benzyl tetraethylphosphorodiamidite | 66954-57-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: benzyl tetraethylphosphorodiamidite
• 英文别名: N-[diethylamino(phenylmethoxy)phosphanyl]-N-ethylethanamine
• CAS: 66954-57-2
• 化学式: C₁₅H₂₇N₂OP
• 分子量: 282.366
• InChiKey: NAYVBFYORGONRM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  19
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  15.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  benzyl tetraethylphosphorodiamidite 生成 氟甲苯
  参考文献：
  名称：

  Advances in Trifluoromethylating Phosphorus Compounds

  摘要：

  DOI：

  10.1080/10426509608545224
• 作为产物：
  描述：

  六乙基亚磷酸胺 以 1,4-二氧六环 为溶剂， 反应 720.0h， 生成 benzyl tetraethylphosphorodiamidite
  参考文献：
  名称：

  Dismutation of Diamidoarylphosphites

  摘要：

  Some examples of spontaneous dismutation of diamidoarylphosphites in different solvents were studied, and features of the process were revealed.

  DOI：

  10.1080/714040960

文献信息

• Two-step phosphorus-mediated substitution of hydroxy groups in selected primary alcohols for fluorinated alkyl or aryl substituents: the molecular structure of 1,1-bis(fluorosulfonyl)-1-fluoro-2-phenylethane
  作者：Alexander Kolomeitsev、Alexander Shtarev、Kyrill Chabanenko、Tatjana Savina、Yurii Yagupolskii、Alexander Shtarev、Kyrill Chabanenko、Yurii Yagupolskii、Michaela Görg、Jan Przyborowski、Enno Lork、Gerd-Volker Röschenthaler

  DOI：10.1039/a707757b

  日期：——

  In an Arbuzov type reaction, amido phosphites (Et2N)2- PORand a broad range of halofluoro organic halides (X = Cl, Br) formed the corresponding alkylated derivatives R1–R2 [R1 = Bn, R2 = C(SO2F)3, CCl2F, CCl2CF3, CBr2F, C(CF3)3, C6F5; R1 = Et, CH2CF3, Me, R2 = CCl2CF3], whereas with FC(SO2F)3 and loss of SO2, BnCF(SO2F)2 was obtained, as shown by X-ray crystallography.

  在阿尔布佐夫反应中，胺基磷酸酯（Et2N）2-POR和一系列氯氟有机卤化物（X = Cl, Br）形成了相应的烷基化衍生物R1–R2 [R1 = Bn，R2 = C(SO2F)3, CCl2F, CCl2CF3, CBr2F, C(CF3)3, C6F5；R1 = Et, CH2CF3, Me，R2 = CCl2CF3]。而使用FC(SO2F)3并失去SO2，则得到BnCF(SO2F)2，这一点通过X射线晶体学证实。
• A Convenient Method for the Transformation of Alcohols into Alkyl Trifluoromethyl Sulfides
  作者：A. A. Kolomeitsev、K. Yu. Chabanenko、G. -V. Röschenthaler、Yu. L. Yagupolskii

  DOI：10.1055/s-1994-25422

  日期：——

  Alkyl trifluoromethyl sulfides are prepared by phosphitylation of alcohols or α-hydroxy esters using bis(diethylamido)chlorophosphite followed by the reaction with bis(trifluoromethyl) disulfide under extremely mild conditions in near by quantitative yields.

  烷基三氟甲基硫化物通过使用双（二乙酰胺）氯磷酸酯对醇或α-羟基酯进行磷酸化，随后在极温和的条件下与双（三氟甲基）二硫反应制备，产率接近定量。
• Synthesis of myo-inositol 4,6-cyclic,1,5-trisphosphate, a conformationally restricted analogue of myo-inositol 1,4,5-trisphosphate
  作者：Stéphanie Ballereau、Stéphane N. Poirier、Gaetan Guillemette、Bernard Spiess、Gilbert Schlewer

  DOI：10.1039/a800311d

  日期：——

  myo-Inositol 4,6-cyclic,1,5-trisphosphate 2 has been prepared starting from myo-inositol. The suitably protected intermediates, obtained by judicious selective protections and deprotections, have been phosphorylated. Final one-pot deprotection gives the expected, conformationally restricted, analogue of myo-inositol 1,4,5-trisphosphate. The physico-chemical behaviour of this derivative could explain its biological inactivity.

