CAS: 163521-08-2; 5-(4-(4-(5-Cyano-1H-Indol-3-yl)Butyl)Piperazin-1-yl)Benzofuran-2-Carboxamide Hydrochloride

上下游产品

3β,11α-diacetoxy-17-hydroxy-16α-methyl-5α-pregnan-20-one 3β,11α-diacetoxy-5α-pregn-16-en-20-one (17Ξ)-3β,11α,20-triacetoxy-16α-methyl-5α-pregn-17(20)-ene

维拉佐酮置于盐酸,甲酸体系中,用 水 用作溶剂,化学反应 0.5H,以96.5%的收率获得盐酸维拉唑酮
参考文献:开发用于大规模制备维拉佐酮的稳健且可扩展的工艺
标题:开发用于大规模制备维拉佐酮的稳健且可扩展的工艺
摘要:开发了一种稳健且可扩展的维拉佐酮合成方法,以避免在酒精条件下形成源自 N-去甲苯基化反应的杂质.在我们的研究中,这些杂质,潜在的基因毒性甲苯磺酸烷基酯和不合格的吲哚 N-烷基化维拉佐酮,被确定为从未报告过的工艺杂质.通过调整官能团的转变,该过程成功地防止了甲苯磺酰基遇到任何醇盐,这将不可避免地导致甲苯磺酸烷基酯和吲哚n-烷基化维拉佐酮副产物的产生.此外,该制造工艺也已在千克规模上进行了演示,可生产 1.05 千克盐酸维拉佐酮,总产率为 71%(以 5-(哌嗪-1-基)苯并呋喃-2-甲酸乙酯盐酸盐计算)7.盐酸).产品HPLC检测纯度>99.5%,任何单一杂质<0.1% HPLC面积百分比.未检测到吲哚 N-烷基化维拉佐酮,产率比之前的 Friedel-Crafts 酰化途径高 10%.
Doi:10.1021/acs.Oprd.2C00206

专利信息

专利号:WO-2025019775-A1
优先权日:2023-07-19
标题 :Endoxifen compositions and methods of use thereof and synthesis thereof
发明人：QUAY STEVEN
权利人:ATOSSA THERAPEUTICS INC
摘要:Described herein are endoxifen compositions comprising novel compounds and methods of use thereof. Methods of synthesis for the compositions are described herein. The endoxifen compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The endoxifen compositions described herein may be useful in the treatment of a condition in a subject, such as cancer.

专利号:US-2025241876-A1
优先权日:2023-07-19
标 题:Anti-tumor compounds and methods of use thereof and synthesis thereof
发明人：QUAY STEVEN CARL
权利人:ATOSSA THERAPEUTICS INC
摘要:Described herein are pharmaceutical compounds and compositions and methods of making thereof. Methods of synthesis for the compounds are described herein. The compounds or compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The compounds and compositions described herein may be useful in the treatment of a condition in a subject.

专利号:WO-2008084057-A1
优先权日:2007-01-10
标题:Compounds with a combination of cannabinoid-cb1 antagonism and serotonin reuptake inhibition
发明人：LANGE JOSEPHUS H M; KRUSE CORNELIS G
权利人:SOLVAY PHARM BV; LANGE JOSEPHUS H M; KRUSE CORNELIS G
摘要:This invention relates to compounds with a combination of cannabinoid-CB1antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the general formula (I): wherein the symbols have the meanings given in the specification.

专利号:US-8138174-B2
优先权日:2007-01-10
标 题:Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition
发明人：LANGE JOSEPHUS H M; KRUSE CORNELIS G
权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SOLVAY PHARM BV
摘要:Compounds with a combination of cannabinoid CB 1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed. n In at least one embodiment, the invention relates to compounds of the general formula (1): n nwherein the substitutents have the definitions given in the specification.

专利号:CN-103880729-B
优先权日:2014-03-27
标题 :A new process for the synthesis of vilazodone intermediate 5-cyano-3(4-chlorobutyl)-indole

专利号:CN-103880729-A
优先权日:2014-03-27
标 题 :A new process for the synthesis of vilazodone intermediate 5-cyano-3(4-chlorobutyl)-indole