthesis of bicyclic aromatic sulfonyl chlorides
摘要:A process for preparing bicyclic aromatic sulfonyl chlorides of the formula wherein, n is 1 or 2; A is -O- or -CH2-; and B is -O-, -CH2-, or -NCH3-; provided at least one of A or B is -O-, which comprises reacting a compound of the formula with a Villsmeier reagent of the formula The bicyclic aromatic sulfonyl chlorides produced by the process can be used to prepare pharmaceutically useful sulfonylureas.

专利号:US-8563590-B2
优先权日:2008-03-05
标 题 :Compounds, compositions and methods for the treatment of islet amyloid polypeptide (IAPP) accumulation in diabetes
发明人：LAKE THOMAS; SNOW ALAN D
权利人:LAKE THOMAS; SNOW ALAN D; PROTEOTECH INC
摘要:Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of IAPP or amylin fibril diseases, and the manufacture of medicaments for such treatment.

专利号:US-6140505-A
优先权日:1995-03-10
标 题:Synthesis of benzo fused heterocyclic sulfonyl chlorides

专利号:US-8829198-B2
优先权日:2007-10-31
标 题:Compounds, compositions and methods for the treatment of beta-amyloid diseases and synucleinopathies
发明人：ESPOSITO LUKE A; HUDSON F MICHAEL; LAKE THOMAS; CUMMINGS JOEL; WEIGELE MANFRED; SNOW ALAN D; LARSEN LESLEY
权利人:ESPOSITO LUKE A; HUDSON F MICHAEL; LAKE THOMAS; CUMMINGS JOEL; WEIGELE MANFRED; SNOW ALAN D; LARSEN LESLEY; PROTEOTECH INC
摘要:Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of β-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

专利号:US-8916598-B2
优先权日:2003-05-30
标题 :Compounds, compositions, and methods for the treatment of β-amyloid diseases and synucleinopathies
发明人：ESPOSITO LUKE A; HUDSON F MICHAEL; LAKE THOMAS; CUMMINGS JOEL; WEIGELE MANFRED; SNOW ALAN D
权利人:ESPOSITO LUKE A; HUDSON F MICHAEL; LAKE THOMAS; CUMMINGS JOEL; WEIGELE MANFRED; SNOW ALAN D; PROTEOTECH INC
摘要:Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.