CAS: 6704-31-0; Oxetan-3-One

上下游产品

CAS号7748-36-9 氧杂环丁-3-醇 | CAS号922500-97-8 3,3-二甲氧基氧杂环丁烷 | CAS号107-19-7 丙炔醇 | CAS号186581-53-3 重氮甲烷 | CAS号79-04-9 氯乙酰氯 | CAS号1093878-32-0 3-(4-溴苯基)氧杂环丁烷-3-醇 | CAS号922500-91-2 氧杂环丁烷-3-亚甲基乙酸乙酯 | CAS号21160-53-2 [2-(4-溴苯基)噻唑-4-基]甲醇 | CAS号885279-75-4 [2-(4-甲氧基苯基)-1,... | CAS号1105665-34-6 2-(氧杂环丁-3-亚基)乙酸甲酯 | CAS号1158098-73-7 3-[(叔丁基亚磺酰基)亚氨基... | CAS号1207360-89-1 N-ETHYL-N'-[4-[... | CAS号138650-20-1 3-(苄基氨基)氧杂环丁烷-3-腈 | CAS号162816-08-2 3-甲基氧杂环丁烷-3-醇 | CAS号23780-13-4 (2-苯基噻唑-4-基)甲醇

氧杂环丁-3-醇置于四磷十氧化物,二甲基亚砜,三乙胺体系中,用 二氯甲烷 作为反应溶剂,以48%的收率获得产物3-氧杂环丁酮
参考文献:药物发现中的氧杂环丁烷:结构和合成见解
标题:药物发现中的氧杂环丁烷:结构和合成见解
摘要:当取代常用的官能团(例如,宝石-二甲基或羰基)时,氧杂环丁烷可以引发水溶性,亲脂性,代谢稳定性和构象偏好的深刻变化.这些变化的幅度取决于结构环境.因此,通过替代宝石与二氧杂环丁烷一起使用时,在大多数情况下,水溶性降低了4倍,达到4000倍以上,同时降低了新陈代谢的降解速率.氧杂环丁烷掺入脂肪族链中可引起构象变化,有利于链的向斜排列而不是反平面排列.另外,螺环氧杂环丁烷(例如2-Oxa-6-氮杂螺环[3.3]庚烷)与药物发现中常用的片段(例如吗啉)具有显着的相似性,甚至能够取代后者的增溶能力.丰富的oxetan-3-One和衍生的michael受体化学物质为制备各种以前未记录的新型oxetanes提供了场所,因此为它们在化学和药物发现中的广泛应用提供了基础.
DOI:10.1021/jm9018788

专利信息

专利号:US-12247037-B2
优先权日:2018-12-12
标题:1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-A][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders
发明人：BRANDT GARY
权利人:NEUMORA THERAPEUTICS INC
摘要:The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).

专利号:US-2024400552-A1
优先权日:2016-11-11
标题 :Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-11622968-B2
优先权日:2011-03-08
标 题:Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-10226449-B2
优先权日:2013-12-20
标 题:Heterocyclic modulators of lipid synthesis and combinations thereof
发明人：HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE
权利人:3 V BIOSCIENCES INC
摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.

专利号:US-11034690-B2
优先权日:2016-11-11
标 题:Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC; SAGINIET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-9428502-B2
优先权日:2012-07-03
标题:Heterocyclic modulators of lipid synthesis
发明人：OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; WAGMAN ALLAN S
权利人:3-V BIOSCIENCES INC
摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.