diallyl phosphoramidate | 54590-46-4

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磷酸及其衍生物
• 英文名称: diallyl phosphoramidate
• 英文别名: amidophosphoric acid diallyl ester；Amidophosphorsaeure-diallylester；Diallyl-amidophosphat；3-[Amino(prop-2-enoxy)phosphoryl]oxyprop-1-ene
• CAS: 54590-46-4
• 化学式: C₆H₁₂NO₃P
• 分子量: 177.14
• InChiKey: AXHNIMHHNSDJPV-UHFFFAOYSA-N

物化性质

• 熔点：
  12-14 °C
• 沸点：
  330.4±31.0 °C(Predicted)
• 密度：
  1.118±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  11
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  61.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  聚合甲醛 、 diallyl phosphoramidate 在 水 作用下， 生成 bis-(diallyloxyphosphoryl-amino)-methane
  参考文献：
  名称：

  Unsaturated aliphatic phosphonamides

  摘要：

  公开号：

  US02574516A1
• 作为产物：
  描述：

  氯磷酸二烯丙酯 在 甲苯 作用下， 生成 diallyl phosphoramidate
  参考文献：
  名称：

  Unsaturated aliphatic phosphonamides

  摘要：

  公开号：

  US02574516A1
• 作为试剂：
  描述：

  6-O-[4-O-[bis(2-propenyloxy)phosphinyl]-2-deoxy-3-O-[(3R)-3-methoxydecyl]-6-O-methyl-2-[[(11Z)-1-oxo-11-octadecenyl]amino]-β-D-glucopyranosyl]-3-O-decyl-2-deoxy-2-[(1,3-dioxotetradecyl)amino]-D-glucopyranose 4-(2-propenylcarbonate) 、 diallyl phosphoramidate 在 diallyl phosphoramidate 作用下， 以83.5的产率得到6-O-[4-O-[bis(2-propenyloxy)phosphynyl]-2-deoxy-3-O-[(3R)-3-methoxydecyl]-6-O-methyl-2-[((11Z)-1-oxo-11-octadecenyl)amino]-β-D-glucopyranosyl]-3-O-decyl-2-deoxy-2-[(1,3-dioxotetradecyl)amino]-α-D-glucopyranose-1-(di-2-propenylphosphate) 4-(2-propenylcarbonate)
  参考文献：
  名称：

  PROCESS FOR PRODUCTION OF LIPID A ANALOGUE

  摘要：

  本发明公开了一种制备α-D-葡萄糖吡喃糖，3-O-癸基-2-脱氧-6-O-[2-脱氧-3-O-[(3R)-3-甲氧基癸基]-6-O-甲基-2-[(11Z)-1-氧代-11-十八碳烯基]氨基]-4-O-膦酸-β-D-葡萄糖吡喃糖-2-[(1,3-二氧代-四十碳基)氨基]-或1-(二氢磷酸)四钠盐的方法，该方法可用作制药活性成分或其合成中间体，具有环保、安全、易操作和重复性优异的特点。一种制备式(I)化合物的方法，包括以下步骤：在核苷酸试剂的存在下，用钯催化剂反应式(VIII)化合物，并用钠源处理产物。

  公开号：

  EP1939209A1

文献信息

• PYRAZOLE COMPOUNDS, FORMULATIONS THEREOF, AND A METHOD FOR USING THE COMPOUNDS AND/OR FORMULATIONS
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US20210061798A1

  公开（公告）日：2021-03-04

  Disclosed herein are embodiments of a pyrazole compound according to formula I. Compositions comprising the compound, and a method for making the composition also are disclosed. The composition may comprise a carrier, such as a polymer and/or the composition may be a spray-dried formulation. Also disclosed is a method for using the compound and/or composition. The compound and/or composition may be useful to inhibit an IRAK protein and/or to ameliorate, treat and/or prevent an IRAK-associated disease or condition in a subject.

