CAS: 17508-17-7; O-(2,4-Dinitrophenyl)Hydroxylamine

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CAS号60506-35-6 2-(2,4-二硝基苯氧基)-... | CAS号54322-32-6 N-(2,4-二硝基苯氧基)乙亚氨酸乙酯 | CAS号97-00-7 1-氯-2,4-二硝基苯 | CAS号17508-16-6 2,4-二硝基苯氧基氨基甲酸叔丁酯 | CAS号584-48-5 1-溴-2,4-二硝基苯 | CAS号70-34-8 2,4-二硝基氟苯 | CAS号51-28-5 2,4-二硝基酚 | CAS号13181-41-4 O-(2,4-dinitrop... | CAS号13181-10-7 2-Propanone,O-(... | CAS号13059-86-4 Benzenamine,N-b... | CAS号42824-47-5 butylammonium s... | CAS号99907-90-1 O-(3,5-二氯苯基)羟胺 | CAS号427878-69-1 1-氨基-3-甲基-1H-吡咯...

1-氯-2,4-二硝基苯置于三乙胺,肼体系中,用 甲醇,二氯甲烷,丙酮 用作溶剂,化学反应 5.5H,反应生成2,4-二硝基苯基羟胺
参考文献:吡啶的脱芳构化:光化学骨架增大用于合成 1,2-二氮杂卓类药物
标题:吡啶的脱芳构化:光化学骨架增大用于合成 1,2-二氮杂卓类药物
摘要:在本报告中,我们开发了一种统一且标准化的一锅序列,通过插入氮原子将吡啶衍生物转化为1,2-二氮杂卓.这种骨架转变利用了 1-氨基吡啶鎓叶立德的原位生成,该叶立德在紫外线照射下会重新排列.对关键参数(波长,反应条件,活化剂)的彻底评估使我们能够制定出简单,温和且用户友好的方案.该模型反应被外推到 40 多个实例,包括药物衍生物,提供了独特的 7 元结构.机理证据支持二氮正环烯类物质的短暂存在.最后,对产品进行了相关转化,包括环收缩反应形成吡唑,并为所开发方案的广泛应用铺平了道路.
Doi:10.1021/jacs.3C14467

专利信息

专利号:US-9988349-B2
优先权日:2014-01-03
标 题:Direct stereospecific synthesis of unprotected aziridines from olefins
发明人：ESS DANIEL HALSELL; FALCK JOHN RUSSELL; JAT JAWAHAR LAL; KURTI LASZLO
权利人:ESS DANIEL HALSELL; FALCK JOHN RUSSELL; JAT JAWAHAR LAL; KURTI LASZLO
摘要:A method for the direct stereospecific conversion of structurally diverse mono-, di-, tri- and tetra-substituted olefins to N—H, N-alkyl, N-cycloalkyl, or N-aralkyl aziridines using a hydroxylamine amination agent with transition metal catalyst. The method is operationally simple (i.e., one-pot), scalable and fast at ambient temperature.

专利号:WO-2024121335-A1
优先权日:2022-12-07
标题:Synthesis of sulfoximine compounds having a stereogenic sulfur atom
发明人：WILLIAMS SIMON; SMITS HELMARS
权利人:SYNGENTA CROP PROTECTION AG
摘要:A process for the preparation of compound of formula (I) which process comprises: (A) stereoselectively oxidizing a sulfanyl compound of formula (II) followed by (B) stereospecific imination of a sulfinyl compound of formula (III) is disclosed wherein the substituents are as defined in claim 1.

专利号:WO-2023091726-A1
优先权日:2021-11-18
标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12)
发明人：BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH
权利人:SYROS PHARMACEUTICALS INC
摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).

专利号:US-2021238187-A1
优先权日:2017-04-11
标 题:Aziridine containing epothilone analogs, methods of synthesis, methods of treatment, and drug conjugates
发明人：NICOLAOU KYRIACOS C; RHOADES DEREK; WANG YANGPING
权利人:UNIV RICE WILLIAM M
摘要:In one aspect, the present disclosure provides epothilone analogs of the formula: (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.

专利号:US-10874646-B2
优先权日:2015-10-16
标 题 :Epothilone analogs, methods of synthesis, methods of treatment, and drug conjugates thereof
发明人：NICOLAOU KYRIACOS C; RHOADES DEREK; WANG YANPING; TOTOKOTSOPOULOS SOTIRIOS
权利人:UNIV RICE WILLIAM M
摘要:In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.

专利号:EP-4630421-A1
优先权日:2022-12-07
标 题:Synthesis of sulfoximine compounds having a stereogenic sulfur atom