  肌醇 4,6-环,1,5-三磷酸肌醇 2 是由肌醇开始制备的。通过明智的选择性保护和脱保护得到的适当保护的中间体已被磷酸化。最后通过一锅脱保护，得到了肌醇 1,4,5-三磷酸酯的预期构象受限类似物。这种衍生物的物理化学行为可以解释其生物活性不强的原因。
• 2' ,5' -Oligoadenylate analogs
  申请人：Koizumi Makoto

  公开号：US20050261235A1

  公开（公告）日：2005-11-24

  A 2-5A analog represented by the formula (1): wherein m is 0 or 1; n is 0 to 2; R 1 represents an alkoxy group having from 1 to 6 carbon atoms which may be substituted, an unprotected mercapto group, a mercapto group protected by a nucleic acid synthesis protecting group, or an alkylthio group having from 1 to 4 carbon atoms which may be substituted; R 2 , R 3 , R 4 , R 5 and R 6 represent an unprotected hydroxyl group, a hydroxyl group protected by a nucleic acid synthesis protecting group, an alkoxy group having from 1 to 6 carbon atoms which may be substituted, an unprotected mercapto group, a mercapto group protected by a nucleic acid synthesis protecting group, or an alkylthio group having from 1 to 4 carbon atoms which may be substituted; R 7 represents an oxygen atom, or a —O(CH 2 CH 2 O)q-group, wherein q is 2 to 6; R 8 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms which may be substituted, or a 5′-phosphorylated oligonucleotide analog which has one hydroxyl group removed from the 5′-phosphoric acid group; E 1 , E 2 , E 3 and E 4 represent a naturally occurring or modified nucleic acid unit, or a pharmacologically acceptable salt thereof.

  一种由公式（1）表示的2-5A模拟物，其中m为0或1；n为0至2；R1表示具有1至6个碳原子的烷氧基，可以被取代，未保护的巯基，通过核酸合成保护基保护的巯基，或者具有1至4个碳原子的烷硫基，可以被取代；R2、R3、R4、R5和R6表示未保护的羟基，通过核酸合成保护基保护的羟基，具有1至6个碳原子的烷氧基，可以被取代，未保护的巯基，通过核酸合成保护基保护的巯基，或者具有1至4个碳原子的烷硫基，可以被取代；R7表示氧原子，或者-O(CH2CH2O)q-基团，其中q为2至6；R8表示氢原子，具有1至6个碳原子的烷基，可以被取代，或者从5'-磷酸基团中去除一个羟基的5'-磷酸寡核苷酸类似物；E1、E2、E3和E4表示天然或修饰的核酸单元，或其药理学上可接受的盐。
• Method of treating a tumor or a viral disease by administering a 2' , 5' -oligoadenylate analog
  申请人：Koizumi Makoto

  公开号：US20100035976A1

  公开（公告）日：2010-02-11

  A method of treating a tumor or a viral disease by administering to a human the following 2′,5′-oligoadenylate analog: Wherein m is 0; n is 0 or 1; R 1 is alkoxy substituted by hydroxyl, mercapto, alkylthio substituted by hydroxyl or X 1 —X 2 —X 3 —S—; R 2 , R 3 , R 4 , R 5 and R 6 are hydroxyl, mercapto, alkylthio substituted by hydroxyl or X 1 —X 2 —X 3 —S—; R 7 is oxygen, sulfur, —NH—, or —O(CH 2 CH 2 O)q-, wherein q is 2 to 6, or oxyalkyleneoxy; R 8 is hydrogen or a 5′-phosphorylated oligonucleotide which has one hydroxyl removed from the 5′-phosphoric acid; E 1 is K 2 ; E 2 is K 1 ; E 3 is K 2 or K 3 and E 4 is K 1 , K 2 or K 3 ; K 1 is K 2 is K 3 is B is adeninyl; A is alkylene; D is alkyl or alkenyl; X 1 is alkyl or phenyl; X 2 is —C(═O)O—, —OC(═O)— or —C(═O)S—; and X 3 is alkylene.

  一种通过向人体内注射以下2′，5′-寡腺苷酸类似物来治疗肿瘤或病毒性疾病的方法：其中m为0；n为0或1；R1为烷氧基，被羟基，巯基，被羟基的烷基硫代基或X1—X2—X3—S—取代的烷氧基；R2，R3，R4，R5和R6为羟基，巯基，被羟基的烷基硫代基或X1—X2—X3—S—；R7为氧，硫，—NH—，或—O(CH2CH2O)q-，其中q为2至6，或氧烷氧基；R8为氢或一个5′-磷酸寡核苷酸，其5′-磷酸上有一个羟基被去除；E1为K2；E2为K1；E3为K2或K3，E4为K1，K2或K3；K1，K2和K3为B为腺苷基；A为烷基；D为烷基或烯基；X1为烷基或苯基；X2为—C(═O)O—，—OC(═O)—或—C(═O)S—；X3为烷基。