  披露了根据公式I的吡唑化合物的一种实施例。还披露了包含该化合物的组合物以及制造该组合物的方法。该组合物可以包含载体，例如聚合物和/或该组合物可以是喷雾干燥的制剂。还披露了一种使用该化合物和/或组合物的方法。该化合物和/或组合物可用于抑制IRAK蛋白和/或在主体上改善、治疗和/或预防IRAK相关疾病或状况。
• [EN] POLYAMINE-FATTY ACID DERIVED LIPIDOIDS AND USES THEREOF<br/>[FR] LIPIDOÏDES DÉRIVÉS DE POLYAMINE-ACIDE GRAS ET LEURS UTILISATIONS
  申请人：MASSACHUSETTS INST TECHNOLOGY

  公开号：WO2016004202A1

  公开（公告）日：2016-01-07

  The present disclosure provides polyamine-fatty acid derived lipidoids (e.g., compounds of Formula (I) or (II)) and methods of preparing the lipidoids. A described lipidoid includes R-C(=0)-0- moieties (where R is a lipid moiety), which may be hydrolyzed into non-toxic fatty acids. Also provided are compositions including a described lipidoid and an agent (e.g., polynucleotide, small molecule, peptide, or protein). The present disclosure also provides methods, kits, and uses that involve the lipidoids or compositions for delivering an agent to a subject, tissue, or cell and/or for treating and/or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, immunological diseases, gastrointestinal diseases, respiratory diseases, painful conditions, psychiatric disorders, and metabolic disorders.

  本公开提供了聚胺脂肪酸衍生的脂质体（例如，化合物的化学式（I）或（II））以及制备脂质体的方法。所述脂质体包括R-C(=0)-0-基团（其中R是脂质基团），可以水解为无毒脂肪酸。还提供了包括所述脂质体和药剂（例如，多核苷酸、小分子、肽或蛋白质）的组合物。本公开还提供了涉及脂质体或组合物用于将药剂传递给受体、组织或细胞和/或用于治疗和/或预防一系列疾病的方法、试剂盒和用途，例如遗传疾病、增殖性疾病、血液疾病、神经系统疾病、免疫系统疾病、胃肠道疾病、呼吸系统疾病、疼痛症状、精神障碍和代谢性疾病。
• [EN] SYNTHESIS OF BACKBONE MODIFIED MORPHOLINO OLIGONUCLEOTIDES AND CHIMERAS USING PHOSPHORAMIDITE CHEMISTRY<br/>[FR] SYNTHÈSE D'OLIGONUCLÉOTIDES MORPHOLINO MODIFIÉS PAR SQUELETTE ET CHIMÈRES UTILISANT LA CHIMIE PHOSPHORAMIDITE
  申请人：UNIV COLORADO REGENTS

  公开号：WO2018057430A1

  公开（公告）日：2018-03-29

  Amine substituted morpholino oligonucleotides, other than the classical N,N-dimethylamino PMO analogue, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. Morpholino oligonucleotides having thiophosphoramidate, phosphoramidate, phosphoramidate diester, and alkyl phosphoramidate linkers. Chimeras containing unmodified DNA/RNA and other analogs of DNA/RNA can be prepared. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous applications.

  提供了替代传统N,N-二甲基氨基PMO类似物的吗啉基寡核苷酸以及高产率有效合成这些寡核苷酸的方法。这些寡核苷酸具有硫代磷酰胺酸酰胺、磷酸酰胺酰胺、磷酸酰胺二酯和烷基磷酰胺酰胺连接基。可以制备含有未修饰DNA/RNA和其他DNA/RNA类似物的嵌合体。这些寡核苷酸与互补的DNA或RNA形成的双链比天然DNA或DNA/RNA复合物更稳定，与RNA酶H1活性，可以使用标准脂质试剂转染到细胞中。因此，这些类似物在许多应用中非常有用。
• [EN] N- [ (2 ' R) -2 ' -DEOXY-2 ' -FLUORO-2 ' -METHYL-P-PHENYL-5 ' -URIDYLYL] -L-ALANINE 1-METHYLETHYL ESTER AND PROCESS FOR ITS PRODUCTION<br/>[FR] ESTER DE N-[(2 ' R) -2' -DÉSOXY-2' -FLUORO-2' -MÉTHYL-P-PHÉNYL-5' -URIDYLYL]-L-ALANINE 1-MÉTHYLÉTHYLE ET SON PROCÉDÉ DE PRODUCTION
  申请人：PHARMASSET INC

  公开号：WO2010135569A1

  公开（公告）日：2010-11-25

  Disclosed herein are nucleoside phosphoramidates of formula 4 and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals. Disclosed is also a process for preparing compound represented by formula 4: (Formula 4) wherein P* represents a chiral phosphorus atom, which comprises: a) reacting an isopropyl-alanate, (Formula A), a di-X'-phenylphosphate, (Formula B), 2'-deoxy-2f-fluoro-2'-C-methyluridine, (Formula 3), and a base to obtain a first mixture comprising 4; wherein X is a conjugate base of an acid, n is 0 or 1, and X' is a halogen, b) reacting the first mixture with a protecting compound to obtain a second mixture comprising 4; and c) optionally subjecting the second mixture to crystallization, chromatography or extraction in order to obtain 4.

  本文披露了化学式4的核苷酸磷酰胺及其作为治疗病毒性疾病的药物的用途。这些化合物是RNA依赖性5RNA病毒复制的抑制剂，可作为HCV NS5B聚合酶的抑制剂，HCV复制的抑制剂以及哺乳动物丙型肝炎感染的治疗药物。还披露了一种制备化合物4的方法：（化学式4），其中P*代表手性磷原子，包括：a）反应异丙基-丙氨酸酯（化学式A）、二-X'-苯基磷酸酯（化学式B）、2'-脱氧-2f-氟-2'-C-甲基尿嘧啶（化学式3）和碱以获得含有4的第一混合物；其中X是酸的共轭碱基，n为0或1，X'是卤素；b）将第一混合物与保护化合物反应以获得含有4的第二混合物；c）可选地将第二混合物经结晶、色谱或萃取处理以获得4。
• [EN] BLOCK CO-POLY(METAL ORGANIC NANOSTRUCTURES) (BCPMONs) AND USES THEREOF<br/>[FR] CO-POLY(NANOSTRUCTURES ORGANOMÉTALLIQUES) SÉQUENCÉES (BCPMON) ET LEURS UTILISATIONS
  申请人：MASSACHUSETTS INST TECHNOLOGY

  公开号：WO2018022944A1

  公开（公告）日：2018-02-01

  The present disclosure provides (block co-polymer)-(metal organic framework) conjugates (BCPMOFs), such as (block co-polymer)-(metal organic nanostructure) conjugates (BCPMONs), and thermoplastic elastomers, gels, and compositions thereof. Exemplary BCPMONs include (block co-polymer)-(metal organic cage) conjugates (BCPMOCs), (block co-polymer)-(metal organic paddlewheel) conjugates, and (block co-polymer)-(metal organic square) conjugates, such as BCPMONs of Formula (A), (B), or (C). Also described herein are macromonomers for preparing the BCPMONs; thermoplastic elastomers, gels, and compositions involving the BCPMONs; methods of preparing the BCPMONs, thermoplastic elastomers, gels, and compositions; and methods of using the BCPMONs, thermoplastic elastomers, gels, and compositions.

  本公开提供（嵌段共聚物）-（金属有机框架）共轭物（BCPMOFs），例如（嵌段共聚物）-（金属有机纳米结构）共轭物（BCPMONs），以及热塑性弹性体、凝胶和它们的组合物。示例BCPMONs包括（嵌段共聚物）-（金属有机笼）共轭物（BCPMOCs），（嵌段共聚物）-（金属有机风车）共轭物和（嵌段共聚物）-（金属有机方形）共轭物，例如公式（A）、（B）或（C）的BCPMONs。还描述了用于制备BCPMONs的大单体；涉及BCPMONs的热塑性弹性体、凝胶和组合物；制备BCPMONs、热塑性弹性体、凝胶和组合物的方法；以及使用BCPMONs、热塑性弹性体、凝胶和组合物的方法。